INS018_055 (INS018-055, INS018 05)

Chemical Structure : INS018_055

CAS No.: 2828567-39-9

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货号: PC-21563Not For Human Use, Lab Use Only.

INS018_055 (INS018-055) a selective small-molecule TRAF2- and NCK-interacting kinase (TNIK) inhibitor with Kd value of 4.32 nM and IC50 of 31 nM, inhibits TGF-β-induced α-SMA protein expression in MRC-5 cells with IC50 of 27.14 nM.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥3280	In stock
100 mg		Get quote

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生物&药学活性

INS018_055 (INS018-055) a selective small-molecule TRAF2- and NCK-interacting kinase (TNIK) inhibitor with Kd value of 4.32 nM and IC50 of 31 nM, inhibits TGF-β-induced α-SMA protein expression in MRC-5 cells with IC50 of 27.14 nM.

INS018_055 demonstrates a broad affinity toward targeting fibrosis-related kinases.

INS018_055 potently inhibits TGF-β-mediated α-SMA expression in primary lung fibroblasts from patients with IPF, effectively inhibits key fibrotic pathways such as WNT–β-catenin, TGF-β–SMAD2, TNF-α–NF-κB and YAP–TAZ signaling.

INS018_055 (3, 10 or 30 mg per kg, BID) attenuates murine bleomycin-induced lung fibrosis.

INS018_055 reduces murine lipopolysaccharide-induced lung inflammation.

物理化学性质&存储条件

分子量	487.58
分子式	C27H30FN7O
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	4-(4-fluorophenyl)-1-isopropyl-N-(4-(4-methylpiperazin-1-yl)phenyl)-1H,1'H-[2,4'-biimidazole]-5-carboxamide

参考文献

1. Patent WO2022179528A1.
2. Aladinskiy V, et al. J Med Chem. 2024 Oct 18. doi: 10.1021/acs.jmedchem.4c01580.