INS018_055 (INS018-055)

Chemical Structure : INS018_055

CAS No.: 2828567-39-9

Catalog No.: 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.

Packing	Price	Stock
5 mg	$248	In stock
10 mg	$398	In stock
25 mg	$598	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	489.60
Formula	C27H32FN7O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(4-fluorophenyl)-3-isopropyl-N-(4-(4-methylpiperazin-1-yl)phenyl)-2,3-dihydro-1H,1'H-[2,4'-biimidazole]-4-carboxamide

References

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