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Product Infomation
Product NameSEL120-34A
CAS No.1609522-33-9
Molecular Weight

414.14

Formula

C₁₅H₁₈Br₂N₄

SMILES

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

Stock statusGet quote



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Product description

Description

SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.


IC50 & Target

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CDK8/CycC

4.4 nM (IC50)


In Vitro

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SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively. SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). SEL120-34A is active against a panel of AML cell lines (GI50<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726[1].






Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month







Peferences:

 [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.