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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Glutaminase-TG2 inhibitor 1-155
TG2 inhibitor 1-155

Chemical Structure : TG2 inhibitor 1-155

CAS No.: 1592640-75-9

TG2 inhibitor 1-155

货号: PC-24404Not For Human Use, Lab Use Only.

TG2 inhibitor 1-155 (TG2 inhibitor 3h) is a potent, selective small molecule Transglutaminase 2 (TG2, TGase2, TGM2) inhibitor with IC50 of 6.1 nM, >1000-fold selective over TG1, TG3, TG6, and Factor XIIIa (FXIIIa).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

TG2 inhibitor 1-155 (TG2 inhibitor 3h) is a potent, selective small molecule Transglutaminase 2 (TG2, TGase2, TGM2) inhibitor with IC50 of 6.1 nM, >1000-fold selective over TG1, TG3, TG6, and Factor XIIIa (FXIIIa).
1-155 significantly inhibited collagen deposition in the lungs in the bleomycin-challenged mice. causes a significant reduction in a key myofibroblast marker α smooth muscle actin and TG2.
1-155 treatment (60 mg/kg twice daily via oral delivery) significantly improved several key lung function parameters, such as cord compliance, vital capacity, and dynamic compliance.

物理化学性质&存储条件

分子量 430.52
分子式 C21H26N4O4S
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

N-(2-(4-((5-(dimethylamino)naphthalen-1-yl)sulfonyl)piperazin-1-yl)-2-oxoethyl)acrylamide

参考文献

1. Wang Z, et al. Cells. 2025 Mar 26;14(7):497.

2. Eduard Badarau, et al. Chem Biol. 2015 Oct 22;22(10):1347-61.

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