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PKA Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
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E4790 H-89 H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 values of 48 nM and has weak inhibition against PKG, PKC, Casein Kinase, and other kinases.
Molecular Cancer Therapeutics, May 2016, 1053-1062
Molecular Pharmacology, January 2020, 2-8
Investigative Ophthalmology & Visual Science, February 2020, 1
E7109 PKI(5-24) PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. It can be used for research to study hormonal regulation of the CAMP-dependent protein kinase.
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.
Oncotarget, November 13, 2018, 35962-35973
Biochemical Journal, May 1, 2014, 513-524
Acta Pharmacologica Sinica, July 23, 2018, 1902-1912
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S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
RSC Adv, 2026, 16(20):18359-18373
Theranostics, 2025, 15(18):9819-9837
Cell Rep, 2025, 44(7):115947
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S1573 Fasudil (HA-1077) Hydrochloride 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.
bioRxiv, March 20 2024, nan
Translational Vision Science & Technology, June 20 2017, 22
PeerJ, June 06 2023, e15494
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S2670 A-674563 HCl A-674563 HCl is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.
PLOS ONE, February 22, 2018, e0193344
Journal for ImmunoTherapy of Cancer, February 06, 2019, 33
Nat Commun, 2025, 16(1):3012
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S8388 ML-7 HCl ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively.
Proc Natl Acad Sci U S A, 2025, 122(8):e2421717122
Cell Mol Life Sci, 2025, 82(1):201
Commun Biol, 2025, 8(1):607
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S7563 AT13148 AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Cancers (Basel), 2022, 14(23)5943
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
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S2554 Daphnetin Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.
Sci Rep, 2021, 11(1):11491
Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
Int Immunopharmacol, 2019, 72:195-203
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S0754 Bisindolylmaleimide IV Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. This compound also inhibits PKA with IC50 of 11.8μM. It is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM.
Elife, 2021, 10e68473
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 Reports Medicine, August 2025, 102297
Cell Rep Med, 2025, 6(8):102297
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
E7359 A-674563 A-674563 is a selective, orally active inhibitor of Akt1 with a Ki of 11 nM. It also inhibits PKA with Ki of 16 nM and CDK2 with Ki of 46 nM. This compound reduces Akt downstream target phosphorylation and inhibits tumor cell proliferation in vitro with an EC50 of 0.4 µM.