PKA inhibitors/activators

Other GPCR & G Protein Related Inhibitors

Hedgehog/Smoothened CGRP Receptor Endothelin Receptor S1P Receptor Cannabinoid Receptor SGLT Opioid Receptor GPR CCR MT Receptor

Cat.No.	Product Name	Information	Product Use Citations
S7858	Dibutyryl cAMP (db cAMP/Bucladesine) sodium	Bucladesine sodium is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.	Cell, 2025, S0092-8674(25)00735-4 Nat Neurosci, 2025, 28(6):1174-1184 Nat Commun, 2025, 16(1):6151
S7857	8-Bromo-cAMP (8-Br-cAMP) Sodium Salt	8-Bromo-cAMP sodium salt is a cell permeable analog of cAMP that activates cyclic-AMP-dependent protein kinase with a Ka value of 0.05 μM; and a PKA activator.	Nat Cell Biol, 2025, NONE Stem Cell Res Ther, 2025, 16(1):336 Elife, 2024, 13RP97507
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
S1582	H-89 Dihydrochloride	H 89 2HCl is a potent PKA inhibitor with K_i 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
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.	Nat Commun, 2025, 16(1):7898 Stem Cell Res Ther, 2025, 16(1):200 Sci Adv, 2025, 11(23):eadt3552
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.
E4793	Bucladesine calcium	Bucladesine calcium (Dibutyryl-cAMP Calcium Salt, DBcAMP calcium salt) is a cell-permeable analog of cyclic AMP. It serves as a potent activator of protein kinase A (PKA) and mimics the effects of endogenous cAMP. It also inhibits phosphodiesterase (PDE) activity, with the potential to treat congestive heart failure, wound healing, and inflammation.	Regen Ther, 2025, 29:499-505
E2506	A-3 hydrochloride	A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively.
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.	Theranostics, 2025, 15(18):9819-9837 Cell Rep, 2025, 44(7):115947 Front Cell Infect Microbiol, 2025, 15:1543186
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.	Stem Cell Res Ther, 2025, 16(1):597 Transl Oncol, 2025, 51:102209 J Immunother Cancer, 2024, 12(11)e009805