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Requires G-protein for activation and therefore belongs to the family of G-protein-dependent receptor kinases (GRKs). All members of this enzyme subfamily possess a highly conserved binding site for 1-phosphatidylinositol 4,5-bisphosphate. (cf. EC 2.7.11.14, rhodopsin kinase and EC 2.7.11.15, β-adrenergic-receptor kinase). Group: Enzymes. Synonyms: G protein-coupled receptor kinase; GPCR kinase; GPCRK; GRK4; GRK5; GRK6; STK16. Enzyme Commission Number: EC 2.7.11.16. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3135; G-protein-coupled receptor kinase; EC 2.7.11.16; G protein-coupled receptor kinase; GPCR kinase; GPCRK; GRK4; GRK5; GRK6; STK16. Cat No: EXWM-3135.
(2, 6-Dichlorophenyl) methanamine
(2, 6-Dichlorophenyl) methanamine was one of the reactants used in making a library of highly selective and potent G protein-coupled receptor kinase 2 inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 6575-27-5. Pack Sizes: 250mg, 1g. Molecular Formula: C7H7Cl2N, Molecular Weight: 176.04. US Biological Life Sciences.
A pyrimidine derivative as G protein-coupled receptor kinase (GRK) inhibitor. Group: Biochemicals. Alternative Names: 5-(Bromomethyl)-2-methyl-4-pyrimidinamine Hydrobromide. Grades: Highly Purified. CAS No. 5423-98-3. Pack Sizes: 50mg. US Biological Life Sciences.
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4-Amino-5-ethoxymethyl-2-methylpyrimidine
A pyrimidine derivative as G protein-coupled receptor kinase (GRK) inhibitor. Group: Biochemicals. Alternative Names: 5-Ethoxymethyl-2-methyl-4-pyrimidinamine. Grades: Highly Purified. Pack Sizes: 100mg. US Biological Life Sciences.
Worldwide
5-(Ethoxymethyl)-2-methyl-4-pyrimidinone
5-(Ethoxymethyl)-2-methyl-4-pyrimidinone has been shown to increase locomotor activity in mice. Intermediate in the preparation of G protein-coupled receptor kinase (GRK) inhibitor. Group: Biochemicals. Alternative Names: 5-(Ethoxymethyl)-2-methyl-4(3H)-pyrimidinone, NSC 13143; NSC 51126; NSC 51127. Grades: Highly Purified. CAS No. 5423-97-2. Pack Sizes: 1g. US Biological Life Sciences.
Worldwide
Adenosine-5'-(γ-thio)-triphosphate tetralithium salt
Adenosine 5-[γ-thio]triphosphate Tetralithium Salt is used as a reagent in the synthesis of DNA N-acetylglucosamine analogs. Adenosine 5'-(γ-thio)-triphosphate (lithium salt) is a stable analog of ATP that acts as a potent agonist of G protein-coupled P2Y2 and P2Y11 receptors (pEC50 = 5.52 for P2Y11).1 It has been used to identify kinase substrates, has been implemented as a reagent in the synthesis of DNA N-acetylglucosamine analogs, and can serve as a substrate for the RNA-stimulated nucleotide hydrolysis and RNA unwinding activities of eukaryotic initiation factor-4A. Group: Biochemicals. Alternative Names: ATP-γS; ATPγS tetralithium salt. Grades: Highly Purified. CAS No. 93839-89-5. Pack Sizes: 1mg, 5mg, 10mg. Molecular Formula: C??H??N?O??P?SLi?, Molecular Weight: 551. US Biological Life Sciences.
Worldwide
ATPγS
ATPγS is an agonist of G protein-coupled P2Y2 and P2Y11 receptors (pEC50 = 5.52 for P2Y11). It has been used to identify kinase substrates, used as a reagent in the synthesis of DNA N-acetylglucosamine analogs and a substrate for the RNA-stimulated nucleotide hydrolysis as well as RNA unwinding activities of eukaryotic initiation factor-4A. Uses: Atpγs is an agonist of g protein-coupled p2y2 and p2y11 receptors (pec50 = 5.52 for p2y11). Synonyms: Adenosine-5'-(γ-thio)-triphosphate, Tetralithium salt; Adenosine-5'-(3-thio)-triphosphate, Adenosine-5'-(3-thiotriphosphate). Grades: ≥ 90% by HPLC, contains < 10% ADP. Molecular formula: C10H16N5O12P3S (free acid). Mole weight: 523.24 (free acid).
ATPγS tetralithium salt
Adenosine 5'-(γ-thio)-triphosphate lithium salt is a stable analog of ATP. It is a potent agonist of G protein-coupled P2Y2 and P2Y11 receptors. Adenosine 5'-(γ-thio)-triphosphate has also been used to identify kinase substrates and can serve as a substrate for the RNA-stimulated nucleotide hydrolysis and RNA unwinding activities of eukaryotic initiation factor-4A. Uses: Affinity labels. Synonyms: Adenosine-5'-(γ-thio)-triphosphate tetralithium salt. Grades: ≥90% by HPLC. CAS No. 93839-89-5. Molecular formula: C10H12Li4N5O12P3S. Mole weight: 546.98.
βARK1 Inhibitor
βARK1 inhibitor is an inhibitor of G protein-coupled receptor kinase 2/β-adrenergic receptor kinase 1 (GRK2/βARK1) with IC50 value of 126 μM. It has been shown to decrease systolic blood pressure in ob/ob and nicotinamide plus streptozotocin-induced mouse models of type 2 diabetes when administered at a dose of 200 μg/kg. Synonyms: betaARK1 Inhibitor; Methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate; GRK2 Inhibitor. Grades: ≥95% (mixture of isomers). CAS No. 24269-96-3. Molecular formula: C12H9NO6. Mole weight: 263.2.
Bisindolylmaleimide XI Hydrochloride
Selective cell permeable protein kinase C (PKC) inhibitor. G protein-coupled receptor kinase (GRK-5) inhibitor. Less potent GRK-2 or GRK-3 inhibitor. Prevents T cell-driven chronic inflammatory responses in vivo. Group: Biochemicals. Alternative Names: Ro 32-0432, BIM XI. Grades: Highly Purified. CAS No. 145333-02-4. Pack Sizes: 1mg, 5mg. Molecular Formula: C28H28N4O2 HCl. US Biological Life Sciences.
Worldwide
CCG215022
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor (IC50s= 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively), with good selectivity against other closely related kinases such as GRK1 and PKA. Synonyms: 4-(4-fluoro-3-((pyridin-2-ylmethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide; CCG215022; CCG 215022; CCG-215022. CAS No. 1813527-81-9. Molecular formula: C26H22FN7O3. Mole weight: 499.5.
CCG-224406
CCG-224406 is a highly selective and potent inhibitor of G Protein-Coupled Receptor Kinase 2 (IC50= 130 nM), with 700-fold selectivity over other GRK subfamilies, and no detectable inhibition of ROCK1. Synonyms: CCG 224406; CCG224406; N-(1H-Indazole-5-yl)-2-oxo-4-[3-(2,6-dimethoxybenzylcarbamoyl)-4-fluorophenyl]-6-methyl-1,2,3,4-tetrahydropyrimidine-5-carboxamide. Grades: >98%. CAS No. 1870843-22-3. Molecular formula: C29H27FN6O5. Mole weight: 558.57.
CCG258208 hydrochloride
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 ?M) and more than 2500-fold selectivity over GRK1 (IC50=87.3 ?M), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research[1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: GRK2-IN-1 hydrochloride. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-109562A.
CCG273441
CCG273441 is a covalent inhibitor of G protein-coupled receptor ( GPCR ) kinase 5 ( GRK5 ) with an IC 50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC 50 =4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2750414-35-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-47573.
GRK2 Inhibitor 2
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]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2592436-21-8. Pack Sizes: 5 mg; 10 mg; 25 mg. Product ID: HY-156863.
GSK-270822A
GSK-270822A is a G protein-coupled receptor kinases(GRK2) inhibitor, which has been directly implicated in the progression of heart failure. It would be used as useful chemical probes and leads for therapeutic applications ranging from heart failure to Parkinson's disease. Uses: Gsk-270822a would be used as useful chemical probes and leads for therapeutic applications ranging from heart failure to parkinson's disease. Synonyms: GSK270822A; GSK 270822A; N-(1H-indazol-5-yl)-2-methyl-4-(naphthalen-2-yl)-6-oxo-1,4,5,6-tetrahydropyridine-3-carboxamide; NSC-756163. Grades: 98%. CAS No. 864082-23-5. Molecular formula: C24H20N4O2. Mole weight: 396.45.
GW9508
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[1][2][3][4]. Uses: Scientific research. Group: Signaling pathways. CAS No. 885101-89-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15589.
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 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] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: UIC-1005. CAS No. 90719-30-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg. Product ID: HY-W013411A.
Pamoic Acid
Agonist of the orphan G protein-coupled receptor GPR35: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Used as an inhibitor in the real-time fluorescence enzymatic characterization study of specialized human DNA polymerases. Group: Biochemicals. Grades: Highly Purified. CAS No. 130-85-8. Pack Sizes: 1g. US Biological Life Sciences.
Worldwide
Protein Kinase C Peptide Substrate
Protein Kinase C Peptide Substrate targets specific cell compartents and activates G protein-coupled receptors, tyrosine kinase receptors or tyrosine kinase-coupled receptors by relying on second messenger and specific adaptor proteins in response to extracellular signals. Protein Kinase C Peptide Substrate regulates a variety of physiological functions, including nervous, endocrine, exocrine, inflammatory and immune system activation. Synonyms: PKCε; PRKCE; Peptide Epsilon; PKC epsilon; H-Glu-Arg-Met-Arg-Pro-Arg-Lys-Arg-Gln-Gly-Ser-Val-Arg-Arg-Arg-Val-OH; L-alpha-glutamyl-L-arginyl-L-methionyl-L-arginyl-L-prolyl-L-arginyl-L-lysyl-L-arginyl-L-glutaminyl-glycyl-L-seryl-L-valyl-L-arginyl-L-arginyl-L-arginyl-L-valine. Grades: 95%. CAS No. 120253-69-2. Molecular formula: C83H155N39O21S. Mole weight: 2067.43.
Protein Kinase C Peptide Substrate acetate
Protein Kinase C Peptide Substrate acetate targets specific cell compartments and activates G protein-coupled receptors, tyrosine kinase receptors, or tyrosine kinase-coupled receptors by relying on second messenger and specific adaptor proteins in response to extracellular signals. It regulates a variety of physiological functions, including nervous, endocrine, exocrine, inflammatory, and immune system activation. Synonyms: L-α-Glutamyl-L-arginyl-L-methionyl-L-arginyl-L-prolyl-L-arginyl-L-lysyl-L-arginyl-L-glutaminylglycyl-L-seryl-L-valyl-L-arginyl-L-arginyl-L-arginyl-L-valine acetate; H-Glu-Arg-Met-Arg-Pro-Arg-Lys-Arg-Gln-Gly-Ser-Val-Arg-Arg-Arg-Val-OH acetate. Grades: ≥95%. Molecular formula: C85H159N39O23S. Mole weight: 2127.52.
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