PKA

PKA製品

• All (14)
• PKA阻害剤 (11)
• PKA活性剤(2)
• PKA拮抗剤(1)
• 新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.	J Extracell Vesicles, 2024, 13(4):e12426 J Extracell Vesicles, 2024, 13(4):e12426 Adv Sci (Weinh), 2024, 11(4):e2304987
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。	Nat Commun, 2024, 15(1):489 Nat Commun, 2024, 15(1):3816 Nat Commun, 2024, 15(1):3816
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9 CNS Neurosci Ther, 2024, 30(8):e14913
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.	Sci China Life Sci, 2024, 67(8):1549-1562 Ren Fail, 2024, 46(2):2396455 PeerJ, 2023, 11:e15494
S7858	Dibutyryl-cAMP (Bucladesine)	Dibutyryl-cAMP (Bucladesine, dbcAMP,Dibutyryl cAMP sodium salt) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.	Cell Rep Med, 2024, 5(3):101477 J Ethnopharmacol, 2024, 324:117829 Invest Ophthalmol Vis Sci, 2024, 65(3):37
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.	Biomed Pharmacother, 2024, 176:116858 J Transl Med, 2024, 22(1):478 Front Physiol, 2024, 15:1304375
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 11.8 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.	J Extracell Vesicles, 2024, 13(4):e12426 J Extracell Vesicles, 2024, 13(4):e12426 Adv Sci (Weinh), 2024, 11(4):e2304987
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。	Nat Commun, 2024, 15(1):489 Nat Commun, 2024, 15(1):3816 Nat Commun, 2024, 15(1):3816
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9 CNS Neurosci Ther, 2024, 30(8):e14913
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.	Sci China Life Sci, 2024, 67(8):1549-1562 Ren Fail, 2024, 46(2):2396455 PeerJ, 2023, 11:e15494
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 11.8 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,Dibutyryl cAMP sodium salt) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.	Cell Rep Med, 2024, 5(3):101477 J Ethnopharmacol, 2024, 324:117829 Invest Ophthalmol Vis Sci, 2024, 65(3):37
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.	Biomed Pharmacother, 2024, 176:116858 J Transl Med, 2024, 22(1):478 Front Physiol, 2024, 15:1304375
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.