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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 | Price | Availability | Quantity |
---|---|---|---|
5 mg | $48 | In Stock | |
10 mg | $83 | In Stock | |
25 mg | $173 | In Stock | |
50 mg | $273 | In Stock | |
100 mg | $395 | In Stock | |
1 mL x 10 mM (in DMSO) | $53 | In Stock |
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 |
Smiles | Cc1cccc(n1)-c1nc(Cc2cccc(c2)C(N)=O)[nH]c1-c1ccc2nccnc2c1 |
Relative Density. | 1.315 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90.0 mg/mL (214.0 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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