Page last updated: 2024-11-06

7-hydroxystaurosporine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

7-Hydroxystaurosporine is a potent and selective inhibitor of protein kinase C (PKC). It was first isolated from the bacterium Streptomyces staphylous in 1987. The compound is a derivative of staurosporine, a natural product with a wide range of biological activities, including inhibition of protein kinases. 7-Hydroxystaurosporine has been shown to be more selective for PKC than staurosporine and has been used as a research tool to study the role of PKC in various cellular processes. 7-Hydroxystaurosporine is also being investigated for its potential therapeutic applications, particularly in the treatment of cancer. The compound has shown anti-proliferative activity against a variety of tumor cell lines, and it has been shown to induce apoptosis in cancer cells. The mechanism of action of 7-hydroxystaurosporine is not fully understood, but it is thought to involve inhibition of PKC and other protein kinases, which leads to disruption of cell signaling pathways that are essential for cell growth and survival. Further research is needed to investigate the potential therapeutic uses of this compound.'

Cross-References

ID SourceID
PubMed CID72271
CHEMBL ID1236539
SCHEMBL ID1551632
MeSH IDM0154702

Synonyms (36)

Synonym
CHEMBL1236539
9,9h-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo [3,4-j][1,7]-benzodiazonin-1-one, 2,3,10,11,12,13- hexahydro-3-hydroxy-10-methoxy-9-methyl- 11-(methylamino)-, [3r-(3.alpha., 9.beta., 10.alpha.,11.alpha., 13.beta.)]-
nsc-638850
(+)-ucn-01
2,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl- 11-(methylamino)-9,13-epoxy-1h,9h-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]-benzodiazonin-1-one
NCI60_012974
kw-2401
krx-0601
ucn01
nsc 638850
9,13-epoxy-1h,9h-diindolo(1,2,3-gh:3',2',1'-lm)pyrrolo(3,4-j)(1,7)benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-11-(methylamino)-, (3-alpha,9-beta,10-alpha,11-alpha,13-beta)-(+)-
8,12-epoxy-1h,8h-2,7b,12a-triazadibenzo(a,g)cyclonona(cde)triinden-1-one, 2,3,9,10,11,12-hexahydro-3-hydroxy-9-methoxy-8-methyl-10-(methylamino)-
9,13-epoxy-1h,9h-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-11-(methylamino)-, (3r,9s,10r,11r,13r)-
7-hydroxystaurosporine
ucn 01
hydroxy-methoxy-methyl-(methylamino)[?]one
NSC638850 ,
UCN ,
DB01933
1OKZ ,
bdbm17054
(5s,6r,7r,9r,16r)-16-hydroxy-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5h,14h-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
7bu5h4v94a ,
unii-7bu5h4v94a
9,13-epoxy-1h,9h-diindolo(1,2,3-gh:3',2',1'-lm)pyrrolo(3,4-j)(1,7)benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-11-(methylamino)-, (3r,9s,10r,11r,13r)-
7-hydroxystaurosporine [who-dd]
gtpl7907
krx0601
(5s,6r,7r,9r,16r)-16-hydroxy-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-14(5h)-one
SCHEMBL1551632
DTXSID20150238
J-002880
AKOS030230764
(5s,6r,7r,9r,16r)-16-hydroxy-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[
(2s,3r,4r,6r,18r)-18-hydroxy-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one
Q27074035

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" These pharmacokinetic parameters were dose-independent in mice and rats."( Pharmacokinetics and pharmacodynamics of a novel protein kinase inhibitor, UCN-01.
Akinaga, S; Akiyama, T; Fuse, E; Kobayashi, H; Kobayashi, S; Kurata, N; Kuwabara, T; Tanii, H; Yamaguchi, K, 1999
)
0.3
"The pharmacokinetic studies showed that UCN-01 has a high clearance and large distribution volume in various experimental animals, and its disposition is linear over the range of doses tested."( Pharmacokinetics and pharmacodynamics of a novel protein kinase inhibitor, UCN-01.
Akinaga, S; Akiyama, T; Fuse, E; Kobayashi, H; Kobayashi, S; Kurata, N; Kuwabara, T; Tanii, H; Yamaguchi, K, 1999
)
0.3
" Pharmacokinetic analysis under conditions assuming rapid equilibrium of protein binding and incorporating the dissociation rate was conducted."( Physiological modeling of altered pharmacokinetics of a novel anticancer drug, UCN-01 (7-hydroxystaurosporine), caused by slow dissociation of UCN-01 from human alpha1-acid glycoprotein.
Fuse, E; Hashimoto, A; Kobayashi, S; Kuwabara, T; Sato, N; Sugiyama, Y; Tanii, H, 2000
)
0.53
" Here, we examined the role of protein binding as a determinant of the pharmacokinetic behavior of UCN-01 in patients."( Effects of alpha1-acid glycoprotein on the clinical pharmacokinetics of 7-hydroxystaurosporine.
Acharya, MR; Chen, H; Figg, WD; Headlee, D; Kuwabara, T; Messmann, RA; Murgo, AJ; Sausville, EA; Senderowicz, AM; Sparreboom, A; Venzon, DJ, 2004
)
0.56
"The results suggest the following: (1) that extensive binding to AAG may explain, in part, the unique pharmacokinetic profile of UCN-01 described previously with a small volume of distribution and slow systemic clearance, and (2) that measurement of total UCN-01 concentrations in plasma is a poor surrogate for that of the pharmacologically active fraction unbound drug."( Effects of alpha1-acid glycoprotein on the clinical pharmacokinetics of 7-hydroxystaurosporine.
Acharya, MR; Chen, H; Figg, WD; Headlee, D; Kuwabara, T; Messmann, RA; Murgo, AJ; Sausville, EA; Senderowicz, AM; Sparreboom, A; Venzon, DJ, 2004
)
0.56
" Median plasma UCN-01 half-life (T(1/2)) was 405 hours."( Modulation of cell cycle progression in human tumors: a pharmacokinetic and tumor molecular pharmacodynamic study of cisplatin plus the Chk1 inhibitor UCN-01 (NSC 638850).
Beaulieu, B; Beelen, AP; Eastman, A; Ernstoff, MS; Johnston, N; Lewis, LD; Olszanski, AJ; Perez, RP; Rhodes, CH, 2006
)
0.33
" The long half-life (292."( Phase I and pharmacokinetic study of UCN-01 in combination with irinotecan in patients with solid tumors.
Baker, SD; Carducci, MA; Dancey, J; Donehower, RC; Hidalgo, M; Jimeno, A; Laheru, DA; Messersmith, WA; Purcell, T; Rudek, MA, 2008
)
0.35
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
"Our goal was to determine the cytotoxicity of 7-OH-hydroxystaurosporine (UCN-01) as a single agent and in combination with cis-diamminedichloroplatinum(II) (CDDP) in a panel of ovarian carcinoma cells."( UCN-01 in ovary cancer cells: effective as a single agent and in combination with cis-diamminedichloroplatinum(II)independent of p53 status.
Aghajanian, C; Husain, A; Rosales, N; Schwartz, GK; Spriggs, DR; Yan, XJ, 1997
)
0.3
" The clinical evaluation of UCN-01 combined with 5-fluoropyrimidines may be of interest."( Biochemical and molecular effects of UCN-01 in combination with 5-fluorodeoxyuridine in A431 human epidermoid cancer cells.
Danenberg, KD; Danenberg, PV; Grem, JL; Kao, V; Nguyen, D, 2002
)
0.31
" We designed a phase I clinical trial of FU in combination with UCN-01."( Phase I trial of the cyclin-dependent kinase inhibitor and protein kinase C inhibitor 7-hydroxystaurosporine in combination with Fluorouracil in patients with advanced solid tumors.
Gonen, M; Ilson, DI; Kaubisch, A; Kelsen, DP; Kemeny, N; Kortmansky, J; Maki, RG; O'reilly, E; Saltz, LB; Schwartz, GK; Shah, MA; Sowers, R; Tong, W; Weyerbacher, A; Yi, S, 2005
)
0.55
"We escalated the weekly FU dose to 2,600 mg/m(2) in combination with once a month infusions of UCN-01."( Phase I trial of the cyclin-dependent kinase inhibitor and protein kinase C inhibitor 7-hydroxystaurosporine in combination with Fluorouracil in patients with advanced solid tumors.
Gonen, M; Ilson, DI; Kaubisch, A; Kelsen, DP; Kemeny, N; Kortmansky, J; Maki, RG; O'reilly, E; Saltz, LB; Schwartz, GK; Shah, MA; Sowers, R; Tong, W; Weyerbacher, A; Yi, S, 2005
)
0.55
" The recommended phase II dose of FU in combination with monthly UCN-01 is 2,600 mg/m(2)."( Phase I trial of the cyclin-dependent kinase inhibitor and protein kinase C inhibitor 7-hydroxystaurosporine in combination with Fluorouracil in patients with advanced solid tumors.
Gonen, M; Ilson, DI; Kaubisch, A; Kelsen, DP; Kemeny, N; Kortmansky, J; Maki, RG; O'reilly, E; Saltz, LB; Schwartz, GK; Shah, MA; Sowers, R; Tong, W; Weyerbacher, A; Yi, S, 2005
)
0.55
" Therefore, we evaluated a pilot clinical trial of ara-C in combination with UCN-01 in patients with relapsed AML."( Pharmacodynamics of cytarabine alone and in combination with 7-hydroxystaurosporine (UCN-01) in AML blasts in vitro and during a clinical trial.
Andreeff, M; Cortes, J; Du, M; Estrov, Z; Gandhi, V; Plunkett, W; Sampath, D; Shi, Z, 2006
)
0.58
"APC and SN-38 exposure decreased when administered in combination with UCN-01."( Phase I and pharmacokinetic study of UCN-01 in combination with irinotecan in patients with solid tumors.
Baker, SD; Carducci, MA; Dancey, J; Donehower, RC; Hidalgo, M; Jimeno, A; Laheru, DA; Messersmith, WA; Purcell, T; Rudek, MA, 2008
)
0.35
" UCN-01, a non-selective Chk1 inhibitor, combined with irinotecan demonstrated activity in advanced TNBC in our Phase I study."( A phase II study of UCN-01 in combination with irinotecan in patients with metastatic triple negative breast cancer.
Bernard, PS; Brenin, CM; Cai, SR; Craig Lockhart, A; Creekmore, AN; Dancey, J; Doyle, LA; Ebbert, M; Ellis, MJ; Fracasso, PM; Guo, Z; Ma, CX; Mwandoro, T; Naughton, MJ; Petroni, GR; Picus, J; Piwnica-Worms, H; Pluard, TJ; Reed, J; Ryan, CE; Watson, M; Yarde, ER, 2013
)
0.39
"The ability of Tetra-O-methyl nordihydroguaiaretic acid (M4N) to induce rapid cell death in combination with Etoposide, Rapamycin, or UCN-01 was examined in LNCaP cells, both in cell culture and animal experiments."( Tetra-O-Methyl Nordihydroguaiaretic Acid Broadly Suppresses Cancer Metabolism and Synergistically Induces Strong Anticancer Activity in Combination with Etoposide, Rapamycin and UCN-01.
Huang, RC; Kimura, K, 2016
)
0.43

Bioavailability

ExcerptReferenceRelevance
" The AUC value was 15 micrograms min ml-1, giving a value for bioavailability of 13%."( Disposition in mice of 7-hydroxystaurosporine, a protein kinase inhibitor with antitumor activity.
Hill, DL; Posey, CF; Rose, LM; Tillery, KF, 1994
)
0.6

Dosage Studied

ExcerptRelevanceReference
" For mice dosed intravenously, subcutaneously, or by oral gavage with this compound, the maximum tolerated doses (MTD) were 20, 10, and > 100 mg/kg, respectively."( Disposition in mice of 7-hydroxystaurosporine, a protein kinase inhibitor with antitumor activity.
Hill, DL; Posey, CF; Rose, LM; Tillery, KF, 1994
)
0.6
" Cytotoxicity was determined from dose-response curves established by the Alamar blue vital dye indicator assay."( UCN-01 in ovary cancer cells: effective as a single agent and in combination with cis-diamminedichloroplatinum(II)independent of p53 status.
Aghajanian, C; Husain, A; Rosales, N; Schwartz, GK; Spriggs, DR; Yan, XJ, 1997
)
0.3
" However, a longer dosing period of UCN-01 increased the residence time in comparison with the shorter infusion."( The effect of different dosing schedules of UCN-01 on its pharmacokinetics and cardiohaemodynamics in dogs.
Imabeppu, S; Kobayashi, H; Kobayashi, S; Kurata, N; Kuwabara, T; Nitoh, M, 2000
)
0.31
" Further investigation into flavopiridol as a clinical agent should focus on alternative dosing schedules and the compound's potential use in combination chemotherapeutic regimens."( Seventy-two hour continuous infusion flavopiridol in relapsed and refractory mantle cell lymphoma.
Howard, OM; Kim, HH; Lin, TS; Neuberg, DS; Shipp, MA, 2002
)
0.31
"25 mumol/L UCN-01, glucose transport is inhibited 66, 29, and 26% at insulin concentrations of 10, 50, and 100,000 (100K) microunits/mL respectively, thus shifting the dose-response curve to the right."( 7-hydroxystaurosporine (UCN-01) inhibition of Akt Thr308 but not Ser473 phosphorylation: a basis for decreased insulin-stimulated glucose transport.
Cushman, SW; Kondapaka, SB; Sausville, EA; Yver, DR; Zarnowski, M, 2004
)
1.77
" Cell proliferation was determined from dose-response curves."( AG490 influences UCN-01-induced cytotoxicity in glioma cells in a p53-dependent fashion, correlating with effects on BAX cleavage and BAD phosphorylation.
Jane, EP; Pollack, IF; Premkumar, DR, 2007
)
0.34
" Pyroptosis assessment leads to a fast FMF diagnosis while combining pyroptosis and IL-1β dosage renders UCN-01-based assays highly sensitive and specific."( Fast diagnostic test for familial Mediterranean fever based on a kinase inhibitor.
Abbas, F; Belot, A; Duquesne, A; Durupt, S; Fauter, M; Georgin-Lavialle, S; Gerfaud-Valentin, M; Giurgea, I; Grateau, G; Henry, T; Hot, A; Jamilloux, Y; Magnotti, F; Malsot, T; Martin, A; Rabilloud, M; Savey, L; Sève, P, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase Chk1Homo sapiens (human)IC50 (µMol)0.00990.00010.45308.8300AID1197204
Serine/threonine-protein kinase Chk1Homo sapiens (human)Ki0.00560.00050.23480.6590AID1797591
3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)IC50 (µMol)0.00550.00251.45139.0000AID1797581; AID1797582
Cyclin-dependent kinase 1Homo sapiens (human)Ki0.06250.00101.25515.0000AID1797592
Cyclin-dependent kinase 4Homo sapiens (human)Ki3.60000.00060.73693.6000AID1797593
Cyclin-A2Homo sapiens (human)Ki0.06250.00100.70075.0000AID1797592
G1/S-specific cyclin-D1Homo sapiens (human)Ki3.60000.00060.66543.6000AID1797593
Cyclin-dependent kinase 2Homo sapiens (human)Ki0.06250.00050.64275.0000AID1797592
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (163)

Processvia Protein(s)Taxonomy
DNA damage checkpoint signalingSerine/threonine-protein kinase Chk1Homo sapiens (human)
G2/M transition of mitotic cell cycleSerine/threonine-protein kinase Chk1Homo sapiens (human)
inner cell mass cell proliferationSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA replicationSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA repairSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromatin remodelingSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase Chk1Homo sapiens (human)
apoptotic processSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleus organizationSerine/threonine-protein kinase Chk1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of double-strand break repair via homologous recombinationSerine/threonine-protein kinase Chk1Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of cell population proliferationSerine/threonine-protein kinase Chk1Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk1Homo sapiens (human)
mitotic G2/M transition checkpointSerine/threonine-protein kinase Chk1Homo sapiens (human)
positive regulation of cell cycleSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of gene expression, epigeneticSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of mitotic nuclear divisionSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of mitotic centrosome separationSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of G0 to G1 transitionSerine/threonine-protein kinase Chk1Homo sapiens (human)
cellular response to mechanical stimulusSerine/threonine-protein kinase Chk1Homo sapiens (human)
cellular response to caffeineSerine/threonine-protein kinase Chk1Homo sapiens (human)
replicative senescenceSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase Chk1Homo sapiens (human)
apoptotic process involved in developmentSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of DNA biosynthetic processSerine/threonine-protein kinase Chk1Homo sapiens (human)
intracellular signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
type B pancreatic cell development3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of protein kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
hyperosmotic response3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
epidermal growth factor receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
insulin receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of phospholipase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic process3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cell migration3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
calcium-mediated signaling3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
actin cytoskeleton organization3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
T cell costimulation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
activation of protein kinase B activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cellular response to insulin stimulus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of toll-like receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
regulation of canonical NF-kappaB signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
regulation of mast cell degranulation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of angiogenesis3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein autophosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cellular response to epidermal growth factor stimulus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
extrinsic apoptotic signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of protein localization to plasma membrane3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of sprouting angiogenesis3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of endothelial cell apoptotic process3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
intracellular signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
microtubule cytoskeleton organizationCyclin-dependent kinase 1Homo sapiens (human)
DNA replicationCyclin-dependent kinase 1Homo sapiens (human)
DNA repairCyclin-dependent kinase 1Homo sapiens (human)
chromatin remodelingCyclin-dependent kinase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IICyclin-dependent kinase 1Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
apoptotic processCyclin-dependent kinase 1Homo sapiens (human)
DNA damage responseCyclin-dependent kinase 1Homo sapiens (human)
mitotic nuclear membrane disassemblyCyclin-dependent kinase 1Homo sapiens (human)
centrosome cycleCyclin-dependent kinase 1Homo sapiens (human)
pronuclear fusionCyclin-dependent kinase 1Homo sapiens (human)
response to xenobiotic stimulusCyclin-dependent kinase 1Homo sapiens (human)
response to toxic substanceCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of gene expressionCyclin-dependent kinase 1Homo sapiens (human)
negative regulation of gene expressionCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
regulation of Schwann cell differentiationCyclin-dependent kinase 1Homo sapiens (human)
response to amineCyclin-dependent kinase 1Homo sapiens (human)
response to activityCyclin-dependent kinase 1Homo sapiens (human)
cell migrationCyclin-dependent kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
chromosome condensationCyclin-dependent kinase 1Homo sapiens (human)
epithelial cell differentiationCyclin-dependent kinase 1Homo sapiens (human)
animal organ regenerationCyclin-dependent kinase 1Homo sapiens (human)
protein localization to kinetochoreCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of protein import into nucleusCyclin-dependent kinase 1Homo sapiens (human)
regulation of circadian rhythmCyclin-dependent kinase 1Homo sapiens (human)
negative regulation of apoptotic processCyclin-dependent kinase 1Homo sapiens (human)
response to ethanolCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of DNA replicationCyclin-dependent kinase 1Homo sapiens (human)
regulation of embryonic developmentCyclin-dependent kinase 1Homo sapiens (human)
response to cadmium ionCyclin-dependent kinase 1Homo sapiens (human)
response to copper ionCyclin-dependent kinase 1Homo sapiens (human)
symbiont entry into host cellCyclin-dependent kinase 1Homo sapiens (human)
fibroblast proliferationCyclin-dependent kinase 1Homo sapiens (human)
rhythmic processCyclin-dependent kinase 1Homo sapiens (human)
response to axon injuryCyclin-dependent kinase 1Homo sapiens (human)
cell divisionCyclin-dependent kinase 1Homo sapiens (human)
ventricular cardiac muscle cell developmentCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of mitotic sister chromatid segregationCyclin-dependent kinase 1Homo sapiens (human)
protein-containing complex assemblyCyclin-dependent kinase 1Homo sapiens (human)
cellular response to hydrogen peroxideCyclin-dependent kinase 1Homo sapiens (human)
ERK1 and ERK2 cascadeCyclin-dependent kinase 1Homo sapiens (human)
cellular response to organic cyclic compoundCyclin-dependent kinase 1Homo sapiens (human)
Golgi disassemblyCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of protein localization to nucleusCyclin-dependent kinase 1Homo sapiens (human)
regulation of attachment of mitotic spindle microtubules to kinetochoreCyclin-dependent kinase 1Homo sapiens (human)
microtubule cytoskeleton organization involved in mitosisCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of mitochondrial ATP synthesis coupled electron transportCyclin-dependent kinase 1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingCyclin-dependent kinase 1Homo sapiens (human)
protein deubiquitinationCyclin-dependent kinase 1Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of cell population proliferationCyclin-dependent kinase 4Homo sapiens (human)
response to xenobiotic stimulusCyclin-dependent kinase 4Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of fibroblast proliferationCyclin-dependent kinase 4Homo sapiens (human)
cell divisionCyclin-dependent kinase 4Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 4Homo sapiens (human)
regulation of transcription initiation by RNA polymerase IICyclin-dependent kinase 4Homo sapiens (human)
regulation of type B pancreatic cell proliferationCyclin-dependent kinase 4Homo sapiens (human)
cellular response to lipopolysaccharideCyclin-dependent kinase 4Homo sapiens (human)
cellular response to interleukin-4Cyclin-dependent kinase 4Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateCyclin-dependent kinase 4Homo sapiens (human)
cellular response to ionomycinCyclin-dependent kinase 4Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 4Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
signal transductionCyclin-dependent kinase 4Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-A2Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-A2Homo sapiens (human)
regulation of DNA replicationCyclin-A2Homo sapiens (human)
DNA-templated transcriptionCyclin-A2Homo sapiens (human)
Ras protein signal transductionCyclin-A2Homo sapiens (human)
animal organ regenerationCyclin-A2Homo sapiens (human)
response to glucagonCyclin-A2Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusCyclin-A2Homo sapiens (human)
post-translational protein modificationCyclin-A2Homo sapiens (human)
cellular response to leptin stimulusCyclin-A2Homo sapiens (human)
cell cycle G1/S phase transitionCyclin-A2Homo sapiens (human)
positive regulation of DNA-templated transcriptionCyclin-A2Homo sapiens (human)
positive regulation of fibroblast proliferationCyclin-A2Homo sapiens (human)
cell divisionCyclin-A2Homo sapiens (human)
cellular response to cocaineCyclin-A2Homo sapiens (human)
cellular response to luteinizing hormone stimulusCyclin-A2Homo sapiens (human)
cellular response to estradiol stimulusCyclin-A2Homo sapiens (human)
cellular response to hypoxiaCyclin-A2Homo sapiens (human)
cellular response to nitric oxideCyclin-A2Homo sapiens (human)
cochlea developmentCyclin-A2Homo sapiens (human)
cellular response to insulin-like growth factor stimulusCyclin-A2Homo sapiens (human)
positive regulation of DNA biosynthetic processCyclin-A2Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityCyclin-A2Homo sapiens (human)
mitotic cell cycle phase transitionCyclin-A2Homo sapiens (human)
G1/S transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIG1/S-specific cyclin-D1Homo sapiens (human)
re-entry into mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of protein phosphorylationG1/S-specific cyclin-D1Homo sapiens (human)
DNA damage responseG1/S-specific cyclin-D1Homo sapiens (human)
lactationG1/S-specific cyclin-D1Homo sapiens (human)
response to xenobiotic stimulusG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
Wnt signaling pathwayG1/S-specific cyclin-D1Homo sapiens (human)
neuron differentiationG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of epithelial cell differentiationG1/S-specific cyclin-D1Homo sapiens (human)
endoplasmic reticulum unfolded protein responseG1/S-specific cyclin-D1Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingG1/S-specific cyclin-D1Homo sapiens (human)
mammary gland epithelial cell proliferationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of mammary gland epithelial cell proliferationG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of neuron apoptotic processG1/S-specific cyclin-D1Homo sapiens (human)
response to leptinG1/S-specific cyclin-D1Homo sapiens (human)
fat cell differentiationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
cell divisionG1/S-specific cyclin-D1Homo sapiens (human)
mammary gland alveolus developmentG1/S-specific cyclin-D1Homo sapiens (human)
response to UV-AG1/S-specific cyclin-D1Homo sapiens (human)
liver regenerationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICyclin-dependent kinase 2Homo sapiens (human)
DNA replicationCyclin-dependent kinase 2Homo sapiens (human)
DNA repairCyclin-dependent kinase 2Homo sapiens (human)
chromatin remodelingCyclin-dependent kinase 2Homo sapiens (human)
DNA-templated transcriptionCyclin-dependent kinase 2Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 2Homo sapiens (human)
potassium ion transportCyclin-dependent kinase 2Homo sapiens (human)
centriole replicationCyclin-dependent kinase 2Homo sapiens (human)
Ras protein signal transductionCyclin-dependent kinase 2Homo sapiens (human)
regulation of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of cell population proliferationCyclin-dependent kinase 2Homo sapiens (human)
peptidyl-serine phosphorylationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of heterochromatin formationCyclin-dependent kinase 2Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA-templated DNA replication initiationCyclin-dependent kinase 2Homo sapiens (human)
telomere maintenance in response to DNA damageCyclin-dependent kinase 2Homo sapiens (human)
post-translational protein modificationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA replicationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionCyclin-dependent kinase 2Homo sapiens (human)
centrosome duplicationCyclin-dependent kinase 2Homo sapiens (human)
cell divisionCyclin-dependent kinase 2Homo sapiens (human)
meiotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
cellular response to nitric oxideCyclin-dependent kinase 2Homo sapiens (human)
cellular senescenceCyclin-dependent kinase 2Homo sapiens (human)
regulation of anaphase-promoting complex-dependent catabolic processCyclin-dependent kinase 2Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
signal transductionCyclin-dependent kinase 2Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 2Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
protein kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein domain specific bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
histone H3T11 kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine/threonine kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
3-phosphoinositide-dependent protein kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
ATP binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
phospholipase activator activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
phospholipase binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein serine kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
virus receptor activityCyclin-dependent kinase 1Homo sapiens (human)
chromatin bindingCyclin-dependent kinase 1Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein bindingCyclin-dependent kinase 1Homo sapiens (human)
ATP bindingCyclin-dependent kinase 1Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 1Homo sapiens (human)
kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 1Homo sapiens (human)
Hsp70 protein bindingCyclin-dependent kinase 1Homo sapiens (human)
histone kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 4Homo sapiens (human)
protein bindingCyclin-dependent kinase 4Homo sapiens (human)
ATP bindingCyclin-dependent kinase 4Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-dependent kinase 4Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 4Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 4Homo sapiens (human)
protein bindingCyclin-A2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-A2Homo sapiens (human)
protein kinase bindingCyclin-A2Homo sapiens (human)
protein domain specific bindingCyclin-A2Homo sapiens (human)
transcription corepressor activityG1/S-specific cyclin-D1Homo sapiens (human)
protein kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
protein bindingG1/S-specific cyclin-D1Homo sapiens (human)
enzyme bindingG1/S-specific cyclin-D1Homo sapiens (human)
protein kinase bindingG1/S-specific cyclin-D1Homo sapiens (human)
histone deacetylase bindingG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activator activityG1/S-specific cyclin-D1Homo sapiens (human)
proline-rich region bindingG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG1/S-specific cyclin-D1Homo sapiens (human)
histone kinase activityCyclin-dependent kinase 2Homo sapiens (human)
magnesium ion bindingCyclin-dependent kinase 2Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein bindingCyclin-dependent kinase 2Homo sapiens (human)
ATP bindingCyclin-dependent kinase 2Homo sapiens (human)
protein domain specific bindingCyclin-dependent kinase 2Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (51)

Processvia Protein(s)Taxonomy
chromosome, telomeric regionSerine/threonine-protein kinase Chk1Homo sapiens (human)
condensed nuclear chromosomeSerine/threonine-protein kinase Chk1Homo sapiens (human)
extracellular spaceSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase Chk1Homo sapiens (human)
replication forkSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase Chk1Homo sapiens (human)
centrosomeSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytosolSerine/threonine-protein kinase Chk1Homo sapiens (human)
intracellular membrane-bounded organelleSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromatinSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein-containing complexSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytoplasm3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytosol3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
plasma membrane3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
focal adhesion3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
postsynaptic density3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytoplasmic vesicle3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cell projection3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
mitochondrial matrixCyclin-dependent kinase 1Homo sapiens (human)
chromosome, telomeric regionCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 1Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 1Homo sapiens (human)
mitochondrionCyclin-dependent kinase 1Homo sapiens (human)
endoplasmic reticulum membraneCyclin-dependent kinase 1Homo sapiens (human)
centrosomeCyclin-dependent kinase 1Homo sapiens (human)
cytosolCyclin-dependent kinase 1Homo sapiens (human)
spindle microtubuleCyclin-dependent kinase 1Homo sapiens (human)
membraneCyclin-dependent kinase 1Homo sapiens (human)
midbodyCyclin-dependent kinase 1Homo sapiens (human)
extracellular exosomeCyclin-dependent kinase 1Homo sapiens (human)
mitotic spindleCyclin-dependent kinase 1Homo sapiens (human)
cyclin A1-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin A2-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin B1-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 1Homo sapiens (human)
cytoplasmCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 4Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 4Homo sapiens (human)
nucleolusCyclin-dependent kinase 4Homo sapiens (human)
cytosolCyclin-dependent kinase 4Homo sapiens (human)
bicellular tight junctionCyclin-dependent kinase 4Homo sapiens (human)
nuclear membraneCyclin-dependent kinase 4Homo sapiens (human)
cyclin D1-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin D2-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin D3-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 4Homo sapiens (human)
chromatinCyclin-dependent kinase 4Homo sapiens (human)
transcription regulator complexCyclin-dependent kinase 4Homo sapiens (human)
nucleusCyclin-dependent kinase 4Homo sapiens (human)
cytoplasmCyclin-dependent kinase 4Homo sapiens (human)
female pronucleusCyclin-A2Homo sapiens (human)
male pronucleusCyclin-A2Homo sapiens (human)
nucleusCyclin-A2Homo sapiens (human)
nucleoplasmCyclin-A2Homo sapiens (human)
cytoplasmCyclin-A2Homo sapiens (human)
cytosolCyclin-A2Homo sapiens (human)
cyclin A2-CDK1 complexCyclin-A2Homo sapiens (human)
cyclin A2-CDK2 complexCyclin-A2Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-A2Homo sapiens (human)
nucleusCyclin-A2Homo sapiens (human)
centrosomeCyclin-A2Homo sapiens (human)
cytoplasmCyclin-A2Homo sapiens (human)
nucleusG1/S-specific cyclin-D1Homo sapiens (human)
nucleoplasmG1/S-specific cyclin-D1Homo sapiens (human)
cytosolG1/S-specific cyclin-D1Homo sapiens (human)
bicellular tight junctionG1/S-specific cyclin-D1Homo sapiens (human)
nuclear membraneG1/S-specific cyclin-D1Homo sapiens (human)
cyclin D1-CDK4 complexG1/S-specific cyclin-D1Homo sapiens (human)
cyclin D1-CDK6 complexG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexG1/S-specific cyclin-D1Homo sapiens (human)
transcription repressor complexG1/S-specific cyclin-D1Homo sapiens (human)
centrosomeG1/S-specific cyclin-D1Homo sapiens (human)
cytoplasmG1/S-specific cyclin-D1Homo sapiens (human)
nucleusG1/S-specific cyclin-D1Homo sapiens (human)
chromosome, telomeric regionCyclin-dependent kinase 2Homo sapiens (human)
condensed chromosomeCyclin-dependent kinase 2Homo sapiens (human)
X chromosomeCyclin-dependent kinase 2Homo sapiens (human)
Y chromosomeCyclin-dependent kinase 2Homo sapiens (human)
male germ cell nucleusCyclin-dependent kinase 2Homo sapiens (human)
nucleusCyclin-dependent kinase 2Homo sapiens (human)
nuclear envelopeCyclin-dependent kinase 2Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 2Homo sapiens (human)
cytoplasmCyclin-dependent kinase 2Homo sapiens (human)
endosomeCyclin-dependent kinase 2Homo sapiens (human)
centrosomeCyclin-dependent kinase 2Homo sapiens (human)
cytosolCyclin-dependent kinase 2Homo sapiens (human)
Cajal bodyCyclin-dependent kinase 2Homo sapiens (human)
cyclin A1-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin A2-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin E1-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin E2-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 2Homo sapiens (human)
transcription regulator complexCyclin-dependent kinase 2Homo sapiens (human)
cytoplasmCyclin-dependent kinase 2Homo sapiens (human)
nucleusCyclin-dependent kinase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID1345407Human protein kinase C alpha (Delta subfamily)1994Molecular pharmacology, Jun, Volume: 45, Issue:6
Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue.
AID1345382Human protein kinase C delta (Delta subfamily)1994Molecular pharmacology, Jun, Volume: 45, Issue:6
Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue.
AID1345650Human checkpoint kinase 1 (CHK1 subfamily)2000Cancer research, Apr-15, Volume: 60, Issue:8
The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1.
AID1345633Human glycogen synthase kinase 3 beta (GSK subfamily)2004Molecular cancer therapeutics, Oct, Volume: 3, Issue:10
Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide.
AID1345304Human mitogen-activated protein kinase 14 (p38 subfamily)2007Cancer cell, Feb, Volume: 11, Issue:2
p53-deficient cells rely on ATM- and ATR-mediated checkpoint signaling through the p38MAPK/MK2 pathway for survival after DNA damage.
AID1345648Human checkpoint kinase 2 (RAD53 family)2000Cancer research, Apr-15, Volume: 60, Issue:8
The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1.
AID1345650Human checkpoint kinase 1 (CHK1 subfamily)2007Cancer cell, Feb, Volume: 11, Issue:2
p53-deficient cells rely on ATM- and ATR-mediated checkpoint signaling through the p38MAPK/MK2 pathway for survival after DNA damage.
AID1345754Human microtubule affinity regulating kinase 1 (MARK subfamily)2000Cancer research, Apr-15, Volume: 60, Issue:8
The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1.
AID1345308Human protein kinase C beta (Alpha subfamily)1994Molecular pharmacology, Jun, Volume: 45, Issue:6
Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue.
AID1345717Human LCK proto-oncogene, Src family tyrosine kinase (Src family)2004Molecular cancer therapeutics, Oct, Volume: 3, Issue:10
Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide.
AID1345388Human 3-phosphoinositide dependent protein kinase 1 (PDK1 family)2002Oncogene, Mar-07, Volume: 21, Issue:11
Interference with PDK1-Akt survival signaling pathway by UCN-01 (7-hydroxystaurosporine).
AID1345650Human checkpoint kinase 1 (CHK1 subfamily)2004Molecular cancer therapeutics, Oct, Volume: 3, Issue:10
Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide.
AID1345397Human protein kinase C epsilon (Eta subfamily)1994Molecular pharmacology, Jun, Volume: 45, Issue:6
Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue.
AID1345307Human protein kinase C gamma (Alpha subfamily)1994Molecular pharmacology, Jun, Volume: 45, Issue:6
Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1197204Inhibition of CHK1 (unknown origin) using FAM-KKKVSRSGLYRSPSMPENLNRPR-COOH peptide substrate incubated for 1 hr by caliper microfluidic assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Identification of novel aminothiazole and aminothiadiazole conjugated cyanopyridines as selective CHK1 inhibitors.
AID1797581PDK1 Kinase Activity Assay from Article 10.1042/BJ20031119: \\Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition.\\2003The Biochemical journal, Oct-15, Volume: 375, Issue:Pt 2
Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition.
AID1797591Chk1 Enzymatic Assay from Article 10.1074/jbc.M201233200: \\Structural basis for Chk1 inhibition by UCN-01.\\2002The Journal of biological chemistry, Nov-29, Volume: 277, Issue:48
Structural basis for Chk1 inhibition by UCN-01.
AID1797592CDK Activity Assay. from Article 10.1074/jbc.M201233200: \\Structural basis for Chk1 inhibition by UCN-01.\\2002The Journal of biological chemistry, Nov-29, Volume: 277, Issue:48
Structural basis for Chk1 inhibition by UCN-01.
AID1797593CDK4 Activity Assay from Article 10.1074/jbc.M201233200: \\Structural basis for Chk1 inhibition by UCN-01.\\2002The Journal of biological chemistry, Nov-29, Volume: 277, Issue:48
Structural basis for Chk1 inhibition by UCN-01.
AID1797582PDK1 Kinase Activity Assay from Article 10.1016/j.str.2004.01.005: \\Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1.\\2004Structure (London, England : 1993), Feb, Volume: 12, Issue:2
Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (304)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (1.64)18.7374
1990's59 (19.41)18.2507
2000's179 (58.88)29.6817
2010's55 (18.09)24.3611
2020's6 (1.97)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.61 (24.57)
Research Supply Index5.84 (2.92)
Research Growth Index5.81 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials20 (6.21%)5.53%
Reviews30 (9.32%)6.00%
Case Studies1 (0.31%)4.05%
Observational0 (0.00%)0.25%
Other271 (84.16%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (22)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase II Study of UCN-01 in Metastatic Melanoma [NCT00072189]Phase 217 participants (Actual)Interventional2003-11-30Terminated(stopped due to Early termination for discouraging results)
Phase I Dose Escalation Study of UCN-01 (NSC 638850) Plus Cisplatin in Advanced Malignant Solid Tumors [NCT00006464]Phase 10 participants Interventional2001-03-31Completed
A Phase I Study of UCN-01 in Combination With Irinotecan in Resistant Solid Tumor Malignancies (Part I) and in Triple Negative (ER-Negative, PgR-Negative, HER-2 Not-Amplified) Recurrent Breast Cancers (Part II) [NCT00031681]Phase 141 participants (Actual)Interventional2001-12-31Completed
A Phase I Study Of UCN-01 In Combination With Gemcitabine In Unresectable Or Metastatic Pancreatic Carcinoma [NCT00039403]Phase 130 participants (Actual)Interventional2002-04-30Completed
A Phase I Study of UCN-01 in Combination With Topotecan in Patients With Solid Tumors [NCT00045175]Phase 133 participants (Actual)Interventional2002-06-30Completed
The Pharmacokinetic and Safety Profile of UCN-01 in Combination With Irinotecan in Solid Tumors (Primarily Lung, Ovarian and GI Cancers) [NCT00047242]Phase 130 participants (Anticipated)Interventional2002-08-31Completed
Phase I Dose Escalation Study of UCN-01 (NSC 638850) Plus Cisplatin in Advanced Malignant Solid Tumors [NCT00012194]Phase 130 participants (Actual)Interventional2001-03-31Terminated
A Phase 2 Study Of UCN-01 In Advanced Renal Cell Carcinoma [NCT00030888]Phase 20 participants Interventional2002-12-31Active, not recruiting
A Phase 1 Study of UCN-01 in Combination With Carboplatin in Advanced Solid Tumors [NCT00036777]Phase 130 participants (Actual)Interventional2002-03-31Completed
Phase I and Pharmacokinetic Study of UCN-01 and Fludarabine in Relapsed or Refractory Low-Grade Lymphoid Malignancies [NCT00019838]Phase 10 participants Interventional1999-07-31Completed
A Phase II Study of UCN-01 in Combination With Topotecan in Patients With Advanced Ovarian Cancer [NCT00072267]Phase 20 participants Interventional2004-01-31Completed
A Phase I Trial Of UCN-01 And Prednisone In Patients With Refractory Solid Tumors And Lymphomas [NCT00045500]Phase 10 participants Interventional2002-06-30Completed
A Phase I Pharmacologic Trial Of Infusional UCN-01 Given With A Weekly Schedule Of 5-Fluorouracil And Leucovorin [NCT00042861]Phase 10 participants Interventional2002-08-31Completed
Phase I/II Study Of UCN-01 In Combination With Fludarabine In Patients With Relapsed Or Refractory Chronic Lymphocytic Leukemia Or Small Lymphocytic Lymphoma [NCT00045513]Phase 1/Phase 20 participants Interventional2002-06-30Completed
Phase II Study of UCN-01 in Combination With Fluorouracil in Advanced Pancreatic Cancer [NCT00045747]Phase 20 participants Interventional2002-07-31Completed
A Phase 1 Study of UCN-01 in Combination With Perifosine in Patients With Relapsed and Refractory Acute Leukemias and High Risk MDS [NCT00301938]Phase 130 participants (Actual)Interventional2005-12-31Completed
A Phase I Trial of Continuous Infusion UCN-01 in Patients With Refractory Neoplasms [NCT00001444]Phase 151 participants Interventional1995-08-31Completed
A Phase I and Pharmacologic Study of UCN-01 (NSC638850) [NCT00003289]Phase 10 participants Interventional1998-06-30Completed
A Phase I Study of the Cyclin-Dependent Kinase (CDK)/Protein Kinase C (PKC) Inhibitor UCN-01 (NSC 638850) in Combination With 5-Fluorouracil in Patients With Advanced Solid Tumors [NCT00004059]Phase 10 participants Interventional1999-07-31Completed
Phase I Study of UCN-01 and Cytarabine (ARA-C) in Patients With Acute Myelogenous Leukemia, and Myelodysplastic Syndromes [NCT00004263]Phase 116 participants (Actual)Interventional1999-12-31Completed
A Phase II Study of UCN-01 in Combination With Topotecan in Patients With SCLC Who Relapsed or Progressed >= 3 Months After Completing First-Line Platinum-Based Chemotherapy [NCT00098956]Phase 219 participants (Actual)Interventional2005-01-31Completed
Phase II Study of UCN-01 in Relapsed or Refractory Systemic Anaplastic Large Cell and Mature T-Cell Lymphomas [NCT00082017]Phase 220 participants (Actual)Interventional2004-04-05Terminated(stopped due to IND was withdrawn by CTEP due to low accrual and cost of maintaining the IND.)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00072189 (3) [back to overview]Overall Survival
NCT00072189 (3) [back to overview]Progression-free Survival
NCT00072189 (3) [back to overview]Response Rate
NCT00082017 (4) [back to overview]Number of Participants With Adverse Events
NCT00082017 (4) [back to overview]Overall Survival (OS)
NCT00082017 (4) [back to overview]Progression Free Survival (PFS)
NCT00082017 (4) [back to overview]Clinical Response Rate
NCT00098956 (3) [back to overview]Adverse Events, Graded Using the CTCAE Version 3.0
NCT00098956 (3) [back to overview]Objective Response Rates (Complete and Partial) Evaluated Using RECIST Criteria
NCT00098956 (3) [back to overview]Stable Disease Rate Evaluated Using RECIST Criteria

Overall Survival

Estimated using the product-limit method of Kaplan and Meier. (NCT00072189)
Timeframe: Up to 7 years

Interventionmonths (Median)
Arm 17.3

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Progression-free Survival

"Estimated using the product-limit method of Kaplan and Meier.~Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions." (NCT00072189)
Timeframe: From the date of study registration to the first documentation of progressive tumor, assessed up to 7 years

Interventionmonths (Median)
Arm 11.3

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Response Rate

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR (NCT00072189)
Timeframe: Up to 7 years

Interventionpercentage of responding participants (Number)
Arm 10

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Number of Participants With Adverse Events

Here is the number of participants with adverse events. For a detailed list of adverse events, see the adverse event module. (NCT00082017)
Timeframe: 76 months

InterventionParticipants (Number)
UCN-01 for T-cell Lymphomas - Cohort 1&219

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Overall Survival (OS)

OS is defined as the date of on-study to the date of death from any cause or last follow up. (NCT00082017)
Timeframe: 55 months

Interventionmonths (Median)
UCN-01 for T-cell Lymphomas - Cohort 1 Every 28 DaysNA
UCN-01 for T-cell Lymphomas - Cohort 2 Every 21 Days5.2

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Progression Free Survival (PFS)

PFS is defined as the time interval from start of treatment to documented evidence of disease progression. Disease progression is assessed by the International Workshop to Standardize Response Criteria for non-Hodgkin's Lymphomas and is defined as a ≥50% increase from nadir in the sum of the products of the greatest diameters of any previously identified abnormal node for partial response's or non-responders or appearance of any new lesion during or at the end of therapy. (NCT00082017)
Timeframe: 3.6 months

Interventionmonths (Median)
UCN-01 for T-cell Lymphomas - Cohort 1 Every 28 Days0.8
UCN-01 for T-cell Lymphomas - Cohort 2 Every 21 Days0.8

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Clinical Response Rate

Clinical Response Rate is the percentage of participants with a response assessed by the International Workshop to Standardize Response Criteria. Complete response (CR) is complete disappearance of all detectable clinical and radiographic evidence of disease. Complete response unconfirmed (CRu) is per CR criteria except that if a residual node is >1.5cm, it must have regressed by >75%. Partial response (PR) is no increase in size of nodes, liver or spleen. Progressive disease (PD) is a greater than or equal to 50% increase from nadir. Details re: response criteria, see the protocol link module (NCT00082017)
Timeframe: 74.5 months

,
InterventionPercentage of participants (Number)
Complete responseComplete response unconfirmedPartial responseProgressive diseaseStable diseaseNot evaluable
UCN-01 for T-cell Lymphomas - Cohort 1 Every 28 Days18095599
UCN-01 for T-cell Lymphomas - Cohort 2 Every 21 Days000453322

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Adverse Events, Graded Using the CTCAE Version 3.0

(NCT00098956)
Timeframe: Up to 5 years

Interventiontypes of grade 3 / 4 toxicities reported (Number)
Treatment (Topotecan Hydrochloride, UCN-01)7

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Objective Response Rates (Complete and Partial) Evaluated Using RECIST Criteria

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Objective Response (OR) = CR + PR. (NCT00098956)
Timeframe: Up to 5 years

Interventionparticipants (Number)
Treatment (Topotecan Hydrochloride, UCN-01)2

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Stable Disease Rate Evaluated Using RECIST Criteria

Per Response Evaluation Criteria In Solid Tumours Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), disappearance of all target lesions; Partial Response (PR), at least 30% decrease in the sum of the longest diameter of target lesions; Objective Response (OR) = CR + PR. (NCT00098956)
Timeframe: Up to 5 years

Interventionparticipants (Number)
Treatment (Topotecan Hydrochloride, UCN-01)9

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