iCDK9( i-CDK9 )

Catalog No. M11102 CAS No. 1263369-28-3

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

iCDK9
Note

Research use only, not for human use.
Brief Description

iCDK9 (i-CDK9) is a potent, highly selective CDK9 inhibitor (IC50<0.4 nM, CDK9-CycT1 kinase), exhibits >600-fold selectivity toward CDK1-CycB, CDK2-CycA, CDK4-CycD1, CDK7-CycH-MAT1 and CDK8-CycC.
Description

iCDK9 (i-CDK9) is a potent, highly selective CDK9 inhibitor (IC50<0.4 nM, CDK9-CycT1 kinase), exhibits >600-fold selectivity toward CDK1-CycB, CDK2-CycA, CDK4-CycD1, CDK7-CycH-MAT1 and CDK8-CycC; potently suppresses CDK9 phosphorylation of substrates and causes genome-wide Pol II pausing; efficiently suppresses P-TEFb's phosphorylation of the Pol II CTD and the DSIF subunit SPT5 and causes widespread Pol II pausing at gene promoters, enhances the MYC mRNA production but not protein stability.
In Vitro

CDK9-IN-2 (200 nM) reduces the expression of MEPCE indicating that MEPCE is a pharmacodynamic (PD) marker for any CDK9 inhibitor. The expression of MCL1 protein is reduced 2 hours after treatment and is further reduced after 16 hour exposure to CDK9-IN-2 (500 nM).
In Vivo

——
Synonyms

i-CDK9
Pathway

Angiogenesis
Target

CDK
Recptor

CDK
Research Area

Infection
Indication

——

CAS Number

1263369-28-3
Formula Weight

425.936
Molecular Formula

C23H25ClFN5
Purity

>98% (HPLC)
Solubility

DMSO : 50 mg/mL 117.39 mM
SMILES

N[C@@H]1CC[C@H](NC2=NC=C(Cl)C(C3=NC(NCC4=CC(F)=CC=C4)=CC=C3)=C2)CC1
Chemical Name

N2'-((1r,4r)-4-aminocyclohexyl)-5'-chloro-N6-(3-fluorobenzyl)-[2,4'-bipyridine]-2',6-diamine

1. Lu H, et al. Elife. 2015 Jun 17;4:e06535. doi: 10.7554/eLife.06535.

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