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Submit ReviewSB 505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). Selectively inhibits signaling from TGF-β and activin; does not inhibit other ALK family members. Promotes adenine base editor activity in vivo and in vitro at 10 μM.
SB 505124 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
M. Wt | 335.4 |
Formula | C20H21N3O2 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 694433-59-5 |
PubChem ID | 9858940 |
InChI Key | WGZOTBUYUFBEPZ-UHFFFAOYSA-N |
Smiles | CC(C)(C)C1=NC(C2=CC(OCO4)=C4C=C2)=C(C3=NC(C)=CC=C3)N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 33.54 | 100 | |
2eq. HCl | 33.54 | 100 |
The following data is based on the product molecular weight 335.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.98 mL | 14.91 mL | 29.82 mL |
5 mM | 0.6 mL | 2.98 mL | 5.96 mL |
10 mM | 0.3 mL | 1.49 mL | 2.98 mL |
50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
References are publications that support the biological activity of the product.
Byfield et al (2004) SB-505124 is a selective inhibitor of transforming growth factor-β type I receptors ALK4, ALK5, and ALK7. Mol.Pharmacol. 65 744 PMID: 14978253
Hu et al (2005) Reactive oxygen species production via NADPH oxidase mediates TGF-β-induced cytoskeletal alterations in endothelial cells. Am.J.Physiol.Renal Physiol. 289 F816 PMID: 16159901
Noma et al (2008) The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis. Gastroenterology 134 1981 PMID: 18439605
Yang et al (2022) Small-molecule activators specific to adenine base editors through blocking the canonical TGF-β pathway. Nucleic Acids Res. 50 9632 PMID: 36043443
If you know of a relevant reference for SB 505124, please let us know.
Keywords: SB 505124, SB 505124 supplier, SB505124, tgfβ, tgfbeta, tgfb, tgfbrI, tgfbetarI, tgfβrI, receptors, transforming, growth, factors, alk5, alk4, alk7, inhibitors, inhibits, ABE, adenine, base, editing, editor, TGF-beta, Receptors, BMP, and, Other, Activin, ALK, 3263, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for SB 505124 include:
Yang et al (2017) Establishment of mouse expanded potential stem cells. Nature 550 393 PMID: 29019987
Asghar et al (2017) Potential role of indoleamine 2,3-dioxygenase in primary biliary cirrhosis. Oncol Lett 14 5497 PMID: 29113177
Boxtel et al (2015) A Temporal Window for Signal Activation Dictates the Dimensions of a Nodal Signaling Domain. Dev Cell 35 175 PMID: 26506307
Ramel and Hill (2013) The ventral to dorsal BMP activity gradient in the early zebrafish embryo is determined by graded expression of BMP ligands. Dev Biol 378 170 PMID: 23499658
Zhu et al (2016) Crosstalk between bone marrow-derived myofibroblasts and gastric cancer cells regulates cancer stemness and promotes tumorigenesis. Oncogene 35 5388 PMID: 27109105
Do you know of a great paper that uses SB 505124 from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.