Page last updated: 2024-12-08

kt 5720

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

Description

KT 5720: indolocarbazole; synthetic derivative of K 252a [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

KT 5720 : An organic heterooctacyclic compound that is 1H,1'H-2,2'-biindole in which the nitrogens have undergone formal oxidative coupling to positions 2 and 5 of hexyl (3S)-3-hydroxy-2-methyltetrahydrofuran-3-carboxylate (the 2R,3S,5S product), and in which the 3 and 3' positions of the biindole moiety have also undergone formal oxidative coupling to positions 3 and 4 of 1,5-dihydro-2H-pyrrol-2-one. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID454202
CHEBI ID85085
SCHEMBL ID16112156
MeSH IDM0160694

Synonyms (29)

Synonym
9,12-epoxy-1h-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9r,10r,12s)-rel-
hexyl hydroxy-methyl-oxo-[?]carboxylate
108068-98-0
kt5720
kt-5720
kt 5720
9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo (3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9alpha,10beta,12alpha)-
9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9r,10r,12s)-rel-
bdbm14030
hexyl (15r,16s,18s)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaene-16-carboxylate
HMS3229H09
58hv29i28s ,
unii-58hv29i28s
9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9r,10s,12s)-
antibiotic kt-5720
SCHEMBL16112156
(9r,10s,12s)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1h-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, hexyl ester
(9r,10s,12s)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1h-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid hexyl ester
hexyl (5r,6s,8s)-6-hydroxy-5-methyl-13-oxo-5,6,7,8,14,15-hexahydro-13h-5,8-epoxy-4b,8a,14-triazadibenzo[b,h]cycloocta[1,2,3,4-jkl]cyclopenta[e]-as-indacene-6-carboxylate
antibiotic kt 5720
CHEBI:85085
AKOS030213134
DTXSID40910614
kt5720 - cas 108068-98-0
hexyl (15r,16r,18s)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate
hexyl (15r,16s,18s)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate
CS-0002494
HY-N6789
BK162735

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" In the present study, the non-xanthine PDE type IV inhibitor rolipram (4-[3'-cyclopentyloxy-4'-methoxyphenyl]-2-pyrrolidone) alone and in combination with adenosine is examined as a potential modulator of TNF alpha-primed PMN oxidative activity."( The specific type IV phosphodiesterase inhibitor rolipram combined with adenosine reduces tumor necrosis factor-alpha-primed neutrophil oxidative activity.
Carper, HT; Mandell, GL; Sullivan, GW, 1995
)
0.29

Dosage Studied

ExcerptRelevanceReference
" The present investigation determined the effect of human natural cycle periovulatory follicular (hFF) and oviductal fluids (hOF) on the human sperm AR in dose-response fashion using the synchronous AR assay."( The acrosome reaction-inducing effect of human follicular and oviductal fluid.
Barratt, CL; Cooke, ID; De Jonge, CJ; Radwanska, E,
)
0.13
" In addition, the dose-response curve for DA concentration-Vte was biphasic, and the maximum stimulation was obtained with 10 micromol l(-1)."( Modulation of ion uptake across posterior gills of the crab Chasmagnathus granulatus by dopamine and cAMP.
Genovese, G; Halperin, J; Luquet, CM; Tresguerres, M, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
EC 2.7.11.11 (cAMP-dependent protein kinase) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of cAMP-dependent protein kinase (EC 2.7.11.11).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (7)

ClassDescription
organic heterooctacyclic compound
gamma-lactamA lactam in which the amide bond is contained within a five-membered ring, which includes the amide nitrogen and the carbonyl carbon.
tertiary alcoholA tertiary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has three other carbon atoms attached to it.
carboxylic esterAn ester of a carboxylic acid, R(1)C(=O)OR(2), where R(1) = H or organyl and R(2) = organyl.
hemiaminalAny organic amino compound that has an amino group and a hydroxy group attached to the same carbon atom. Hemiaminals are intermediates in the formation of imines by addition of an amine to an aldehyde or ketone; those derived from primary amines are particularly unstable.
semisynthetic derivativeAny organic molecular entity derived from a natural product by partial chemical synthesis.
indolocarbazoleCompounds based upon an indolo[2,3-a]carbazole skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)IC50 (µMol)2.10970.00201.24099.0000AID1797134
Rho-associated protein kinase 2Bos taurus (cattle)IC50 (µMol)2.10970.00121.38849.0000AID1797134
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
mesoderm formationcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein phosphorylationcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
peptidyl-serine phosphorylationcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cellular response to heatcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
negative regulation of TORC1 signalingcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
smooth muscle contractionRho-associated protein kinase 2Bos taurus (cattle)
positive regulation of centrosome duplicationRho-associated protein kinase 2Bos taurus (cattle)
actin cytoskeleton organizationRho-associated protein kinase 2Bos taurus (cattle)
regulation of actin cytoskeleton organizationRho-associated protein kinase 2Bos taurus (cattle)
regulation of circadian rhythmRho-associated protein kinase 2Bos taurus (cattle)
rhythmic processRho-associated protein kinase 2Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein serine/threonine kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
AMP-activated protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cAMP-dependent protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein bindingcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
ATP bindingcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein domain specific bindingcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein serine kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein serine/threonine kinase activityRho-associated protein kinase 2Bos taurus (cattle)
protein kinase activityRho-associated protein kinase 2Bos taurus (cattle)
ATP bindingRho-associated protein kinase 2Bos taurus (cattle)
small GTPase bindingRho-associated protein kinase 2Bos taurus (cattle)
metal ion bindingRho-associated protein kinase 2Bos taurus (cattle)
protein serine kinase activityRho-associated protein kinase 2Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
acrosomal vesiclecAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
nucleuscAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cytoplasmcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
mitochondrioncAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
plasma membranecAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
neuromuscular junctioncAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
sperm flagellumcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
perinuclear region of cytoplasmcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cAMP-dependent protein kinase complexcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cytosolRho-associated protein kinase 2Bos taurus (cattle)
nucleusRho-associated protein kinase 2Bos taurus (cattle)
plasma membraneRho-associated protein kinase 2Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1797134Kinase Activity Assay from Article 10.1074/jbc.M512374200: \\Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.\\2006The Journal of biological chemistry, Aug-25, Volume: 281, Issue:34
Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (376)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.27)18.7374
1990's109 (28.99)18.2507
2000's192 (51.06)29.6817
2010's73 (19.41)24.3611
2020's1 (0.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.81

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 Index27.81 (24.57)
Research Supply Index5.95 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index30.30 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.26%)5.53%
Reviews1 (0.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other380 (99.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]