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GPCR & G Protein

CGRP Receptor Endothelin Receptor S1P Receptor Cannabinoid Receptor Hedgehog/Smoothened SGLT Opioid Receptor GPR CCR MT Receptor LPA Receptor PAFR OX Receptor PKA CaSR cAMP Vasopressin Receptor Protease-activated Receptor Adenosine Receptor Glucagon Receptor TAAR GRK AdipoR Prostaglandin Receptor CCK receptor GHSR Guanylate Cyclase GPCR19 GPR139 NPY receptor PAR TAS1R Sigma Receptor RGS Imidazoline Receptor Angiotensin Receptor PKG Neurokinin Receptor FPR DOCK Taste Receptor Melanocortin Receptor Somatostatin Receptor Bombesin Receptor Bradykinin Receptor CRFR GNRH Receptor TSH Receptor Parathyroid Hormone Receptor GLP-1 Receptor Adenylyl Cyclase Apelin receptor Arrestin MCHR Orphan Receptor Oxytocin Receptor Platelet aggregation RXFP receptor
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  • PKG Inhibitors (7)
  • PKG Activator (1)
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Cat.No. Product Name Information Product Use Citations Product Validations
S0152 PKG drug G1 PKG drug G1 is an activater of Protein Kinase G Iα (PKG Iα) targeting C42, resulting vasodilation and blood pressure lowering.
Front Pharmacol, 2022, 13:1028046
S0378 MBP146-78 MBP146-78 is a potent and selective inhibitor of cyclic GMP(cGMP)-dependent protein kinases/Protein Kinase G (PKG) and displays cytostatic activity against Toxoplasma gondii.
E2646 HA-100 HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase.
S2964 HA-100 dihydrochloride HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively.
Adv Sci (Weinh), 2024, 11(4):e2304987
S1582 H-89 Dihydrochloride H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy.
Nat Commun, 2025, 16(1):7115
Nucleic Acids Res, 2025, 53(17)gkaf882
Cell Rep Med, 2025, 6(8):102254
Verified customer review of H-89 Dihydrochloride
S1421 Staurosporine (STS) Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. This compound also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
Cell Metab, 2025, S1550-4131(25)00149-4
Mol Cell, 2025, 85(19):3711-3728.e11
EMBO J, 2025, 10.1038/s44318-025-00526-w
Verified customer review of Staurosporine (STS)
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Stem Cell Res Ther, 2025, 16(1):597
Transl Oncol, 2025, 51:102209
J Immunother Cancer, 2024, 12(11)e009805
Verified customer review of Fasudil HCl
S6214 H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
Cell Rep Med, 2025, 6(8):102297
S0378 MBP146-78 MBP146-78 is a potent and selective inhibitor of cyclic GMP(cGMP)-dependent protein kinases/Protein Kinase G (PKG) and displays cytostatic activity against Toxoplasma gondii.
E2646 HA-100 HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase.
S2964 HA-100 dihydrochloride HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively.
Adv Sci (Weinh), 2024, 11(4):e2304987
S1582 H-89 Dihydrochloride H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy.
Nat Commun, 2025, 16(1):7115
Nucleic Acids Res, 2025, 53(17)gkaf882
Cell Rep Med, 2025, 6(8):102254
 Verified customer review of H-89 Dihydrochloride
S1421 Staurosporine (STS) Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. This compound also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
Cell Metab, 2025, S1550-4131(25)00149-4
Mol Cell, 2025, 85(19):3711-3728.e11
EMBO J, 2025, 10.1038/s44318-025-00526-w
 Verified customer review of Staurosporine (STS)
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Stem Cell Res Ther, 2025, 16(1):597
Transl Oncol, 2025, 51:102209
J Immunother Cancer, 2024, 12(11)e009805
 Verified customer review of Fasudil HCl
S6214 H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
Cell Rep Med, 2025, 6(8):102297
S0152 PKG drug G1 PKG drug G1 is an activater of Protein Kinase G Iα (PKG Iα) targeting C42, resulting vasodilation and blood pressure lowering.
Front Pharmacol, 2022, 13:1028046