Bulk Inquiry
SB 431542
- Soluble in DMSO
- MF: C22H16N4O3
- MW: 384.39
Description
SB 431542 is a potent and selective inhibitor of TGF-β superfamily activin receptor-like kinases (ALKs), targeting ALK5 with an IC50 value of 94 nM and ALK4 with an IC50 value of 140 nM. SB 431542 also inhibits ALK7 and effectively blocks endogenous activin and TGF-β signaling while having no effect on BMP signaling.
The TGF-β/Activin pathway regulates cell proliferation, differentiation, epithelial-to-mesenchymal transition (EMT), stem cell fate, and tissue homeostasis. SB 431542 is widely used as a research tool to study TGF-β and activin signaling and is frequently applied in stem cell culture, cellular reprogramming, and differentiation protocols.
Key Features
- Potent and selective ALK5 and ALK4 inhibitor
- IC50: 94 nM (ALK5) and 140 nM (ALK4)
- Also inhibits ALK7
- Blocks endogenous TGF-β and activin signaling
- No effect on BMP signaling (ALK2, ALK3, and ALK6) or on more than 20 other commonly tested protein kinases.
Applications
- TGF-β and activin signaling research
- Stem cell maintenance and differentiation studies
- Cellular reprogramming research
- Epithelial-to-mesenchymal transition (EMT) studies
- Developmental biology and tissue homeostasis research
Promotion: SB 431542 is also part of Inhibitor Set(s):
| Stem Cell LSB inhibitor Set (Axon 5004) |
| Stem Cell LSC inhibitor Set (Axon 5005) |
| Stem Cell 5i inhibitor Set (Axon 5007) |
| Stem Cell 4i inhibitor Set (Axon 5009) |
More Information
| Parent CAS No. | 301836-41-9 |
|---|---|
| Chemical Name | 4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide |
| SMILES | C1=C(C2N=C(C3C=CC(C(=O)N)=CC=3)NC=2C2N=CC=CC=2)C=CC2OCOC1=2 |
| MFCD | MFCD05865244 |
| InChi | InChI=1S/C22H16N4O3/c23-21(27)13-4-6-14(7-5-13)22-25-19(20(26-22)16-3-1-2-10-24-16)15-8-9-17-18(11-15)29-12-28-17/h1-11H,12H2,(H2,23,27)(H,25,26) |
| InChiKey | FHYUGAJXYORMHI-UHFFFAOYSA-N |
| CID | 4521392 |
| Short Description | ALK5 inhibitor |
References
- NJ Laping et al. Inhibition of transforming growth factor (TGF)-b1-induced extracellular matrix with a novel inhibitor of the TGF-b type I receptor kinase activity: SB-431542. Mol. Pharmacol. 2002, 62 58-64.
- GJ Inman et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-b superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol. Pharmacol. 2002, 62 65-74.
- S Matsuyama et al. SB-431542 and Gleevec inhibit transforming growth factor-b-induced proliferation of human osteosarcoma cells. Cancer Res. 2003, 63 7791-7798.
- MD Hjelmeland et al. SB-431542, a small molecule transforming growth factor-β-receptor antagonist, inhibits human glioma cell line proliferation and motility. Mol. Cancer Ther. 2004, 3, 737.
- List of publications using SB 431542 (Axon 1661) purchased from Axon Medchem
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