A83-01

SKU: orb1304606

Description

A 83-01 is a potent inhibitor of TGF-β type I receptors ALK5, ALK4, and ALK7. It facilitates the generation of induced pluripotent stem cells (iPSCs) from somatic cells and is widely used to support the growth and maintenance of various organoid cultures in vitro.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 909910-43-6
• MW: 421.5
• Purity: >98%
• Formula: C₂₅H₁₉N₅S
• SMILES: Cc1cccc(n1)-c1nn(cc1-c1ccnc2ccccc12)C(=S)Nc1ccccc1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 20 mg/ml).

Bioactivity

• Target IC50:
  ALK5:12 nM|ALK4:45 nM|ALK7:7.5 nM
• 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. 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.
• 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. 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.
• 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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

A8301, A83-01, A 83 01, A 8301, A 83-01, ALK4, ALK5, ALK5 Inhibitor IV, ALK, ALK7, inhibit, Inhibitor, TGF-β/Smad, TGFβ, TGF-β Receptor, Transforming growth factor beta receptors, TGFbeta, TGF-b/Smad, TGFb, TGF-beta, TGFbeta/Smad, Smad

Compound Identifiers

PubChem CID

16218924