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IN-1130

Catalog No. T15572 CAS 868612-83-3

IN-1130 is a selective inhibitor of ALK5 with IC50 values of 5.3 nM, 36 nM, and 4.3 μM for phosphorylation of ALK5-mediated Smad3, ALK5 phosphorylation of casein and p38α mitogen-activated protein kinase.

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IN-1130, CAS 868612-83-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 139.00
25 mg	In stock	$ 289.00
50 mg	In stock	$ 455.00
100 mg	In stock	$ 672.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 98.08%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	IN-1130 is a selective inhibitor of ALK5 with IC50 values of 5.3 nM, 36 nM, and 4.3 μM for phosphorylation of ALK5-mediated Smad3, ALK5 phosphorylation of casein and p38α mitogen-activated protein kinase.
In vitro	IN-1130 (0.5 -1 μM) inhibits the phosphorylation and nuclear translocation of TGF-β-stimulated Smad2 in HepG2 and 4T1 cells. In MCF10A cells, IN-1130 (1 μM) restores the TGF-β-mediated decrease in E-cadherin protein expression, inhibits TGF-β-induced MMPs mRNA expression, and reduces the gelatinolytic activity of secreted MMPs[2].
In vivo	In unilateral ureteral obstruction rats, intraperitoneal administration of IN-1130 (10-20 mg/kg) decreases the extent of interstitial nephritis and fibrosis. dose-dependently reduces the levels of TGF-β1 mRNA and suppresses Smad2, α-SMA, myofibroblasts phosphorylation[1]. In MMTV/c-Neu mice intraperitoneal administration of IN-1130 (40 mg/kg) blocks breast cancer lung metastasis[2].

Molecular Weight	420.47
Formula	C25H20N6O
CAS No.	868612-83-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (214.0 mM), Sonication is recommended.

References and Literature

1. Moon JA, et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 2006 Oct;70(7):1234-43. 2. Park CY, et al. An novel inhibitor of TGF-β type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 2014 Aug 28;351(1):72-80.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

IN-1130 868612-83-3 Angiogenesis Tyrosine Kinase/Adaptors ALK IN1130 IN 1130 inhibitor inhibit

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