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Purity: ≥98%
SB431542 (SB-431542; SB 431542) is a novel and selective inhibitor of ALK5/TGF-β type I Receptor with potential antitumor activity. It inhibits ALK5/TGF-β with an IC50 of 94 nM in a cell-free assay, and exhibits 100-fold selectivity for ALK5 over p38 MAPK and other kinases.
| ln Vitro |
ALK4, ALK5, and ALK7 activities can be inhibited by SB-431542, with IC50 values of 1 μM, 0.75 μM, and 2 μM, respectively [1]. ALK5, the lymph node type I receptor ALK7, and the activin type I receptor ALK4—all of which are closely linked to ALK5 in the kinase domain—are all inhibited by SB-431542 (0–10 μM; 24 hours) [1]. SB-431542 (0.1, 0.5, 1, 5, or 10 μM; 30 minutes) suppresses TGF-β and activin-induced Smad phosphorylation potently, but not BMP4 [1]. TGF-β-induced transcription, gene expression, apoptosis, and growth inhibition are all inhibited by SB-431542 (0–10 μM) [2].
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| ln Vivo |
In New Zealand rabbits, SB-431542 (subconjunctival; 0.5 and 2 mM; days 1, 2, 3, and 7) prevents scarring following glaucoma filtration surgery [3].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: NIH 3T3 cells; HaCaT, NIH 3T3, C2C12 cells and T47D cells Tested Concentrations: 10 μM; 0.1, 0.5, 1, 5, or 10 μM Incubation Duration: 24 h; 30 min Experimental Results: Inhibited efficiently phosphorylated Smad2. Inhibited the TGF-β- and activin-induced phosphorylation of Smad2 but not BMP-induced phosphorylation of Smad1. Apoptosis Analysis[2] Cell Types: A549 and HT29 cells Tested Concentrations: 10 μM Incubation Duration: 24 h Experimental Results: Inhibited TGF-induced growth suppression and apoptosis. Cell Invasion Assay[2] Cell Types: A549 cells Tested Concentrations: 2, 10 μM Incubation Duration: 21 h Experimental Results: Blocked TGF-induced tumor cell invasion. Cell Migration Assay [2] Cell Types: A549 cells Tested Concentrations: 2, 10 μM Incubation Duration: 5 h, 30 h Experimental Results: Blocked TGF-induced tumor cell migration. |
| Animal Protocol |
Animal/Disease Models: Rabbits (3 to 5 months, 1.8 - 2.5 kg)[3]
Doses: 0.5 and 2 mM Route of Administration: Subconjunctival injection, on days 1, 2, 3, and 7 Experimental Results: demonstrated wound healing and less severe scar formation. |
| References |
[1]. Gareth J Inman, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2002 Jul;62(1):65-74.
[2]. Sunil K Halder, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia. 2005 May;7(5):509-21. [3]. Yi-qin Xiao, et al. SB-431542 inhibition of scar formation after filtration surgery and its potential mechanism. Invest Ophthalmol Vis Sci. 2009 Apr;50(4):1698-706. |
| Molecular Formula |
C22H16N4O3
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| Molecular Weight |
384.39
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| CAS # |
301836-41-9
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| Related CAS # |
SB-431542 (GMP);301836-41-9
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| SMILES |
O1C([H])([H])OC2C([H])=C([H])C(=C([H])C1=2)C1=C(C2=C([H])C([H])=C([H])C([H])=N2)N([H])C(C2C([H])=C([H])C(C(N([H])[H])=O)=C([H])C=2[H])=N1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6015 mL | 13.0076 mL | 26.0152 mL | |
| 5 mM | 0.5203 mL | 2.6015 mL | 5.2030 mL | |
| 10 mM | 0.2602 mL | 1.3008 mL | 2.6015 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Cancer Res.2003 Nov 15;63(22):7791-8. |
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Effects of SB-431542 and Gleevec on TGF-β-induced proliferation of NIH3T3 cells.Cancer Res.2003 Nov 15;63(22):7791-8. |
Effect of SB-431542 on TGF-β-stimulated responses in MG63 cells. Cancer Res.2003 Nov 15;63(22 |
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