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882976-95-6 (Cortistatin A)

1

Identification

Cortistatin A Cortistatin A
Name Cortistatin A
Formula C30H36N2O3
MW 472.62
CAS No. 882976-95-6
EINECS
Smiles [[email protected]@]123O[[email protected]@]4(C[[email protected]](N(C)C)[[email protected]@H](O)[[email protected]](O)C4=CC1=CC[[email protected]]1(C)[[email protected]@H](C4=CC5C=NC=CC=5C=C4)CCC21)CC3 |&1:0,2,4,8,10,17,19,r|
Synonyms
InChI InChI=1/C30H36N2O3/c1-28-10-8-21-15-23-26(33)27(34)24(32(2)3)16-29(23)11-12-30(21,35-29)25(28)7-6-22(28)19-5-4-18-9-13-31-17-20(18)14-19/h4-5,8-9,13-15,17,22,24-27,33-34H,6-7,10-12,16H2,1-3H3/t22-,24+,25?,26-,27-,28-,29-,30-/s3
2

Introduction

Cortistatin A is a natural product isolated from the marine sponge Corticium simplex and is found to be a potent and selective CDK8 inhibitor with an IC50 of 15 nM. Inhibition of CDK8 by Cortistatin A may be a promising approach for cancer therapy. Cortistatin A binds CDK8 and CDK19, as well as ROCK1 and ROCK2, as individual proteins in vitro. Cortistatin A potently inhibits the kinase activity of the CDK8 module in vitro (IC50=12 nM). In cells, Cortistatin A dose-dependently inhibits phosphorylation of known CDK8 substrates STAT1 S727 (IC50<10 nM), Smad2 T220 and Smad3 T179 (IC50<100 nM).  Cortistatin A shows antiproliferative activity against human umbilical vein endothelial cells (HUVECs) at a low concentration with an IC50=1.8 nM, while Cortistatin A demonstrates a selectivity index of more than 3000-fold against HUVECs in comparison with NHDF (normal human dermal fibroblast), KB3-1 (KB epidermoid carcinoma cells).

Background Information

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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB100149813

Storage condition

Solubility

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Mechanism and Indication

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
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Safety Data of Cortistatin A

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AMEDCHEM CHINA
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Related Products

Other Forms of 882976-95-6

Name CAS No Formula MW

Recommended Compounds in CDK

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
CDK9-IN-6 1391855-95-0 C27H37ClN6O2 513.07468
ML167 1285702-20-6 C19H17N3O3 335.36
AMG 925 1401033-86-0 C26H29N7O2 471.55
LDC000067 1073485-20-7 C18H18N4O3S 370.43
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 570.64
LEE011 (succinate) 1374639-75-4 C27H36N8O5 552.63
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 471.0
LEE011 1211441-98-3 C23H30N8O 434.54
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
Wogonin 632-85-9 C16H12O5 284.26
1-NM-PP1 221244-14-0 C20H21N5 331.41
WHI-P180 211555-08-7 C16H15N3O3 297.31
THZ1 1604810-83-4 C31H28ClN7O2 566.05
Senexin A 1366002-50-7 C17H14N4 274.32
CDK4-IN-1 1256963-02-6 C22H29ClN8 440.97
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

Cortistatin A

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