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SM253

Chemical Structure : SM253

CAS No.: 1610546-52-5

SM253 (SM 253;SM-253)

Catalog No.: PC-60497Not For Human Use, Lab Use Only.

SM253 (SM 253, SM-253) is a novel potent Hsp90 inhibitor that does not induce heat shock response.

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Biological Activity

SM253 (SM 253, SM-253) is a novel potent Hsp90 inhibitor that does not induce heat shock response.
SM253 demonstrates cytotoxicity to both HCT-116 and MiaPaCa-2 cells lines with IC50 of 5 and 5.5 uM, respectively.
SM253 also induces apoptosis and significantly increases caspase 3/7 activity compared to 17-AAG (2-fold); binds to the N-middle linker region of Hsp90, resulting in reduced client protein activation and preventing C-terminal co-chaperones and client proteins from binding to Hsp90.
SM253 exhibits antiproliferative and pro-apoptotic activity in multiple prostate cancer cell lines (LNCaP, 22Rv1, and PC-3) at low micromolar concentrations.

Physicochemical Properties

M.Wt 716.942
Formula C39H52N6O5S
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

Soluble in 30%ACN/H2O

Chemical Name/SMILES

(3R,6R,9R,12S,15S)-9-benzhydryl-3,12-diisobutyl-15-isopropyl-1-methyl-6-(thiazol-4-ylmethyl)-1,4,7,10,13-pentaazacyclopentadecane-2,5,8,11,14-pentaone

References

1. Koay YC, et al. ACS Med Chem Lett. 2014 May 13;5(7):771-6.

2. Armstrong HK, et al. Prostate. 2016 Dec;76(16):1546-1559.

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