Compounds > apcin
Page last updated: 2024-12-10

apcin

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

Description

apcin: inhibits the anaphase-promoting complex; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2830389
CHEMBL ID4455572
SCHEMBL ID17264260
MeSH IDM000600098

Synonyms (26)

Synonym
CBDIVE_011610
CBDIVE_010656 ,
PROBES1_000324
PROBES2_000474
2-(2-methyl-5-nitroimidazol-1-yl)ethyl n-[2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl]carbamate
AKOS001019259
S9605
300815-04-7
apcin
SCHEMBL17264260
3-(2-methyl-5-nitroimidazol-1-yl)-n-(2,2,2-trichloro-1-phenylaminoethyl)propionamide
CS-0033155
HY-110287
CHEMBL4455572 ,
apcin, >=98% (hplc)
2-(2-methyl-5-nitro-1h-imidazol-1-yl)ethyl 2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethylcarbamate
E73483
EX-A4033
2-(2-methyl-5-nitro-1h-imidazol-1-yl)ethyl n-{2,2,2-trichloro-1-[(pyrimidin-2-yl)amino]ethyl}carbamate
BCP33506
2-(2-methyl-5-nitro-1h-imidazol-1-yl)ethyl (2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl)carbamate ,
EN300-105883
bdbm50527906
AC-36474
Z56813082
AKOS040759454

Research Excerpts

Overview

Acin is a novel cell‑permeable molecule that blocks the interaction between APC/C and Cdc20.

ExcerptReferenceRelevance
"Apcin is a novel cell‑permeable molecule that blocks the interaction between APC/C and Cdc20."( Cdc20 inhibitor apcin inhibits the growth and invasion of osteosarcoma cells.
Gao, Y; Shang, G; Wang, Y; Zhang, B, 2018)		1.55

Effects

ExcerptReferenceRelevance
"Apcin has the potential to treat GBM and is expected to provide new ideas for individualized treatment."( Apcin inhibits the growth and invasion of glioblastoma cells and improves glioma sensitivity to temozolomide.
Ding, Y; He, L; Pan, Y; Song, X; Yu, S; Zhang, C; Zheng, C, 2021)		2.79

Actions

ExcerptReferenceRelevance
"Apcin can inhibit the adhesion of JAR cells and embryo implantation of mouse."( CDC20 inhibitor Apcin inhibits embryo implantation in vivo and in vitro.
Gao, N; Guo, C; Kong, F; Lv, Y; Sun, X; Xiu, X, 2020)		1.63
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
mitotic sister chromatid cohesionCell division cycle protein 20 homologHomo sapiens (human)
mitotic spindle assembly checkpoint signalingCell division cycle protein 20 homologHomo sapiens (human)
regulation of mitotic cell cycleCell division cycle protein 20 homologHomo sapiens (human)
nervous system developmentCell division cycle protein 20 homologHomo sapiens (human)
protein ubiquitinationCell division cycle protein 20 homologHomo sapiens (human)
cell differentiationCell division cycle protein 20 homologHomo sapiens (human)
anaphase-promoting complex-dependent catabolic processCell division cycle protein 20 homologHomo sapiens (human)
positive regulation of synaptic plasticityCell division cycle protein 20 homologHomo sapiens (human)
regulation of meiotic nuclear divisionCell division cycle protein 20 homologHomo sapiens (human)
metaphase/anaphase transition of cell cycleCell division cycle protein 20 homologHomo sapiens (human)
positive regulation of mitotic metaphase/anaphase transitionCell division cycle protein 20 homologHomo sapiens (human)
cell divisionCell division cycle protein 20 homologHomo sapiens (human)
regulation of meiotic cell cycleCell division cycle protein 20 homologHomo sapiens (human)
positive regulation of synapse maturationCell division cycle protein 20 homologHomo sapiens (human)
mitotic spindle assemblyCell division cycle protein 20 homologHomo sapiens (human)
positive regulation of ubiquitin protein ligase activityCell division cycle protein 20 homologHomo sapiens (human)
metaphase/anaphase transition of meiosis ICell division cycle protein 20 homologHomo sapiens (human)
positive regulation of anaphase-promoting complex-dependent catabolic processCell division cycle protein 20 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
protein bindingCell division cycle protein 20 homologHomo sapiens (human)
anaphase-promoting complex bindingCell division cycle protein 20 homologHomo sapiens (human)
ubiquitin-like ligase-substrate adaptor activityCell division cycle protein 20 homologHomo sapiens (human)
ubiquitin ligase activator activityCell division cycle protein 20 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
anaphase-promoting complexCell division cycle protein 20 homologHomo sapiens (human)
kinetochoreCell division cycle protein 20 homologHomo sapiens (human)
spindle poleCell division cycle protein 20 homologHomo sapiens (human)
nucleoplasmCell division cycle protein 20 homologHomo sapiens (human)
centrosomeCell division cycle protein 20 homologHomo sapiens (human)
spindleCell division cycle protein 20 homologHomo sapiens (human)
cytosolCell division cycle protein 20 homologHomo sapiens (human)
mitotic checkpoint complexCell division cycle protein 20 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID1606959Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP level at 30 to 100 uM incubated for 48 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606960Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-3 level at 30 to 100 uM incubated for 48 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606936Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1819684Cytotoxicity against human TNBC MDA-MB-231 cells assessed as cell viability measured after 72 hrs2022ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2
Design, Synthesis, and Biological Evaluation of Apcin-Based CDC20 Inhibitors.
AID1819696Upregulation of cyclin B1 level in human TNBC MDA-MB-468 cells at 80 uM measured after 24 hrs by western blot analysis relative to control2022ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2
Design, Synthesis, and Biological Evaluation of Apcin-Based CDC20 Inhibitors.
AID1606934Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606974Induction of apoptosis in human HepG2 cells assessed as necrotic cells level at 100 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 1.48%)2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606938Cytotoxicity in human Caov3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606933Cytotoxicity in human A375 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606932Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606969Induction of apoptosis in human HepG2 cells assessed as late apoptotic cells level at 300 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 5.12%)2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606973Induction of apoptosis in human HepG2 cells assessed as late apoptotic cells level at 100 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 5.12%)2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606937Cytotoxicity in human OVCAR3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606941Inhibition of CDC20 in human HepG2 cells assessed as increase in Bim protein levels at 100 uM incubated for 48 hrs by Western blot Analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606968Induction of apoptosis in human HepG2 cells assessed as early apoptotic cells level at 300 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 4.02%)2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606939Binding affinity to CDC20 (unknown origin) by SPR analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606967Induction of apoptosis in human HepG2 cells assessed as viable cells level at 300 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 89.38%)2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606935Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606949Inhibition of mitotic exit in human HepG2 cells assessed as increase in nuclear phosphohistone H3 levels incubated for 48 hrs by immunofluorescence assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606970Induction of apoptosis in human HepG2 cells assessed as necrotic cells level at 300 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 1.48%)2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606971Induction of apoptosis in human HepG2 cells assessed as viable cells level at 100 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 89.38%)2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606952Inhibition of mitotic exit in human HepG2 cells assessed as increase in nuclear phosphohistone H3 levels at 10 to 100 uM incubated for 48 hrs by by Western blot analysis relative to control2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1606972Induction of apoptosis in human HepG2 cells assessed as early apoptotic cells level at 100 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 4.02%)2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
AID1819685Cytotoxicity against human TNBC MDA-MB-468 cells assessed as cell viability measured after 72 hrs2022ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2
Design, Synthesis, and Biological Evaluation of Apcin-Based CDC20 Inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (41.67)24.3611
2020's7 (58.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.65

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index37.65 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index47.16 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (37.65)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
carbamates
[no description available]		5.59110amino-acid anion
nocodazole
[no description available]		2.2510aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes		antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
temozolomide
[no description available]		7.3110imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		2.4110alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
cyclopentane
Cyclopentanes: A group of alicyclic hydrocarbons with the general formula R-C5H9.. cyclopentanes : Cyclopentane and its derivatives formed by substitution.		2.1510cycloalkane;
cyclopentanes;
volatile organic compound		non-polar solvent
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.7220taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		2.1310L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
tosylarginine methyl ester
Tosylarginine Methyl Ester: Arginine derivative which is a substrate for many proteolytic enzymes. As a substrate for the esterase from the first component of complement, it inhibits the action of C(l) on C(4).		2.110guanidines;
L-arginine ester;
methyl ester;
sulfonamide
sch 51344
SCH 51344: inhibits ras transformation; structure given in first source. SCH51344 : A pyrazoloquinoline that is 6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinoline bearing an additional 2-[(2-hydroxyethoxy)ethyl]amino substituent at position 4		3.2110aromatic amine;
aromatic ether;
primary alcohol;
pyrazoloquinoline;
secondary amino compound		antineoplastic agent
adenanthin
adenanthin: inhibits both peroxiredoxin I and II; isolated from Rabdosia adenantha; structure in first source		3.2110
pevonedistat
pevonedistat: a potent and selective inhibitor of NAE (NEDD8-activating enzyme). pevonedistat : A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine which is substituted by a (1S)-2,3-dihydro-1H-inden-1-ylnitrilo group at position 4 and by a (1S,3S,4S)-3-hydroxy-4-[(sulfamoyloxy)methyl]cyclopentyl group at position 7. It is a potent and selective NEDD8-activating enzyme inhibitor with an IC50 of 4.7 nM, and currently under clinical investigation for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndromes.		2.1510cyclopentanols;
indanes;
pyrrolopyrimidine;
secondary amino compound;
sulfamidate		antineoplastic agent;
apoptosis inducer
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		3.2110benzenes;
hydroxycoumarin;
methyl ketone
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms, Brain
[description not available]		02.3110
Astrocytoma, Grade IV
[description not available]		02.3110
Glial Cell Tumors
[description not available]		02.3110
Invasiveness, Neoplasm
[description not available]		02.3110
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		02.3110
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		07.3110
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		07.3110
Acute Kidney Failure
[description not available]		02.610
Ureteral Obstruction
Blockage in any part of the URETER causing obstruction of urine flow from the kidney to the URINARY BLADDER. The obstruction may be congenital, acquired, unilateral, bilateral, complete, partial, acute, or chronic. Depending on the degree and duration of the obstruction, clinical features vary greatly such as HYDRONEPHROSIS and obstructive nephropathy.		02.610
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		02.610
Genome Instability
[description not available]		03.1710
Benign Neoplasms
[description not available]		03.9520
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.9520
Disease Exacerbation
[description not available]		02.1710
Osteogenic Sarcoma
[description not available]		02.1710
Osteosarcoma
A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)		07.1710
Kahler Disease
[description not available]		02.1310
Multiple Myeloma
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.		02.1310
Cancer of Prostate
[description not available]		02.1510
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.1510