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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
52 Results for "
G protein-coupled receptor kinase
" in MedChemExpress (MCE) Product Catalog:
Products (52)
52 Results for "G protein-coupled receptor kinase" in MCE Product Catalog:
9
9 Publications Verification
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
6
6 Cited Publications
Cat. No.: HY-18990
CAS No.: 817194-38-0
Research Areas:
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
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:
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
Research Areas:
GRK6/Aurora A-IN-1 is a dual inhibitor of G protein-coupled receptor kinase 6 (GRK6)/Aurora A, with IC50 values of 120 nM and 11 nM, respectively. GRK6 is a key kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for research on multiple myeloma .
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 .
3
Research Areas:
Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
1
1 Cited Publications
Research Areas:
GRK2 Inhibitor 2 is an orally active and selective G protein-coupled receptor kinase 2 (GRK) inhibitor with an IC50 of 19 nM. GRK2 Inhibitor 2 also inhibits Aurora-A with an IC50 of 137 nM. GRK2 Inhibitor 2 can be used in the study of congestive heart failure (HF) .
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 .
Cat. No.: HY-W355700
CAS No.: 89576-29-4
Target:
Research Areas:
1-oleoyl-sn-glycero-3-phosphoethanolamine (LysoPE 18:1) is a lysophosphatidylethanolamine molecule involved in phospholipid metabolism, targeting cell membrane receptors (such as G protein-coupled receptors) to regulate cell signaling pathways. 1-oleoyl-sn-glycero-3-phosphoethanolamine may activate mitogen-activated protein kinase (MAPK) signaling, promote cell migration, regulate inflammatory responses and lipid metabolism, and has both pro-inflammatory and anti-inflammatory activities. 1-oleoyl-sn-glycero-3-phosphoethanolamine is mainly used in the screening of biomarkers for metabolic diseases (such as non-alcoholic fatty liver disease and obesity), as well as the study of the mechanism of lysophospholipids in cell membrane homeostasis and signal transduction .
Category:
Target:
Cat. No.: HY-123520
CAS No.: 864082-35-9
Research Areas:
GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and PKA inhibitor .
Cat. No.: HY-W036034A
CAS No.: 5423-98-3
Research Areas:
GRK-IN-1 is a potential G protein-coupled receptor kinase (GRK) inhibitor.
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-P1396
CAS No.: 148505-03-7
Research Areas:
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-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-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-15589R
CAS No.: 885101-89-3
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
GW9508 (Standard) is the analytical standard of GW9508. This product is intended for research and analytical applications. GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
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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
