SB-505124 (hydrochloride)

SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

Product Specifications

CAS Number

[356559-13-2]

UNSPSC

12352005

Target

TGF-β Receptor

Type

Reference compound

Related Pathways

TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/sb-505124-hydrochloride.html

Purity

98.52

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C) |Methanol : 125 mg/mL (ultrasonic)

Smiles

CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1.[H]Cl

Molecular Formula

C20H22ClN3O2

Molecular Weight

371.86

References & Citations

[1]DaCosta Byfield S, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65 (3) :744-52.|[2]Sutariya V, et al. Thermoreversible gel for delivery of receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol. 2013 Jul-Aug;18 (4) :957-62.|[3]Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by receptor-like kinase 5 inhibitor. Mol Vis. 2010 Sep 16;16:1880-92.|[4]Marini KD, et al. Inhibition of activin signaling in lung adenocarcinoma increases the therapeutic index of platinum chemotherapy. Sci Transl Med. 2018 Jul 25;10 (451) . pii: eaat3504.