| 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
-
Cell Rep Med, 2025, 6(8):102254
-
Transl Neurodegener, 2025, 14(1):43
|
|
| 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
|
|
| 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. This compound also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. It 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 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. |
-
Transl Oncol, 2025, 51:102209
-
J Immunother Cancer, 2024, 12(11)e009805
-
Sci China Life Sci, 2024, 67(8):1549-1562
|
|
| S7858 |
Dibutyryl 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
|
|
| 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. |
-
Nat Commun, 2025, 16(1):3012
-
J Biol Chem, 2024, 300(2):105641
-
Nat Commun, 2023, 14(1):886
|
|
| S7857 |
8-Bromo-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
|
|
| 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. |
-
Cell Mol Life Sci, 2025, 82(1):201
-
Commun Biol, 2025, 8(1):607
-
Commun Biol, 2025, 8(1):1190
|
|
| 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
|
|
| 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
|
|
| 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
|
|
| F1294 |
PKA RI-α Antibody [J14D6]
|
|
|
|
| E4790New |
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
-
Sci Adv, 2025, 11(23):eadt3552
|
|
| E7109New |
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
|
|
| E7359New |
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. |
|
|
| 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. |
|
|
| 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
|
|
| 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
- Cell Rep Med, 2025, 6(8):102254
- Transl Neurodegener, 2025, 14(1):43
|
|
| 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
|
|
| 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. This compound also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. It 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 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. |
- Transl Oncol, 2025, 51:102209
- J Immunother Cancer, 2024, 12(11)e009805
- Sci China Life Sci, 2024, 67(8):1549-1562
|
|
| 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. |
- Nat Commun, 2025, 16(1):3012
- J Biol Chem, 2024, 300(2):105641
- Nat Commun, 2023, 14(1):886
|
|
| 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. |
- Cell Mol Life Sci, 2025, 82(1):201
- Commun Biol, 2025, 8(1):607
- Commun Biol, 2025, 8(1):1190
|
|
| 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
|
|
| 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
|
|
| 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
|
|
| E4790New |
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
- Sci Adv, 2025, 11(23):eadt3552
|
|
| E7109New |
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. |
|
|
| E7359New |
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. |
|
|
| 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
|
|
| 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
|
|