IN-1130

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 ALK5 抑制剂；抑制 ALK5 介导的 Smad3 磷酸化的纯化激酶结构域，IC50 为 5.3 nM。

A potent ALK5 inhibitor; inhibits the purified kinase domain of ALK5-mediated Smad3 phosphorylation with an IC50 of 5.3 nM; highly selective in a panel of 27 serine/threonine and tyrosine kinases including p38α; decreases levels of TGF-beta1 mRNA, type I collagen mRNA, and pSmad2, compared to UUO control rats; inhibits renal fibrosis in obstructive nephropathy in vivo models.

Western Blot Analysis Cell Line:HepG2 and 4T1 cells Concentration:0.5, 1 μM Incubation Time:For 2 hours Result:Inhibited TGF-β-stimulated Smad2 phosphorylation.RT-PCR Cell Line:MCF10A cells Concentration:1 μM Incubation Time:For 72 hours Result:Inhibited TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs.

Animal Model:Six-week-old male Sprague–Dawley rats weighing 180-200 g Dosage:10 and 20 mg/kg Administration:IP; daily; for 7 and 14 days Result:Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.

IN1130 | IN 1130

TGF-beta/Smad

TGFBR

TGFBR

——

——

868612-83-3

420.47

C25H20N6O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (237.83 mM)

O=C(N)C1=CC=CC(CC2=NC(C3=CC=C4N=CC=NC4=C3)=C(C5=NC(C)=CC=C5)N2)=C1

Benzamide, 3-[[4-(6-methyl-2-pyridinyl)-5-(6-quinoxalinyl)-1H-imidazol-2-yl]methyl]- (9CI)

(-20℃)

With Ice Pack

≥ 2 years