R-268712|R268712|DC Chemicals

Cas No.:	879487-87-3
Chemical Name:	4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
Synonyms:	R 268712,R268712
SMILES:	FC1C=CC(C2C(C3N=C(C)C=CC=3)=NNC=2)=CC=1C1C=NN(CCO)C=1
Formula:	C₂₀H₁₈FN₅O
M.Wt:	363.39
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
In Vivo:	Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]
In Vitro:	R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1]

Cat. No.	Product name	Field of application
DC74372	CDD-1281	CDD-1281 (CDD1281) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.2 nM and Kiapp value of 8 nM.
DC41012	ALK2-IN-4	ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
DC8022	R-268712	Potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). Exhibits ~ 5000-fold selectivity over p38 MAPK. Suppresses development of renal fibrosis in a unilateral ureteral obstruction model. Also reduces proteinuria, glomeruloscler
DC7980	GW-6604	GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity.