PKA

抑制剂选择性比较

PKA产品

所有产品(11) PKA抑制剂(9) PKA激活剂(2)

目录号	产品描述	文献引用	实验数据
S1113	GSK690693 GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。	Cell, 2020, 25;181(7):1596-1611.e27. J Clin Invest, 2020, 1;130(5):2422-2434 Biomaterials, 2020, 239:119839	UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
S1573	Fasudil (HA-1077) HCl Fasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。	Proc Natl Acad Sci U S A, 2021, 118(2)e2016034118 Nat Cell Biol, 2020, 25 Nat Commun, 2020, 11(1):71	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S2670	A-674563 A-674563是一种Akt抑制剂，在无细胞试验中K_i为11 nM，对PKA适度有效，作用于Akt1比作用于PKC选择性高30多倍。	Sci Signal, 2020, 13(619) Cancers (Basel), 2020, 12(9)E2668 Biomolecules, 2020, 10(2)	B cells were pre-treated with the indicated concentrations of A-674563 for 1h prior to R848 treatment (500 ng/ml). Thymidine incorporation was analyzed 24h later.
S1582	H 89 2HCl H 89 2HCl是一种有效的PKA抑制剂，无细胞试验中K_i为48 nM，作用于PKA比作用于PKG选择性高10倍，比作用于PKC，MLCK，钙调蛋白激酶II和酪蛋白激I/II选择性高500倍。H 89 2HCl可诱导自噬。	Autophagy, 2020, 16(6):1061-1076 EMBO Mol Med, 2020, 12(4):e11177 Oncogene, 2020, 10.1038/s41388-020-01453-2	The effects of H89 on bTSH-induced FASN downregulation in 3T3-L1 adipocytes. Differentiated 3T3-L1 adipocytes were pretreated with either 20 µmol/L H89 or vehicle for 1 h, then treated with 0.2 µM bTSH for 8 h. Levels of FASN, pCREB, pERK1/2 and pJNK were determined by Western blotting.
S1421	Staurosporine Staurosporine (CGP 41251) 是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。	Eur J Med Chem, 2021, 211:113003 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
S2964^New	HA-100 dihydrochloride HA-100 dihydrochloride 是 cGMP-dependent protein kinase (PKG)、cAMP-dependent protein kinase (PKA)、protein kinase C (PKC) 和 MLC-kinase 的抑制剂，对应的IC50值分别为4 μM、8 μM、12 μM和240 μM。
S2554	Daphnetin Daphnetin是天然香豆素衍生物，是一种蛋白激酶抑制剂，抑制EGFR， PKA和PKC，IC50分别为7.67 μM， 9.33 μM和25.01 μM，且具有抗炎和抗氧化剂活动性。	Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7 Int Immunopharmacol, 2019, 72:195-203 Inflamm Res, 2017, 66(7):579-589	C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
S8388	ML-7 HCl ML-7 是平滑肌肌球蛋白轻链激酶MLCK抑制剂，Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。ML-7 还可抑制 PKA 和 PKC，对应的Ki值分别为21 μM和42 μM。	J Cell Sci, 2021, 134(1)jcs244616 Cancer Lett, 2020, 28;483:75-86 Stem Cells, 2020, 11	Platelets (3 × 10⁸/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
S7563	AT13148 AT13148是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。Phase 1。	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Cancer Cell, 2020, 37(1):85-103	AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
S7857	8-Bromo-cAMP 8-Bromo-cAMP是一种细胞渗透性环AMP(cAMP)类似物，激活cAMP依赖的蛋白激酶的Ka值为0.05 μM。是一种PKA激活剂。	FASEB J, 2020, 10.1096/fj.202001561R Aging (Albany NY), 2020, 7;12(9):8120-8136 J Cell Mol Med, 2020, 10.1111/jcmm.16029	(E) 8-Bromo-cAMP treatment could not restore the T cell defects in rpc9-/- mutants.
S7858	Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP)是一种细胞可渗透性 PKA 激活剂，通过模拟内源性 cAMP 发挥作用。Dibutyryl-cAMP (Bucladesine)也是一种 phosphodiesterase (PDE) 抑制剂。	EMBO Mol Med, 2021, e12632 Neurogastroenterol Motil, 2020, 11;e13877 EBioMedicine, 2019, 44:563-573

目录号	产品描述	文献引用	实验数据
S1113	GSK690693 GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。	Cell,2020, 25;181(7):1596-1611.e27. J Clin Invest,2020, 1;130(5):2422-2434 Biomaterials,2020, 239:119839	UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
S1573	Fasudil (HA-1077) HCl Fasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。	Proc Natl Acad Sci U S A,2021, 118(2)e2016034118 Nat Cell Biol,2020, 25 Nat Commun,2020, 11(1):71	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S2670	A-674563 A-674563是一种Akt抑制剂，在无细胞试验中K_i为11 nM，对PKA适度有效，作用于Akt1比作用于PKC选择性高30多倍。	Sci Signal,2020, 13(619) Cancers (Basel),2020, 12(9)E2668 Biomolecules,2020, 10(2)	B cells were pre-treated with the indicated concentrations of A-674563 for 1h prior to R848 treatment (500 ng/ml). Thymidine incorporation was analyzed 24h later.
S1582	H 89 2HCl H 89 2HCl是一种有效的PKA抑制剂，无细胞试验中K_i为48 nM，作用于PKA比作用于PKG选择性高10倍，比作用于PKC，MLCK，钙调蛋白激酶II和酪蛋白激I/II选择性高500倍。H 89 2HCl可诱导自噬。	Autophagy,2020, 16(6):1061-1076 EMBO Mol Med,2020, 12(4):e11177 Oncogene,2020, 10.1038/s41388-020-01453-2	The effects of H89 on bTSH-induced FASN downregulation in 3T3-L1 adipocytes. Differentiated 3T3-L1 adipocytes were pretreated with either 20 µmol/L H89 or vehicle for 1 h, then treated with 0.2 µM bTSH for 8 h. Levels of FASN, pCREB, pERK1/2 and pJNK were determined by Western blotting.
S1421	Staurosporine Staurosporine (CGP 41251) 是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。	Eur J Med Chem,2021, 211:113003 Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19
S2964^New	HA-100 dihydrochloride HA-100 dihydrochloride 是 cGMP-dependent protein kinase (PKG)、cAMP-dependent protein kinase (PKA)、protein kinase C (PKC) 和 MLC-kinase 的抑制剂，对应的IC50值分别为4 μM、8 μM、12 μM和240 μM。
S2554	Daphnetin Daphnetin是天然香豆素衍生物，是一种蛋白激酶抑制剂，抑制EGFR， PKA和PKC，IC50分别为7.67 μM， 9.33 μM和25.01 μM，且具有抗炎和抗氧化剂活动性。	Acta Neuropathol,2020, 10.1007/s00401-020-02226-7 Int Immunopharmacol,2019, 72:195-203 Inflamm Res,2017, 66(7):579-589	C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
S8388	ML-7 HCl ML-7 是平滑肌肌球蛋白轻链激酶MLCK抑制剂，Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。ML-7 还可抑制 PKA 和 PKC，对应的Ki值分别为21 μM和42 μM。	J Cell Sci,2021, 134(1)jcs244616 Cancer Lett,2020, 28;483:75-86 Stem Cells,2020, 11	Platelets (3 × 10⁸/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
S7563	AT13148 AT13148是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。Phase 1。	Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19 Cancer Cell,2020, 37(1):85-103	AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.

目录号

产品描述

文献引用

实验数据

S7857

8-Bromo-cAMP

8-Bromo-cAMP是一种细胞渗透性环AMP(cAMP)类似物，激活cAMP依赖的蛋白激酶的Ka值为0.05 μM。是一种PKA激活剂。

FASEB J, 2020, 10.1096/fj.202001561R

Aging (Albany NY), 2020, 7;12(9):8120-8136

J Cell Mol Med, 2020, 10.1111/jcmm.16029

S7858

Dibutyryl-cAMP (Bucladesine)

Dibutyryl-cAMP (Bucladesine, dbcAMP)是一种细胞可渗透性 PKA 激活剂，通过模拟内源性 cAMP 发挥作用。Dibutyryl-cAMP (Bucladesine)也是一种 phosphodiesterase (PDE) 抑制剂。

EMBO Mol Med, 2021, e12632

Neurogastroenterol Motil, 2020, 11;e13877

EBioMedicine, 2019, 44:563-573