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INS018_055

Chemical Structure : INS018_055

CAS No.: 2828567-39-9

INS018_055 (INS018-055)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

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.

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