PKA

PKA製品

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  • PKA阻害剤 (14)
  • PKA活性剤(3)
  • PKA拮抗剤(1)
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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.
Nat Commun, 2025, 16(1):7115
Cell Rep Med, 2025, 6(8):102254
Transl Neurodegener, 2025, 14(1):43
H89-2HCl-S158201W0520150921.gif
S1421 Staurosporine (STS) スタウロスポリン (Staurosporine (AM-2282、Antiviotic AM-2282、STS)) は、PKCα、PKCγ、および PKCη に対する強力な PKC 阻害剤であり、IC50 は 2 nM、5 nM、および 4 nM です。 無細胞アッセイでは、PKCδ (20 nM)、PKCε (73 nM) に対して効力が低く、PKCζ (1086 nM) に対してほとんど活性がありません。 また、PKA、PKG、S6K、CaMKII などの他のキナーゼに対しても阻害活性を示します。臨床フェーズ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
Staurosporine-S142101Y0220140126.gif
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
GSK690693-S1113W0120141117.gif
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
fasudil-S157301W0120140228.gif
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
A-674563-S267001Z0120121015.gif
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
8-Bromo-cAMP-S785701I0820161110.gif
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
ML-7-S838801W0220190428.gif
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
AT13148-S756301Z0120161118.gif
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
Daphnetin-S255401H0120180502.gif
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 11.8 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. A-674563 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 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.
Nat Commun, 2025, 16(1):7115
Cell Rep Med, 2025, 6(8):102254
Transl Neurodegener, 2025, 14(1):43
H89-2HCl-S158201W0520150921.gif
S1421 Staurosporine (STS) スタウロスポリン (Staurosporine (AM-2282、Antiviotic AM-2282、STS)) は、PKCα、PKCγ、および PKCη に対する強力な PKC 阻害剤であり、IC50 は 2 nM、5 nM、および 4 nM です。 無細胞アッセイでは、PKCδ (20 nM)、PKCε (73 nM) に対して効力が低く、PKCζ (1086 nM) に対してほとんど活性がありません。 また、PKA、PKG、S6K、CaMKII などの他のキナーゼに対しても阻害活性を示します。臨床フェーズ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
Staurosporine-S142101Y0220140126.gif
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
GSK690693-S1113W0120141117.gif
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
fasudil-S157301W0120140228.gif
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
A-674563-S267001Z0120121015.gif
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
ML-7-S838801W0220190428.gif
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
AT13148-S756301Z0120161118.gif
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
Daphnetin-S255401H0120180502.gif
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 11.8 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. A-674563 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
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
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
8-Bromo-cAMP-S785701I0820161110.gif
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.
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. A-674563 reduces Akt downstream target phosphorylation and inhibits tumor cell proliferation in vitro with an EC50 of 0.4 µM.