1695550-43-6
Chemical Structure
SMTIN-P01
- CAS No.: 1695550-43-6
- Formula:C36H34BrIN5O2PS
- Molecular Weight:838.53
InChIKey: IGLVCZKBEMGZFY-UHFFFAOYSA-M
SMILES: IC1=C(SC2=NC3=C(N2CCCCCC[P+](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)N=CN=C3N)C=C7OCOC7=C1.[Br-]
Biological Activity: SMTIN-P01 is a TRAP1 inhibitor that is selective for cytosolic Hsp90 and accumulates in mitochondria. SMTIN-P01 binds to the ATP-binding site of TRAP1 as an ATP mimic, thereby inhibiting ATPase and foldase activities. SMTIN-P01 induces mitochondrial membrane depolarization and proteolytic degradation in cancer cells. SMTIN-P01 exhibits significant cytotoxicity, but shows extremely low toxicity to primary mouse hepatocytes, and does not interfere with SIRT3-related functions or the levels of cytosolic Hsp90 substrates. SMTIN-P01 has important application value in cancer-related research[1][2][3][4].
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SMTIN-P01 | SMTIN-P01 is a TRAP1 inhibitor that is selective for cytosolic Hsp90 and accumulates in mitochondria. SMTIN-P01 binds to the ATP-binding site of TRAP1 as an ATP mimic, thereby inhibiting ATPase and foldase activities. SMTIN-P01 induces mitochondrial membrane depolarization and proteolytic degradation in cancer cells. SMTIN-P01 exhibits significant cytotoxicity, but shows extremely low toxicity to primary mouse hepatocytes, and does not interfere with SIRT3-related functions or the levels of cytosolic Hsp90 substrates. SMTIN-P01 has important application value in cancer-related research. | |||||||||||||||||||||
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References
- [1]. Lee C, et al. Development of a mitochondria-targeted Hsp90 inhibitor based on the crystal structures of human TRAP1. J Am Chem Soc. 2015;137(13):4358-4367. [Content Brief]
- [2]. Serapian SA, et al. Targeting the mitochondrial chaperone TRAP1: strategies and therapeutic perspectives. Trends Pharmacol Sci. 2021;42(7):566-576. [Content Brief]
- [3]. Kang S, et al. Structure, Function, and Inhibitors of the Mitochondrial Chaperone TRAP1. J Med Chem. 2022;65(24):16155-16172. [Content Brief]
- [4]. Hu S, et al. Chemical approaches to development of mitochondrial-targeted Hsp90 inhibitor in anti-cancer therapeutics: Mechanism and structure change of mitochondrial Hsp90[J]. Cancer Research, 2017, 77(13_Supplement): 1492-1492.
