| DC11765 |
GRK2-IN-115h hydrochloride |
A highly potent and selective GRK2 inhibitor with IC50 of 18 nM. |
|
| DC11958 |
CCG 258001 |
A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 280 nM. |
|
| DC11957 |
CCG 224061 |
A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 66 nM. |
|
| DC11956 |
CCG 258748 |
A potent, selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 8 nM. |
|
| DC11302 |
CCG215022
Featured
|
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively. |
|
| DC11955 |
Takeda compound 101
Featured
|
Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3. |
|
| DC10124 |
GSK180736A
Featured
|
GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM. |
|
| DC70442 |
GRK6 inhibitor 18
Featured
|
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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
