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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-TG2-179-1
TG2-179-1

Chemical Structure : TG2-179-1

CAS No.: 1135023-19-6

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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.

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5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

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.

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