| S1421 |
Staurosporine (STS)
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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.
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Cell Metab, 2025, S1550-4131(25)00149-4
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Mol Cell, 2025, 85(19):3711-3728.e11
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EMBO J, 2025, 10.1038/s44318-025-00526-w
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| S0152 |
PKG drug G1
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PKG drug G1 is an activater of Protein Kinase G Iα (PKG Iα) targeting C42, resulting vasodilation and blood pressure lowering.
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Front Pharmacol, 2022, 13:1028046
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| S2964 |
HA-100 dihydrochloride
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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.
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Adv Sci (Weinh), 2024, 11(4):e2304987
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| S0378 |
MBP146-78
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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.
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| E2646 |
HA-100
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HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase.
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| S1582 |
H-89 Dihydrochloride
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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.
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Nat Commun, 2025, 16(1):7115
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Nucleic Acids Res, 2025, 53(17)gkaf882
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Cell Rep Med, 2025, 6(8):102254
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| S1573 |
Fasudil (HA-1077) Hydrochloride
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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.
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Stem Cell Res Ther, 2025, 16(1):597
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Transl Oncol, 2025, 51:102209
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J Immunother Cancer, 2024, 12(11)e009805
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| S6214 |
H-1152 dihydrochloride
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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.
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Cell Rep Med, 2025, 6(8):102297
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