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A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $52 | In Stock | |
10 mg | $88 | In Stock | |
25 mg | $165 | In Stock | |
50 mg | $269 | In Stock | |
100 mg | $398 | In Stock | |
500 mg | $939 | In Stock |
Description | A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures. |
Targets&IC50 | ALK4:45 nM, ALK7:7.5 nM, ALK5:12 nM |
In vitro | METHODS: Wild-type mink lung epithelial cells, Mv1Lu, were treated with A 83-01 (0.03-10 μM) and TGF-β (1 ng/mL) for 48 h, and cell proliferation was detected using a Coulter counter. RESULTS: A 83-01 prevented the inhibition of Mv1Lu cell growth by TGF-β in a dose-dependent manner. [1] METHODS: Mouse ovarian cancer cells HM-1 were treated with A 83-01 (1-10 μM) for 30 min, followed by treatment with TGF-β (1-10 ng/mL) for 60 min, and the expression levels of target proteins were detected using Western Blot. RESULTS: The addition of TGF-β1 increased the expression of pSmad3, and A 83-01 inhibited the up-regulation of TGF-β. [2] |
In vivo | METHODS: To detect anti-tumor activity in vivo, A 83-01 (150 μg/each) was administered intraperitoneally three times a week for four weeks to a B6C3F1 mouse model of peritoneal spread of HM-1 cancer. RESULTS: Ascites formation tended to be slower in the A 83-01-treated group, and A 83-01 significantly improved the survival rate of the mice. [2] METHODS: To investigate the role in myocardial injury, A 83-01 (10 mg/kg) was administered intraperitoneally to Nkx2.5 enh-Cre/mTmG mice once daily for seven days. RESULTS: A 83-01 treatment significantly increased the number of Nkx2.5+ myocardial myofibroblasts at baseline and after myocardial injury, leading to an increase in the number of newly formed myocardial cells. A 83-01 treatment significantly improved ventricular elasticity and stroke work, which led to an improvement of contractility after injury. [3] |
Cell Research | HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A-83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay following the manufacturer's instructions. |
Alias | ALK5 Inhibitor IV, A8301 |
Molecular Weight | 421.52 |
Formula | C25H19N5S |
Cas No. | 909910-43-6 |
Smiles | Cc1cccc(n1)-c1nn(cc1-c1ccnc2ccccc12)C(=S)Nc1ccccc1 |
Relative Density. | 1.27g/cm3 |
Storage | store at low temperature | Powder: -20°C for 3 years | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 10 mg/mL (23.72 mM), The compound is unstable in solution. Please use soon. ![]() | |||||||||||||||||||||||||
In Vivo Formulation | 10% DMSO+90% Saline: 1 mg/mL (2.37 mM), In vivo: 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. 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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