Romaciclib (monohydrochloride)

SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726[1]. Has anti-tumor activity[1].

Product Specifications

CAS Number

[2443816-41-7]

Product Name Alternative

SEL120-34A (monohydrochloride)

UNSPSC

12352005

Target

CDK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/SEL120-34A_monohydrochloride.html

Purity

99.29

Solubility

DMSO : 16.67 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 50 mg/mL (ultrasonic)

Smiles

CC1=C2C3=C(C(Br)=C1Br)CCCN3C(N4CCNCC4)=N2.Cl

Molecular Formula

C15H19Br2ClN4

Molecular Weight

450.60

References & Citations

[1]Rzymski T, et al. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8 (20) :33779-33795.