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SEL120-34A

Chemical Structure : SEL120-34A

CAS No.: 1609522-33-9

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

Catalog No.: PC-61658Not For Human Use, Lab Use Only.

SEL120-34A is an ATP-competitive, selective, orally active CDK8/19 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) Select Batch:

Biological Activity

SEL120-34A is an ATP-competitive, selective, orally active CDK8/19 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively.
SEL120-34A shows no significant inhibition on other members of the CDK family (200-fold over CDK9).
SEL120-34A inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells, inhibits IFN- responsive genes expression in vitro.
SEL120-34A exhibits complete inhibitions of STAT1 S727 and STAT5 S726 in Colo-205 CRC xenograft tissues in mice (60mg/kg).

Physicochemical Properties

M.Wt 414.145
Formula C15H18Br2N4
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

References

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

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