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R-268712

R-268712

Item no.	HY-12953-10mM
Manufacturer	MedChem Express
CASRN	879487-87-3
Amount	10 mM/1 mL
Quantity options	100 mg 10 mM/1 mL 10 mg 25 mg 2 mg 50 mg 5 mg
Category	Neuroscience Molecular Targets for Neuroscience Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	99.92
Citations	[1]Terashima H, et al. Attenuation of pulmonary fibrosis in type I collagen-targeted reporter mice with ALK-5 inhibitors. Pulm Pharmacol Ther. 2019 Feb;54:31-38.\|[2]Terashima H, et al. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014 Jul 5;734:60-6. \|[3]Wang H, et al. Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage. Eur J Med Chem. 2020 Apr 1;191:112154.
Smiles	FC1=C(C2=CN(CCO)N=C2)C=C(C3=CNN=C3C4=CC=CC(C)=N4)C=C1
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	879487-87-3
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Cancer-Kinase/protease
Manufacturer - Targets	Anaplastic lymphoma kinase (ALK); TGF-beta/Smad; TGF-β Receptor
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	363.39
Product Description	R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer[1][2].
Manufacturer - Research Area	Cancer; Inflammation/Immunology; Cardiovascular Disease
Solubility	DMSO : 125 mg/mL (ultrasonic)
Manufacturer - Pathway	Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; TGF-beta/Smad
Clinical information	No Development Reported
Isoform	ALK5

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