GRK2

GRK2 관련 제품 (36):

By Type:	Pan (2) Selective (2)
By Effects:	Inhibitors (31) Modulators (2) Degrader (1)

Cat. No.	상품명	효과	Purity

HY-B0492

Paroxetine hydrochloride	Inhibitor	99.98%
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.

HY-103045

CMPD101	Inhibitor	98.96%
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.

HY-18991

CCG215022	Inhibitor	99.79%
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.

HY-109562A

CCG258208 hydrochloride		98.05%
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.

HY-121983

CAY10594	Modulator	98.64%
CAY10594 is an orally active PLD2 inhibitor with an IC₅₀ of 140 nM. CAY10594 has activities such as anti-tumor, anti-oxidation and liver protection. CAY10594 can be used for the research of diseases like breast cancer, acute liver injury and colitis.

HY-177948

GRK2 degrader-1	Degrader	98.83%
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.

HY-120718

CCG 224061	Inhibitor
CCG 224061 is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with a IC₅₀ of 0.066 μM. CCG 224061 inhibits GRK activity in cardiomyocytes. CCG 224061 is applicable to research related to heart disease, heart failure, myocardial hypertrophy and hypertension.

HY-120168

CCG 258001	Inhibitor
CCG 258001 is a GRK inhibitor with IC₅₀ values of 0.29, 51.8, and 33 µM against GRK2, GRK1, and GRK5, respectively. CCG 258001 inhibits GRK activity in cardiomyocytes and other muscle cells. CCG 258001 is applicable to the research of heart diseases, including heart failure, myocardial hypertrophy, and hypertension.

HY-156863

GRK2 Inhibitor 2	Inhibitor	99.92%
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).

HY-W013411A

Locostatin	Inhibitor	99.88%
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 .

HY-18990

GSK180736A	Inhibitor	98.81%
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.

HY-B0492A

Paroxetine hydrochloride hemihydrate	Inhibitor	99.96%
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.

HY-47573

CCG273441	Inhibitor	98.78%
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.

HY-123538

GRK2 Inhibitor 1	Inhibitor	98.06%
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.

HY-139690

CCG258747	Inhibitor	98.96%
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).

HY-P1396A

GRK2i TFA	Inhibitor	99.89%
GRK2i TFA is a GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. GRK2i TFA corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist.

HY-129118

Takeda103A	Inhibitor	98.69%
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.

HY-RS05813

GRK2 Human Pre-designed siRNA Set A	Inhibitor
GRK2 Human Pre-designed siRNA Set A contains three designed siRNAs for GRK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-109562

CCG258208	Inhibitor
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.

HY-B0492R

Paroxetine hydrochloride (Standard)	Inhibitor
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.

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