TG2-179-1 | BAP1 inhibitor | Probechem Biochemicals

Chemical Structure : TG2-179-1

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TG2-179-1 (BAP1 inhibitor)

货号: 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.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	484.95
分子式	C22H14ClFN4O2S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-[[5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]sulfanyl]-N-[3-cyano-4-(4-fluorophenyl)-5-methylthiophen-2-yl]acetamide

参考文献

1. Kang M, et al. Sci Rep. 2023 Feb 8;13(1):2264.