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VER-49009

Chemical Structure : VER-49009

CAS No.: 558640-51-0

VER-49009 (CCT0129397)

Catalog No.: PC-49669Not For Human Use, Lab Use Only.

VER-49009 (CCT0129397, VER49009) is a potent, selective small-molecule inhibitor of Hsp90 with IC50 of 25 nM and Kd value of 78 nM, inhibits ATPase activity of full length yeast Hsp90 protein with IC50 of 0.14 uM.

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Biological Activity

VER-49009 (CCT0129397, VER49009) is a potent, selective small-molecule inhibitor of Hsp90 with IC50 of 25 nM and Kd value of 78 nM, inhibits ATPase activity of full length yeast Hsp90 protein with IC50 of 0.14 uM.
VER-49009 caused significant reduction in cellular levels of Raf-1, and the client protein CDK4.
VER-49009 potently inhibits HCT116 cell proliferation with GI50 of 0.26 uM.
VER-49009 caused induction of HSP72 and HSP27 alongside depletion of client proteins, including C-RAF, B-RAF, and survivin, and the protein arginine methyltransferase PRMT5.
VER-49009 exhibited mean cellular antiproliferative GI(50) values of685 nM against a human cancer cell line panel, induced cell cycle arrest and apoptosis.

Physicochemical Properties

M.Wt 387.82
Formula C19H18ClN3O4
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

5-(5-Chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1H-pyrazole-3-carboxamide

References

1. Dymock BW, et al. J Med Chem. 2005 Jun 30;48(13):4212-5.

2. Sharp SY, et al. Mol Cancer Ther. 2007 Apr;6(4):1198-211.

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