1610546-52-5
Chemical Structure
SM253
- CAS No.: 1610546-52-5
- Formula:C39H52N6O5S
- Molecular Weight:716.94
IUPAC Name: (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
InChIKey: PXIJKHQDVFNMQY-LGALFMESSA-N
SMILES: C([C@@H]1C(=O)N[C@H](CC2=CSC=N2)C(=O)N[C@H](CC(C)C)C(=O)N(C)[C@@H]([C@H](C)C)C(=O)N[C@@H](CC(C)C)C(=O)N1)(C3=CC=CC=C3)C4=CC=CC=C4
Biological Activity: SM253 is an Hsp90 inhibitor that inhibits Hsp90-dependent protein folding. SM253 blocks chaperone function by binding to the N-middle linker region and the C-terminal M domain, reducing co-chaperone and client protein binding and activation. SM253 induces cancer cell apoptosis, activates caspase 3/7, causes cell cycle arrest and reduces cell proliferation, while decreasing Hsp90 client proteins such as AR, FKBP51, PSA, Cdk4, AKT, ERK, and p23, and reducing Hsp27/Hsp70 expression without inducing heat shock proteins. SM253 causes dose-dependent fibronectin loss in cells expressing LRP1. SM253 can be used for research on colon cancer, pancreatic cancer, and prostate cancer[1][2][3].
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SM253 | SM253 is an Hsp90 inhibitor that inhibits Hsp90-dependent protein folding. SM253 blocks chaperone function by binding to the N-middle linker region and the C-terminal M domain, reducing co-chaperone and client protein binding and activation. SM253 induces cancer cell apoptosis, activates caspase 3/7, causes cell cycle arrest and reduces cell proliferation, while decreasing Hsp90 client proteins such as AR, FKBP51, PSA, Cdk4, AKT, ERK, and p23, and reducing Hsp27/Hsp70 expression without inducing heat shock proteins. SM253 causes dose-dependent fibronectin loss in cells expressing LRP1. SM253 can be used for research on colon cancer, pancreatic cancer, and prostate cancer. | |||||||||||||||||||||
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References
- [1]. Koay YC, et al. Chemically accessible hsp90 inhibitor that does not induce a heat shock response. ACS medicinal chemistry letters. 2014 Jul 10;5(7):771-6.
- [2]. Armstrong HK, et al. A Novel Class of Hsp90 C-Terminal Modulators Have Pre-Clinical Efficacy in Prostate Tumor Cells Without Induction of a Heat Shock Response. The Prostate. 2016 Dec;76(16):1546-1559.
- [3]. Boel NM, et al. LRP1 is required for novobiocin-mediated fibronectin turnover. Scientific reports. 2018 Jul 30;8(1):11438.
