1. TGF-beta/Smad
  2. TGF-β Receptor
  3. IN-1130

IN-1130 

Cat. No.: HY-18758
Handling Instructions

IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.

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IN-1130 Chemical Structure

IN-1130 Chemical Structure

CAS No. : 868612-83-3

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Description

IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis[1][2].

IC50 & Target[1]

ALK5

 

In Vitro

IN-1130 (0.5, 1 μM; for 2 hours) inhibits TGF-β-stimulated Smad2 phosphorylation and subsequent nuclear translocation in HepG2 and 4T1 cells[2].
IN-1130 (1 μM; for 72 hours) restores the TGF-β-mediated decrease in E-cadherin protein expression. IN-1130 (1 μM; for 72 hours) inhibits TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs in MCF10A cells[2].
IN-1130 (1 μM; pretreated for 30 min) inhibits TGF-β-induced MDA-MB-231 cells, NMuMG, and MCF10A cells mobility and invasion[2].

Western Blot Analysis[2]

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[2]

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.
In Vivo

IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) reduces the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats[1].
IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys[1].
IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c mice)[2].

Animal Model: Six-week-old male Sprague–Dawley rats weighing 180-200 g[1]
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.
Molecular Weight

420.47

Formula

C₂₅H₂₀N₆O

CAS No.

868612-83-3

SMILES

O=C(N)C1=CC=CC(CC2=NC(C3=NC(C)=CC=C3)=C(C4=CC=C5N=CC=NC5=C4)N2)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

IN-1130IN1130IN 1130TGF-β ReceptorTransforming growth factor beta receptorsSmad3phosphorylationcaseinp38αmitogen-activatedproteinrenalfibrosisobstructivenephropathybreastcancerlungmetastasiInhibitorinhibitorinhibit

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