PKA

PKA Products

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  • PKA Inhibitors (11)
  • PKA Activators (2)
  • PKA Antagonist (1)
  • New PKA Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1582 H 89 2HCl 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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Commun Signal, 2024, 22(1):48
iScience, 2024, 27(3):109125
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. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
Nat Commun, 2024, 15(1):489
Nat Commun, 2024, 15(1):1300
Mol Syst Biol, 2024, 20(1):28-55
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.
Cancer Res, 2023, 83(19):3237-3251
Biomed Pharmacother, 2023, 158:114176
Cancer Metab, 2023, 11(1):26
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.
PeerJ, 2023, 11:e15494
Alcohol, 2023, 115:5-12
medRxiv, 2023, 10.1101/2023.12.19.23299785
S7858 Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.
Regen Ther, 2024, 25:229-237
Biology (Basel), 2024, 13(1)58
Nat Commun, 2023, 14(1):3212
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.
J Biol Chem, 2024, 300(2):105641
Nat Commun, 2023, 14(1):886
Exp Gerontol, 2023, 173:112091
S7857 8-Bromo-cAMP 8-bromo-cAMP (8-Br-Camp) 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.
Protein Cell, 2023, 14(4):262-278
Reprod Biol Endocrinol, 2023, 21(1):99
Reprod Biol Endocrinol, 2023, 21(1):99
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.
Ecotoxicol Environ Saf, 2023, 257:114940
Mol Biol Cell, 2023, 34(8):ar79
Nat Commun, 2022, 13(1):1768
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. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM.
Elife, 2021, 10e68473
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.
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 2HCl 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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Commun Signal, 2024, 22(1):48
iScience, 2024, 27(3):109125
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. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
Nat Commun, 2024, 15(1):489
Nat Commun, 2024, 15(1):1300
Mol Syst Biol, 2024, 20(1):28-55
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.
Cancer Res, 2023, 83(19):3237-3251
Biomed Pharmacother, 2023, 158:114176
Cancer Metab, 2023, 11(1):26
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.
PeerJ, 2023, 11:e15494
Alcohol, 2023, 115:5-12
medRxiv, 2023, 10.1101/2023.12.19.23299785
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.
J Biol Chem, 2024, 300(2):105641
Nat Commun, 2023, 14(1):886
Exp Gerontol, 2023, 173:112091
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.
Ecotoxicol Environ Saf, 2023, 257:114940
Mol Biol Cell, 2023, 34(8):ar79
Nat Commun, 2022, 13(1):1768
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. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV 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.
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
S7858 Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.
Regen Ther, 2024, 25:229-237
Biology (Basel), 2024, 13(1)58
Nat Commun, 2023, 14(1):3212
S7857 8-Bromo-cAMP 8-bromo-cAMP (8-Br-Camp) 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.
Protein Cell, 2023, 14(4):262-278
Reprod Biol Endocrinol, 2023, 21(1):99
Reprod Biol Endocrinol, 2023, 21(1):99
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.

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