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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
28 Results for "
GRK2 inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "GRK2 inhibitor" in MCE Product Catalog:
6
6 Publications Verification
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:
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 .
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:
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
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) .
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
Cat. No.: HY-P1396A
Research Areas:
Research Areas:
GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a dual GRK2/β-ARK1 inhibitor that induces dopamine (DA) inhibition reversal (DIR). GRK2 Inhibitor 1 can also block serotonin-induced or neurotensin-induced DIR reversal. Note: DIR refers to the phenomenon in which neurons in addiction-related brain pathways become less sensitive to DA inhibition when exposed to moderate concentrations of DA for a long time .
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-B0492S1
CAS No.: 2714485-95-5
Synonyms: BRL29060-d4 hydrochloride; BRL29060A-d4
Cat. No.: HY-177948
CAS No.: 3052947-04-0
Research Areas:
GRK2 degrader-1 (compound 1) is a potent and orally active GRK2 degrader. GRK2 degrader-1 degrades GRK2 via the ubiquitin-proteasome pathway. GRK2 degrader-1 inhibits right ventricular remodeling and elevation of pulmonary artery pressure in a pulmonary artery hypertension (PAH) mouse model. GRK2 degrader-1 can be used for PAH research .
Cat. No.: HY-168971
CAS No.: 1390658-79-3
Synonyms: CP-25
Target:
IFNAR STAT TNF Receptor Interleukin Related CXCR JAK G Protein-coupled Receptor Kinase (GRK)
Research Areas:
Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model .
Cat. No.: HY-103045A
CAS No.: 1941168-71-3
Research Areas:
CMPD101 hydrochloride is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 hydrochloride also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s =1.4 μM and 8.1 μM, respectively) .
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).
Research Areas:
Takeda103A is a potent inhibitor of GRK2. G protein-coupled receptors (GPCRs) are central to many physiological processes. Takeda103A has the potential for the research of heart failure .
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 .
Cat. No.: HY-B0492AR
CAS No.: 110429-35-1
Synonyms: BRL29060 hydrochloride hemihydrate (Standard); BRL29060A hemihydrate (Standard)
Research Areas:
Paroxetine (hydrochloride hemihydrate) (Standard) is the analytical standard of Paroxetine (hydrochloride hemihydrate). This product is intended for research and analytical applications. Paroxetine hydrochloride hemihydrate is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14?μM.
Cat. No.: HY-B0492R
CAS No.: 78246-49-8
Synonyms: BRL29060 hydrochloride (Standard); BRL29060A (Standard)
Research Areas:
Paroxetine (hydrochloride) (Standard) is the analytical standard of Paroxetine (hydrochloride). This product is intended for research and analytical applications. Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder .
Cat. No.: HY-123254
CAS No.: 1870843-22-3
Research Areas:
CCG-224406 is a selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with the IC50 values of 13 nM, greater than 700-fold selectivity over other GRK subfamilies, and no inhibition of ROCK1. CCG-224406 can be used for study of heart failure .
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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
