| Name | SB-505124 hydrochloride |
| Description | SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer. |
| In vitro | METHODS: Rabbit subconjunctival fibroblasts were incubated with 10 μM SB-505124 or 0.04% MMC and then incubated with or without TGF-β2 (2 ng/ml) in 12-well plates for 48 h. The effects of ALK-5 inhibitor SB-505124 on TGF-β2-induced downstream effects were analyzed by Western blotting.
RESULTS: The levels of pSmad2, CTGF, and α-SMA in rabbit subconjunctival fibroblasts treated with SB-505124 were decreased in a concentration-dependent manner. [3] |
| In vivo | SB-505124 (5 mg/kg; i.p.) alone does not elicit any response in C57Bl6 mice bearing A549 xenografts. However, when combined with a single dose of Carboplatin (60 mg/kg), SB-505124 induces sustained therapeutic effects in five subjects, eliminating the need for ongoing maintenance therapy. This synergy presents a potent treatment strategy without continuous intervention in the specified animal model, highlighting its potential efficacy. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Methanol : 120 mg/mL (322.7 mM), Sonication is recommended.
DMSO : 40 mg/mL (107.57 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.38 mM), Sonication is recommended.
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| Keywords | SB-505124 Hydrochloride | ALK7 | ALK5 | ALK4 |
| Inhibitors Related | Alectinib | Trimethylamine N-oxide | Melamine | SB-431542 | Hydrochlorothiazide | Crizotinib | Brigatinib | Pirfenidone | A 83-01 | Cetrimonium bromide | Galunisertib | Alantolactone |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
