PKA

抑制剂选择性比较

PKA产品

所有产品 PKA抑制剂(4) PKA激活剂(2)

产品目录	产品描述	文献引用	实验数据
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。	J Immunother Cancer, 2019, 7(1):33 Cell Death Dis, 2019, 9(10):1013 Front Physiol, 2019, 10:412	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。	Nat Cell Biol, 2019, 21(6):778-790 Proc Natl Acad Sci U S A, 2019, 116(27):13374-13383 J Clin Endocrinol Metab, 2019, 104(5):1697-1711	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.
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。	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.
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。	Nat Cell Biol, 2019, 21(6):778-790 Cancer Sci, 2016, 107(11):1563-1571 Biochem Biophys Res Commun, 2016, 478(1):330-6	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。	EBioMedicine, 2019, 39:540-551 J Cell Mol Med, 2018, 22(11):5518-5532 Development, 2016, 143(12):2103-10	(E) 8-Bromo-cAMP treatment could not restore the T cell defects in rpc9-/- mutants.
S7858	Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine)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。	EBioMedicine, 2019, 44:563-573 J Clin Endocrinol Metab, 2019, 104(5):1697-1711 Theranostics, 2017, 7(6):1447-1462

产品目录	产品描述	文献引用	实验数据
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。	J Immunother Cancer,2019, 7(1):33 Cell Death Dis,2019, 9(10):1013 Front Physiol,2019, 10:412	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。	Nat Cell Biol,2019, 21(6):778-790 Proc Natl Acad Sci U S A,2019, 116(27):13374-13383 J Clin Endocrinol Metab,2019, 104(5):1697-1711	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.
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。	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.
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。	Nat Cell Biol,2019, 21(6):778-790 Cancer Sci,2016, 107(11):1563-1571 Biochem Biophys Res Commun,2016, 478(1):330-6	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.

产品目录

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。

EBioMedicine, 2019, 39:540-551

J Cell Mol Med, 2018, 22(11):5518-5532

Development, 2016, 143(12):2103-10

S7858

Dibutyryl-cAMP (Bucladesine)

Dibutyryl-cAMP (Bucladesine)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。

EBioMedicine, 2019, 44:563-573

J Clin Endocrinol Metab, 2019, 104(5):1697-1711

Theranostics, 2017, 7(6):1447-1462