Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
26 Results for "
GRK5 inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "GRK5 inhibitors" in MCE Product Catalog:
5
5 Cited Publications
Cat. No.: HY-18991
CAS No.: 1813527-81-9
Research Areas:
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.
4
4 Cited Publications
Research Areas:
CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .
4
4 Cited Publications
Research Areas:
GRK6-IN-1 (Compound 18) is the inhibitor for G protein-coupled receptorkinase 6 (GRK6) with an IC50 of 3.8-8 nM. GRK6-IN-1 also inhibits GRK7, GRK5, GRK4 and GRK1 with IC50s of 6.4, 12, 22 and 52 nM, respectively. GRK6-IN-1 has the potential for the research of multiple myeloma .
4
4 Cited Publications
Research Areas:
GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC50 of 49.7 μM. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research .
3
3 Cited Publications
Cat. No.: HY-47573
CAS No.: 2750414-35-6
Research Areas:
CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle .
1
1 Cited Publications
Research Areas:
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 .
1
Research Areas:
CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research .
1
1 Cited Publications
Target:
Opioid Receptor G Protein-coupled Receptor Kinase (GRK) Mas-related G-protein-coupled Receptor (MRGPR)
Research Areas:
CCG258747 is a selective GRK2 inhibitor (IC50 = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance) .
Research Areas:
AM-001 is a selective Epac1 inhibitor with an IC50 value of 47.8-53.7 μM. AM-001 blocks cAMP (Cyclic AMP) (HY-B1511)-induced conformational changes of Epac1, inhibits Epac1-dependent activation of Rap1, and does not compete with cAMP for binding to Epac1. AM-001 disrupts the formation of the Epac1-GRK5 complex, blocks nuclear import of GRK5, and inhibits GRK5-mediated nuclear export of HDAC5 and activation of MEF2. AM-001 can be used in research related to heart disease, myocardial ischemia/reperfusion injury, SARS-CoV-2 infection, influenza A virus infection, atrial fibrillation and idiopathic pulmonary fibrosis .
Research Areas:
GRL018-21 is a potent and highly selective G protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC50 value of 10 nM .
Cat. No.: HY-109562
CAS No.: 2055990-90-2
Synonyms: GRKs-IN-1
Research Areas:
CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research .
Cat. No.: HY-150021
CAS No.: 2410793-22-3
Research Areas:
GRK5-IN-3 is a covalent inhibitor of GRK5 (G Protein-Coupled Receptor Kinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively .
Cat. No.: HY-108601A
CAS No.: 1781828-85-0
Target:
Research Areas:
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
Cat. No.: HY-179226
CAS No.: 2816062-15-2
Target:
Research Areas:
AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). AP-7-168 can promote β2AR homodimerization and inhibit GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma .
Cat. No.: HY-174256
Research Areas:
GRL-098-22 (Compound 6t) is a potent inhibitor targeting G protein-coupled receptor kinase 5 (GRK5) and GRK6 with IC50 values of 0.6 μM and 0.19 μM, respectively. GRL-098-22 is promising for research of diseases such as heart failure and multiple myeloma .
Cat. No.: HY-118046
CAS No.: 1123163-20-1
Research Areas:
GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that can be used as a probe for studying heart failure and Parkinson's disease. GSK2163632A potently inhibits GRK1 and GRK5, and also inhibits Rho-associated coiled-coil kinase (ROCK) and insulin-like growth factor receptor IGF-1R. GSK2163632A binds to GRK2 in a manner similar to Paroxetine (HY-122272).
Cat. No.: HY-150022
CAS No.: 2410794-89-5
Synonyms: CCG-265328
Research Areas:
GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research . GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-150039
CAS No.: 2750413-88-6
Research Areas:
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 Ca 2+ transience . CCG-271423 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-150040
CAS No.: 2750413-99-9
Research Areas:
CCG-273463 is a potent, selective and covalent GRK5 inhibitor with an IC50 value of 8.6 nM. CCG-273463 can be used in the research of heart failure, hypertrophic cardiomyopathy, and cancer .
Cat. No.: HY-119232
CAS No.: 864082-48-4
Research Areas:
GSK466317A is a PKA inhibitor, with an IC50 of 12.59 μM. GSK466317A also inhibits GRK1, GRK2, and GRK5, with IC50s of 1000, 31.62, and 39.81 μM, respectively .
- 1
- 2
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
