Molecular structure of SB-505124, CAS Number: 694433-59-5
SB-505124 (CAS 694433-59-5)
See product citations (2)
Application:
SB-505124 is an inhibitor of Activin receptor-like kinase 5
CAS Number:
694433-59-5
Purity:
≥99%
Molecular Weight:
335.4
Molecular Formula:
C20H21N3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
SB-505124 is a potent and selective inhibitor of the TGF-β type I receptor, also known as activin receptor-like kinase 4 (ALK4). It functions by binding to the ATP-binding site of the receptor, preventing its activation and subsequent downstream signaling. This inhibition leads to the suppression of TGF-β signaling pathways, including Smad-dependent and Smad-independent pathways. By blocking the TGF-β type I receptor, SB-505124 effectively hinders cellular responses to TGF-β, such as cell proliferation, differentiation, and migration. Its ability to target the TGF-β type I receptor without affecting other kinases may be a useful compound for elucidating the mechanisms of TGF-β signaling in experimental applications.
SB-505124 (CAS 694433-59-5) References
- When the Smad signaling pathway is impaired, fibroblasts advance open wound contraction. | Au, K. and Ehrlich, HP. 2010. Exp Mol Pathol. 89: 236-40. PMID: 20705067
- Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor. | Sapitro, J., et al. 2010. Mol Vis. 16: 1880-92. PMID: 21031133
- Thermoreversible gel for delivery of activin receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. | Sutariya, V., et al. 2013. Pharm Dev Technol. 18: 957-62. PMID: 22206499
- Cdk4/6 inhibition induces epithelial-mesenchymal transition and enhances invasiveness in pancreatic cancer cells. | Liu, F. and Korc, M. 2012. Mol Cancer Ther. 11: 2138-48. PMID: 22869556
- TGF-ß induces Lysyl hydroxylase 2b in human synovial osteoarthritic fibroblasts through ALK5 signaling. | Remst, DF., et al. 2014. Cell Tissue Res. 355: 163-71. PMID: 24192939
- Development and validation of an LC-MS/MS method for the determination of SB-505124 in rat plasma: Application to pharmacokinetic study. | Jiang, J., et al. 2016. J Pharm Biomed Anal. 117: 205-9. PMID: 26363490
- Ketamine-induced bladder fibrosis involves epithelial-to-mesenchymal transition mediated by transforming growth factor-β1. | Wang, J., et al. 2017. Am J Physiol Renal Physiol. 313: F961-F972. PMID: 28331066
- Combined delivery of a TGF-β inhibitor and an adenoviral vector expressing interleukin-12 potentiates cancer immunotherapy. | Jiang, J., et al. 2017. Acta Biomater. 61: 114-123. PMID: 28483693
- TGFβ1-induced SMAD2/3 and SMAD1/5 phosphorylation are both ALK5-kinase-dependent in primary chondrocytes and mediated by TAK1 kinase activity. | van Caam, A., et al. 2017. Arthritis Res Ther. 19: 112. PMID: 28569204
- TGFβ-mediated expression of TGFβ-activating integrins in SSc monocytes: disturbed activation of latent TGFβ? | van Caam, A., et al. 2020. Arthritis Res Ther. 22: 42. PMID: 32143707
- Integrated pan-cancer of AURKA expression and drug sensitivity analysis reveals increased expression of AURKA is responsible for drug resistance. | Miralaei, N., et al. 2021. Cancer Med. 10: 6428-6441. PMID: 34337875
- Local inhibition of TGF-β1 signaling improves Th17/Treg balance but not joint pathology during experimental arthritis. | Aarts, J., et al. 2022. Sci Rep. 12: 3182. PMID: 35210510
- Identification of Transcription Factors Responsible for a Transforming Growth Factor-β-Driven Hypertrophy-like Phenotype in Human Osteoarthritic Chondrocytes. | Thielen, NGM., et al. 2022. Cells. 11: PMID: 35406794
- Strontium Regulates the Proliferation and Differentiation of Isolated Primary Bovine Chondrocytes via the TGFβ/SMAD Pathway. | Liu, S., et al. 2022. Front Pharmacol. 13: 925302. PMID: 35712700
- Genetically Engineered Hematopoietic Stem Cells Deliver TGF-β Inhibitor to Enhance Bone Metastases Immunotherapy. | Wang, B., et al. 2022. Adv Sci (Weinh). 9: e2201451. PMID: 35948516
Inhibitor of:
ACTR-IIB, ADMP, ALK, ALK-1, BMPR-IB, Cryptic, DCAMKL3, dsg1α, GDF-1, GDF-9B, Inhibin α, LRRC70, MAWDBP1, MIXL1, Myogenin, netrin-1, NOMO, NOMO1, NOMO3, OTTMUSG00000012817, SARA, Smad8, SNIP1, Tβ-b, TBX22, TGF B-1, TGF B3, TGF beta 1, TGFα, and TGFβ RIII.Activator of:
Cytokeratin 12, FGF-BP3, FucU, GDF-1, Inhibin β-B, Lefty, Lefty-1, Lefty-A, Lefty-B, NUDE1, Smad5, Smad6, TGF B-1, and TMEM100.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SB-505124, 10 mg | sc-362794 | 10 mg | $327.00 | |||
| US: Only available in the US | ||||||
SB-505124, 50 mg | sc-362794A | 50 mg | $1377.00 | |||
| US: Only available in the US | ||||||