Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90.0 mg/mL (214.0 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
bottom
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.
IN-1130 868612-83-3 Angiogenesis Tyrosine Kinase/Adaptors ALK IN1130 IN 1130 inhibitor inhibit