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Chemical Structure : TG2-179-1
Catalog No.: PC-20004Not For Human Use, Lab Use Only.
TG2-179-1 is a potent, selective and covalently inhibitor of deubiquitinase (DUB) BRCA1-associated protein-1 (BAP1), covalently binds to the active site of BAP1 (Cys91), exhibits potent cytotoxic activity against colon cancer cells.
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TG2-179-1 is a potent, selective and covalently inhibitor of deubiquitinase (DUB) BRCA1-associated protein-1 (BAP1), covalently binds to the active site of BAP1 (Cys91), exhibits potent cytotoxic activity against colon cancer cells.
TG2-179-1 has potent cytotoxic activity against colon cancer cells with IC50 of <10 uM against HCT116, HT29 and SW48 cells, and BAP1-proficient cells are more sensitive to TG2-179-1 than BAP1-deficient cells.
TG2-179-1 exerts its cytotoxic activity against colon cancer cells as well as other types of cancer cells, such as mesothelioma and ccRCC, by targeting BAP1.
TG2-179-1 induces replication defects in colon cancer cells and increases the level of γ-H2AX in a dose-dependent manner in HCT116 cells, which is similar to BAP1 depletion.
TG2-179-1 inhibits the growth of colon tumors in mice.
| M.Wt | 484.95 | |
| Formula | C22H14ClFN4O2S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kang M, et al. Sci Rep. 2023 Feb 8;13(1):2264.
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