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PKA-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (3) Biochemical Assay Reagents (1) CaMK (1) CDK (1) Drug Derivative (1) Drug Intermediate (1) Endogenous Metabolite (1) ERK (3) G Protein-coupled Receptor Kinase (GRK) (1) MEK (1) Nuclear Factor of activated T Cells (NFAT) (1) P2Y Receptor (1) p38 MAPK (2) Pim (1) PKA (11) PPAR (2) Raf (1) Ras (1) Reactive Oxygen Species (ROS) (1) Reference Standards (2) Serpin (1) SphK (1)
By Research Areas:	Cancer (7) Cardiovascular Disease (1) Endocrinology (2) Inflammation/Immunology (2) Metabolic Disease (5) Neurological Disease (1)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N2118

Bilobetin 2 Publications Verification	PPAR PKA Akt p38 MAPK ERK	Metabolic Disease
Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and *PKA* activity .

HY-115732

*PKA-IN-1* 1 Publications Verification	PKA	Inflammation/Immunology
PKA-IN-1 is a potent and selective cyclic AMP-dependent protein kinase (PKA) catalytic subunit (cAK) inhibitor with an IC₅₀ of 0.03 μM. PKA-IN-1 inhibits cAK in a fashion that is competitive with respect to ATP as substrate ^[1].

HY-175232

GL64	Nuclear Factor of activated T Cells (NFAT) Endogenous Metabolite	Endocrinology
GL64 is a selective agonist of ADGRD1 (EC₅₀ = 3.98 μM). GL64 has low selectivity for ADGRD2, ADGRG5, ADGRG6, CELSR1, CELSR2, CELSR3, and ADGRG4 isoforms. GL64 activates ADGRD1 by mimicking the satchel sequence. GL64 regulates osteoclast maturation through the cAMP-PKA-NFATC1 pathway. GL64 effectively inhibits osteoclastogenesis and prevents bone loss both in vitro and in vivo. GL64 is useful in the study of osteoclast-related diseases ^[1].

HY-W001242

1-(Tetrahydropyran-2-yl)-1H-pyrazole-5-boronic acid pinacol ester	Biochemical Assay Reagents Drug Intermediate	Others
1-(Tetrahydropyran-2-yl)-1H-pyrazole-5-boronic acid pinacol ester is a pharmaceutical intermediate used in the synthesis of naphthyl *FXIa/PKa** inhibitors* .

HY-136172

ESI-08 1 Publications Verification	Ras	Cardiovascular Disease Metabolic Disease Cancer
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both *EPAC1* and EPAC2 (IC₅₀ of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation .

HY-119016

SK1-I 1 Publications Verification BML-258	SphK CaMK	Cancer
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive *SPHK1* inhibitor with a K_i value of 10 μM ^[1]. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity .

HY-107544

8-pCPT-2'-O-Me-cAMP-AM	PKA	Metabolic Disease
8-pCPT-2'-O-Me-cAMP-AM is a cyclic AMP analogue, selectively activates Epac-Rap signaling pathway. 8-pCPT-2'-O-Me-cAMP-AM protects renal function by activating Epac from ischemia injury. 8-pCPT-2'-O-Me-cAMP-AM also stimulates insulin secretion by interaction with *PKA* pathway .

HY-P10336

Serpinin	Serpin	Neurological Disease Endocrinology
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function ^[1]. Serpinin is a selective agonist for β-adrenergic receptors. Serpinin interacts with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .

HY-123520

GSK299115A	G Protein-coupled Receptor Kinase (GRK) PKA	Cancer
GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and *PKA* inhibitor .

HY-N0521R

(-)-Gallocatechin (Standard)	Reference Standards Reactive Oxygen Species (ROS)	Metabolic Disease Cancer
(-)-Gallocatechin (Standard) is the analytical standard of (-)-Gallocatechin. This product is intended for research and analytical applications. (-)-Gallocatechin, an epimer of (-)-Epigallocatechin (EGC), is contained in various tea products. (-)-Gallocatechin has antioxidant activities. (-)-Gallocatechin is the main active component in green tea extract (HTP-GTE) responsible for its effect of improving age-related cognitive impairments involving protein kinase A (PKA) pathway .

HY-143898

PIM1-IN-4	Pim	Cancer
PIM1-IN-4 (Compound 8) is a potent inhibitor of *PIM1. PIM1-IN-4* reveals strong inhibition of five other enzymes, i.e., SGK-1, PKA, CaMK-1, GSK3β, and MSK1. PIM1-IN-4 has the potential for the research of cancer diseases ^[1].

HY-148868

Akt1&PKA-IN-1	Akt PKA CDK	Others
Akt1&PKA-IN-1 is a potent dual Akt/PKA inhibitor with IC₅₀ values of 0.03 , 0.11 μM, and 9.8 μM for PKAa, Akt, and CDK2, respectively. Akt1&PKA-IN-1 is selective for cyclin-dependent kinase 2 (CDK2) ^[1].

HY-179133

HDB-1	P2Y Receptor PKA Raf MEK ERK	Inflammation/Immunology
HDB-1 is a selective inhibitor of the P2Y14 receptor (P2Y14R) with an IC₅₀ of 26 pM. HDB-1 shows no significant inhibition on P2Y1R, P2Y2R, P2Y4R, P2Y6R, and P2Y12R. HDB-1 blocks the activation of hepatic stellate cells (HSC) by inhibiting the *PKA/Raf1/MEK/ERK* signaling pathway mediated by P2Y14R, thereby alleviating the core pathological process of liver fibrosis. HDB-1 can be used for the study of liver fibrosis ^[1].

HY-P10098

PKA Substrate	PKA	Cancer
PKA Substrate is a potent and selective substrate peptide of PKA that can be used to detect PKA activity .

HY-111159

CP-467688	Drug Derivative	Others
CP-467688 is a retinal toxicant with a basic pKa=8.1 and lipophilic clogP=5.0. CP-467688 is promising for research of drug-induced retinopathy ^[1].

HY-P3920

Cys-Kemptide	PKA	Cancer
Cys-Kemptide is a cysteine-terminated substrate peptide that can used to measure protein kinase A (PKA) activity .

HY-134298

8-CPT-6-Phe-cAMP 8-(4-Chlorophenylthio)-N6-phenyl-cAMP	PKA	Others
8-CPT-6-Phe-cAMP is an analogue of signal molecule cAMP and a potent protein kinase A (PKA) activator .

HY-P3745

H1-7 (histone H1 phosphorylation site), PKA Substrate	PKA	Others
H1-7 (histone H1 phosphorylation site), PKA Substrate, a synthetic polypeptide, can be used as PKA substrate .

HY-N2118R

Bilobetin (Standard)	Reference Standards PPAR PKA Akt p38 MAPK ERK	Metabolic Disease
Bilobetin (Standard) is the analytical standard of Bilobetin. This product is intended for research and analytical applications. Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity .

1-(Tetrahydropyran-2-yl)-1H-pyrazole-5-boronic acid pinacol ester	Biochemical Assay Reagents
1-(Tetrahydropyran-2-yl)-1H-pyrazole-5-boronic acid pinacol ester is a pharmaceutical intermediate used in the synthesis of naphthyl *FXIa/PKa** inhibitors* .

Cat. No.	Product Name	Target	Research Area

HY-P10336

Serpinin	Serpin	Neurological Disease Endocrinology
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function ^[1]. Serpinin is a selective agonist for β-adrenergic receptors. Serpinin interacts with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .

HY-P10098

PKA Substrate	PKA	Cancer
PKA Substrate is a potent and selective substrate peptide of PKA that can be used to detect PKA activity .

HY-P3920

Cys-Kemptide	PKA	Cancer
Cys-Kemptide is a cysteine-terminated substrate peptide that can used to measure protein kinase A (PKA) activity .

HY-P3745

H1-7 (histone H1 phosphorylation site), PKA Substrate	PKA	Others
H1-7 (histone H1 phosphorylation site), PKA Substrate, a synthetic polypeptide, can be used as PKA substrate .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2118

Bilobetin 2 Publications Verification	Flavonoids Ginkgoaceae Classification of Application Fields Phenols Polyphenols Metabolic Disease Plants Biflavones Ginkgo biloba Disease Research Fields Source Classification	PPAR PKA Akt p38 MAPK ERK
Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and *PKA* activity .

HY-N0521R

(-)-Gallocatechin (Standard)	Structural Classification Flavonoids Flavanols Phenols Polyphenols Camellia sinensis (L.) O. Ktze. Plants Source Classification Theaceae	Reference Standards Reactive Oxygen Species (ROS)
(-)-Gallocatechin (Standard) is the analytical standard of (-)-Gallocatechin. This product is intended for research and analytical applications. (-)-Gallocatechin, an epimer of (-)-Epigallocatechin (EGC), is contained in various tea products. (-)-Gallocatechin has antioxidant activities. (-)-Gallocatechin is the main active component in green tea extract (HTP-GTE) responsible for its effect of improving age-related cognitive impairments involving protein kinase A (PKA) pathway .

HY-N2118R

Bilobetin (Standard)	Structural Classification Flavonoids Ginkgoaceae Phenols Polyphenols Plants Biflavones Ginkgo biloba Source Classification	Reference Standards PPAR PKA Akt p38 MAPK ERK
Bilobetin (Standard) is the analytical standard of Bilobetin. This product is intended for research and analytical applications. Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity .

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PKA-IN-1

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

NaturalProducts

Natural
Products