Chemical Structure : E966-0530-45418
CAS No.:
2906968-72-5
E966-0530-45418
Catalog No.: PC-23770Not For Human Use, Lab Use Only.
E966-0530-45418 is a potent, selective inhibitor of CDK8 with IC50 of 129 nM, shows slightly weaker activity against CDK19 and does not inhibit other CDKs.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
E966-0530-45418 is a potent, selective inhibitor of CDK8 with IC50 of 129 nM, shows slightly weaker activity against CDK19 and does not inhibit other CDKs.
E966-0530-45418 significantly inhibits the phosphorylation of STAT1 at Ser727 in a concentration-dependent manner without affecting CDK8 expression in DU145 and PC-3 cells transfected with pcDNA3 CDK8-HA plasmid.
E966-0530-45418 significantly inhibits cell migration and the expression of EMT proteins in prostate cancer cells.
E966-0530-45418 suppresses TGF-β1/Smad signaling through inhibition of RNA polymerase II and Smad linker phosphorylation, inhibits β-catenin signaling and downstream proteins via CDK8 inhibition.
E966-0530-45418 (50 mg/kg, q.d., oral) exhibits antimetastatic properties in PC-3 SCID mouse model.
Physicochemical Properties
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M.Wt
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496.51
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Formula
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C24H21FN4O5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-(3-fluoro-4-((2-oxo-3-(propan-2-ylidene)indoline)-5-sulfonamido)phenoxy)-N-methylpicolinamide
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References
1. Ho TY, et al. Biomed Pharmacother. 2023 Jun;162:114667.
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