Chemical Structure : SMTIN-C10
CAS No.:
2771335-63-6
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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842.80
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Formula
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C42H46IN5O2PS+
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(12-(6-amino-8-((6-iodobenzo[d][1,3]dioxol-5-yl)thio)-9H-purin-9-yl)dodecyl)triphenylphosphonium
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References
1. Sung Hu, et al. J Med Chem. 2020 Mar 26;63(6):2930-2940.
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