PKA

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  • New PKA Products
Catalog No. Product Name Information Product Use Citations Product Validations
P1154New PKI 14-22 amide,myristoylated PKI 14-22 amide, myristoylated is a potent cAMP-dependent PKA inhibitor, which can reduce the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
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
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 Cell, 2022, S1535-6108(22)00312-9
Am J Cancer Res, 2022, 12(4):1535-1555
Cell Death Discov, 2022, 8(1):197
S1421 Staurosporine (AM-2282) Staurosporine (AM-2282, Antibiotic AM-2282, 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, 2022, 13(1):3775
EMBO Mol Med, 2022, 14(3):e15295
Cancer Res, 2022, canres.0218.2021
S1573 Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877), 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.
Aging Cell, 2022, e13587
Cell Death Dis, 2022, 13(2):138
iScience, 2022, 25(6):104398
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.
Signal Transduct Target Ther, 2022, 7(1):46
Nat Commun, 2022, 13(1):3419
Nat Commun, 2022, 13(1):2256
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
S2670 A-674563 A-674563 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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Nat Commun, 2022, 13(1):668
Cancers (Basel), 2022, 14(6)1575
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.
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.
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.
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
Sci Rep, 2021, 11(1):18532
Cell, 2020, 182(3):685-712.e19
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.
Nat Commun, 2022, 13(1):1768
J Biol Chem, 2022, S0021-9258(22)00494-X
Oxid Med Cell Longev, 2021, 2021:6620873
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.
Cell Res, 2022, 10.1038/s41422-022-00668-0
Signal Transduct Target Ther, 2022, 7(1):46
Evid Based Complement Alternat Med, 2022, 2022:3311250
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.
Autophagy, 2022, 1-14
Nucleic Acids Res, 2022, 50(5):2700-2718
Nat Commun, 2021, 12(1):4050
E2506New 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.
P1155New CREBtide CREBtide, a synthetic 13 amino acid peptide, has been reported as a PKA substrate.
P1156New Malantide Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase, which is a highly specific substrate for PKA with a Km of 15 μM.
P1154New PKI 14-22 amide,myristoylated PKI 14-22 amide, myristoylated is a potent cAMP-dependent PKA inhibitor, which can reduce the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
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
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 Cell, 2022, S1535-6108(22)00312-9
Am J Cancer Res, 2022, 12(4):1535-1555
Cell Death Discov, 2022, 8(1):197
S1421 Staurosporine (AM-2282) Staurosporine (AM-2282, Antibiotic AM-2282, 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, 2022, 13(1):3775
EMBO Mol Med, 2022, 14(3):e15295
Cancer Res, 2022, canres.0218.2021
S1573 Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877), 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.
Aging Cell, 2022, e13587
Cell Death Dis, 2022, 13(2):138
iScience, 2022, 25(6):104398
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.
Signal Transduct Target Ther, 2022, 7(1):46
Nat Commun, 2022, 13(1):3419
Nat Commun, 2022, 13(1):2256
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
S2670 A-674563 A-674563 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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Nat Commun, 2022, 13(1):668
Cancers (Basel), 2022, 14(6)1575
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.
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.
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.
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
Sci Rep, 2021, 11(1):18532
Cell, 2020, 182(3):685-712.e19
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.
Nat Commun, 2022, 13(1):1768
J Biol Chem, 2022, S0021-9258(22)00494-X
Oxid Med Cell Longev, 2021, 2021:6620873
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.
Cell Res, 2022, 10.1038/s41422-022-00668-0
Signal Transduct Target Ther, 2022, 7(1):46
Evid Based Complement Alternat Med, 2022, 2022:3311250
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.
Autophagy, 2022, 1-14
Nucleic Acids Res, 2022, 50(5):2700-2718
Nat Commun, 2021, 12(1):4050
E2506New 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.
P1154New PKI 14-22 amide,myristoylated PKI 14-22 amide, myristoylated is a potent cAMP-dependent PKA inhibitor, which can reduce the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
E2506New 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.
P1155New CREBtide CREBtide, a synthetic 13 amino acid peptide, has been reported as a PKA substrate.
P1156New Malantide Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase, which is a highly specific substrate for PKA with a Km of 15 μM.
Tags: PKA inhibitor|PKA agonist|PKA activator|PKA inducer|PKA antagonist|PKA signaling pathway|PKA assay kit