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CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2(Gprotein-coupledreceptorkinase 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 .
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 Gprotein-coupledreceptorkinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
CCG215022 is a Gprotein-coupledreceptorkinases (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.
GRK6-IN-2 (compound 10a) is a potent inhibitor of Gprotein-coupledreceptorkinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for the research of multiple myeloma .
CCG258208 (GRK2-IN-1) is a potent and selective GRK2(Gprotein-coupledreceptorkinase 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 .
GRK5-IN-3 is a covalent inhibitor of GRK5(GProtein-CoupledReceptorKinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively .
GRL093-22 is a potent and selective Gprotein-coupledreceptorkinase (GRK) inhibitor, with IC50s of 60 and 40 nM for GRK5 and GRK6, respectively. GRL093-22 has the potential for the research of heart failure and multiple myeloma .
CCG-224406 is a selective Gprotein-coupledreceptorkinase 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 .
GRK2 Inhibitor 2 is an orally active and selective Gprotein-coupledreceptorkinase 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) .
GRL-098-22 (Compound 6t) is a potent inhibitor targeting Gprotein-coupledreceptorkinase 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 .
CCG273441 is a covalent inhibitor of Gprotein-coupledreceptor (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 .
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 .
GSK2163632A is a selective Gprotein-coupledreceptorkinase (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 receptorIGF-1R. GSK2163632A binds to GRK2 in a manner similar to Paroxetine (HY-122272).
(E/Z)-Locostatin ((E/Z)-UIC-1005) is a racemic of Locostatin. 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 Gprotein-coupledreceptorkinase 2. Locostatin inhibits cell proliferation and migration. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
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 Gprotein-coupledreceptorkinase 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 .
GRK2i is a Gβγ-inhibitory peptide that selectively prevents Gβγ-mediated signaling. GRK2i corresponds to the Gβγ-binding domain of GRK2 (G-protein-coupledreceptorkinase 2) .
KR-39038 is an orally active and potent GRK5 (Gprotein-coupledreceptorkinase 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 .
ProteinKinase C Peptide Substrate is targeted to a specific cellular compartment in a manner dependent on second messengers and on specific adapter proteins in response to extracellular signals that activate G-protein-coupledreceptors, tyrosine kinasereceptors, or tyrosine kinase-coupledreceptors. ProteinKinase C Peptide Substrate then regulates various physiological functions including the activation of nervous, endocrine, exocrine, inflammatory, and immune systems .
GW9508 is a potent and selective Gprotein-coupledreceptors 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 .
GRK6-IN-4 is a Gprotein coupledreceptor 6 kinase (GRK6) inhibitor with an IC50 of 1.56 μM. GRK6-IN-4 can be utilized in research related to hematological malignancies, inflammatory diseases, and autoimmune disorders .
(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 Gprotein-coupledreceptorkinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (Gprotein-coupledreceptorkinase 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.
GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupledreceptorkinase 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 .
(S)-Ro 32-0432 free base is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 free base 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 free base is also a selective Gprotein-coupledreceptorkinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 free base prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
GW9508 (Standard) is the analytical standard of GW9508. This product is intended for research and analytical applications. GW9508 is a potent and selective Gprotein-coupledreceptors 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 .
1-oleoyl-sn-glycero-3-phosphoethanolamine (LysoPE 18:1) is a lysophosphatidylethanolamine molecule involved in phospholipid metabolism, targeting cell membrane receptors (such as Gprotein-coupledreceptors) to regulate cell signaling pathways. 1-oleoyl-sn-glycero-3-phosphoethanolamine may activate mitogen-activated proteinkinase (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 .
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lynkinase and the αi subunits of inhibitory Gprotein-coupledreceptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
PIK3CG Recombinant Human Active Lipid Kinase belongs to PI3K enzyme family that is directly regulated by Gβγ and Ras in the Gprotein coupledreceptor (GPCR) pathway. PIK3CG has the function of regulating cellular inflammation and immunity. PIK3CG is also a potential target for the treatment of a few malignant tumors such as acute lymphoblastic leukemia, medulloblastoma, claudin-low breast cancer (CLBC) and Kaposi sarcoma .
Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for Gprotein-coupledreceptorkinase 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 .
LacCer (d18:1/16:0)-d3 (C16 Lactosylceramide (d18:1/16:0)-d3) is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory Gprotein-coupledreceptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
GRK2i is a Gβγ-inhibitory peptide that selectively prevents Gβγ-mediated signaling. GRK2i corresponds to the Gβγ-binding domain of GRK2 (G-protein-coupledreceptorkinase 2) .
ProteinKinase C Peptide Substrate is targeted to a specific cellular compartment in a manner dependent on second messengers and on specific adapter proteins in response to extracellular signals that activate G-protein-coupledreceptors, tyrosine kinasereceptors, or tyrosine kinase-coupledreceptors. ProteinKinase C Peptide Substrate then regulates various physiological functions including the activation of nervous, endocrine, exocrine, inflammatory, and immune systems .
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lynkinase and the αi subunits of inhibitory Gprotein-coupledreceptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
GRK6 selectively phosphorylates activated G protein-coupled receptors, triggering beta-arrestin-mediated desensitization, internalization, and signaling events. It is implicated in desensitizing D2-like dopamine receptors in the striatum and chemokine receptor CXCR4, crucial for CXCL12-induced cell chemotaxis. Additionally, GRK6 phosphorylates rhodopsin (RHO) and the non-GPCR LRP6 during Wnt signaling, as observed in vitro. GRK6 Protein, Human (sf9, His-GST) is the recombinant human-derived GRK6 protein, expressed by Sf9 insect cells , with N-GST, N-His labeled tag.
LacCer (d18:1/16:0)-d3 (C16 Lactosylceramide (d18:1/16:0)-d3) is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory Gprotein-coupledreceptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
1-oleoyl-sn-glycero-3-phosphoethanolamine (LysoPE 18:1) is a lysophosphatidylethanolamine molecule involved in phospholipid metabolism, targeting cell membrane receptors (such as Gprotein-coupledreceptors) to regulate cell signaling pathways. 1-oleoyl-sn-glycero-3-phosphoethanolamine may activate mitogen-activated proteinkinase (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 .
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