GRL018-21|CAS |DC Chemicals

Cas No.:
Chemical Name:	GRL018-21
Formula:	C₂₉H₂₃FN₄O₅
M.Wt:	526.52

Cat. No.	Product name	Field of application
DC70442	GRK6 inhibitor 18	GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM.GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases.GRK6 inhibitor 18 has potent cellular target engagement and antiproliferative activity against MM cells (IC50=0.4-0.46 uM) and is synergistic with bortezomib.
DC11955	Takeda compound 101	Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.
DC73878	GRL018-21	GRL018-21 is a highly selective, potent, and non-covalent GRK5 inhibitor with IC50 of 10 nM, >100,000-fold selectivity over GRK2.
DC72121	CCG-273220	CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 220 nM. CCG-273220 is highly selective to GRK5 over GRK2 (IC50=350 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle.
DC71959	CCG-273463	CCG-273463 is a potent, selective and covalent GRK5 inhibitor with an IC50 value of 9 nM. CCG-273463 can be used in the research of heart failure, hypertrophic cardiomyopathy, and cancer.
DC71958	CCG-271423	CCG-271423 is a potent and selective GRK5 inhibitor with IC50 values of 0.0021 μM and 44 μM for GRK5 and GRK2, respectively. CCG-271423 inhibits cardiomyocyte contractility and decreases in Ca2+ transience.
DC71670	KR-39038	KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research.