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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $48 | In Stock | In Stock | |
| 10 mg | $83 | In Stock | In Stock | |
| 25 mg | $173 | In Stock | In Stock | |
| 50 mg | $273 | In Stock | In Stock | |
| 100 mg | $395 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $53 | In Stock | 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/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 90 mg/mL (214.05 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: 1 mg/mL (2.38 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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