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Chemical Structure : SMTIN-C10
Catalog No.: PC-21380Not For Human Use, Lab Use Only.
SMTIN-C10 is a potent, allosteric tumor necrosis factor receptor-associated protein-1 (TRAP1) inhibitor with IC50 of 1.88 uM, by conjugating TPP a C10 linker, and PU-H71.
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SMTIN-C10 is a potent, allosteric tumor necrosis factor receptor-associated protein-1 (TRAP1) inhibitor with IC50 of 1.88 uM, by conjugating TPP a C10 linker, and PU-H71.
SMTIN-C10 interacts with the E115 residue in the N-terminal domain through the TPP moiety and subsequently induces structural transition of TRAP1 to a tightly packed closed form.
SMTIN-C10 reduces chaperone activity of TRAP1 more effectively than PU-H71.
SMTIN-C10 shows inhibition of TRAP1 in cancer cells and enhances production of mitochondrial ROS.
SMTIN-C10 (5 mg/kg, i.p., daily) reduces tumor growth significantly in H460-xenograft mice, exhibits superior TRAP1 inhibition and anticancer activity of SMTIN-C10 in vitro and in vivo as compared with other Hsp90 and TRAP1 inhibitors.
| M.Wt | 842.80 | |
| Formula | C42H46IN5O2PS+ | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sung Hu, et al. J Med Chem. 2020 Mar 26;63(6):2930-2940.
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