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SEL120-34A hydrochloride

Chemical Structure : SEL120-34A hydrochloride

CAS No.: 1609452-30-3

SEL120-34A hydrochloride (SEL 120-34A)

Catalog No.: PC-61659Not For Human Use, Lab Use Only.

SEL120-34A is an ATP-competitive, selective, orally active CDK8 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SEL120-34A is an ATP-competitive, selective, orally active CDK8 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively; shows no significant inhibition on other members of the CDK family (200-fold over CDK9); inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells, inhibits IFN- responsive genes expression in vitro; exhibits complete inhibitions of STAT1 S727 and STAT5 S726 in Colo-205 CRC xenograft tissues in mice (60mg/kg).

Physicochemical Properties

M.Wt 450.6
Formula C15H19Br2ClN4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7,8-Dibromo-9-methyl-2-piperazin-1-yl-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline hydrochloride

References

1. Rzymski T, et al. Oncotarget. 2017 May 16;8(20):33779-33795.

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