Chemical Structure : TH-407a
CAS No.:
1903103-73-0
TH-407a
(TH407a)
Catalog No.: PC-26913Not For Human Use, Lab Use Only.
TH-407a is a potent and selective, reversible, non-competitive inhibitor of ubiquitin-specific peptidase 15 (USP15) with IC50 of 0.76 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TH-407a is a potent and selective, reversible, non-competitive inhibitor of ubiquitin-specific peptidase 15 (USP15) with IC50 of 0.76 uM.
TH-407a inhibits the hydrolysis of Ub-AMC by USP15 in vitro, also inhibits the binding of USP15 to Ub-PA.
TH-407a exhibits negligible inhibition of USP1, USP2, and USP7 at 10 uM.
TH-407a inhibits USP15 via an allosteric regulatory mechanism rather than direct competition with the catalytic site.
TH-407a inhibits breast cancer cell proliferation with IC50 of 19.57 uM and 38.66 uM for MCF-7 and MDA-MB-436 cells, inhibits colony formation, and cancer cell migration.
TH-407a activates the p53 signaling pathway and inhibits the expression of PARP1.
TH-407a (100 mg/kg, oral gavage daily) significantly reduces tumor growth in mice xenografts with MCF-7 and MDA-MB-436 cells.
Physicochemical Properties
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M.Wt
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354.41
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Formula
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C22H18N4O
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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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naphthalen-2-yl(3-(4-phenyl-1H-1,2,3-triazol-1-yl)azetidin-1-yl)methanone
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References
1. Zhang T, et al. Discovery of a potent and selective small-molecule inhibitor of ubiquitin-specific peptidase 15 (USP15) for the treatment of breast cancer. Eur J Med Chem. 2026 May 25;316:119005.
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