RepSox

SKU: orb1300856

Description

RepSox is a potent and selective TGFβR-1/ALK5 inhibitor (IC50=23/4 nM) that blocks ATP binding and autophosphorylation. It is widely used in research to study TGF-β signaling, cellular differentiation like adipogenesis in MEFs, and in models of fibrosis and cancer.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 446859-33-2
• MW: 287.32
• Purity: 99.73%
• Formula: C₁₇H₁₃N₅
• SMILES: Cc1cccc(n1)-c1n[nH]cc1-c1ccc2ncccc2n1
• Target: TGF-beta/Smad,ALK
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (17.4 mM);DMSO:51 mg/mL (177.5 mM)

Bioactivity

• Target IC50:
  TGFβRI:4 nM|autophosphorylation of ALK5:4 nM|K562 cells:> 100 μM|the binding of ATP to ALK5:23 nM|MCF-7 cells:> 100 μM|ALK5:4 nM
• In Vivo:
  METHODS: To test the effect on the differentiation of EGCs from intestinal glial cells, RepSox (3-10 mg/kg in 0.5% CMC-Na) was injected intraperitoneally to GFAP-Cre:Rosa26-tdTomato mice once daily for two weeks. RESULTS: RepSox promotes the conversion of EGCs into neurons and improves gastrointestinal motility in vivo. METHODS: To detect anti-tumor activity in vivo, RepSox (5-20 mg/kg) was injected intraperitoneally into a nude mouse model bearing osteosarcoma 143B every two days for three weeks. RESULTS: RepSox effectively inhibited the growth of osteosarcoma and had low toxicity in nude mice.
• In Vitro:
  METHODS: Mouse embryonic fibroblast MEFs were treated with RepSox (10 µM) for 10 days and cellular lipids were detected using oil red O staining. RESULTS: Many adipocyte-like cells appeared in RepSox-treated MEFs, and oil red O staining of lipid droplets confirmed adipocyte differentiation. METHODS: Sheep fibroblasts were treated with RepSox (10-25 nM) for 3 days, and cell morphology was observed using a microscope. RESULTS: After three days of RepSox treatment, sheep fibroblasts acquired a significantly different morphology and changed from a spindle shape to an elongated shape with more clusters.
• Cell Research:
  RepSox is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 1%) before use. To test anti-TGF-β activity of compounds, HepG2 cells are seeded in 96 well microplates at a concentration of 35000 cells per well in 200 μL of serum-containing medium. The microplates are then placed for 24 h in a cell incubator at 37°C, 5% CO2 atm. RepSox dissolved in DMSO are then added at concentrations of 50 nM to 10 μM (final concentration of DMSO 1%) for 30 min prior to the addition of recombinant TGF-β (1 ng/mL). After an overnight incubation, the cells are washed with PBS and lysed by addition of 10 μL of passive lysis buffer. Inhibition of luciferase activity relative to control groups is used as a measure of compound activity. A concentration response curve is constructed from which an IC50 value is determined graphically.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E616452, E-616452, E 616452, ALK5, ALK5 Inhibitor II, Inhibitor, inhibit, SJN 2511, SJN2511, SJN-2511, RepSox, Smad, Transforming growth factor beta receptors, TGFb, TGF-b/Smad, TGFbeta/Smad, TGF-beta, TGFbeta, TGFβ, TGF-β Receptor, TGF-β/Smad, TGFβR1

Compound Identifiers

PubChem CID

449054