PKG

抑制剂选择性比较

PKG产品

所有产品 PKG抑制剂(5) PKG激活剂(1)

目录号	产品描述	文献引用	实验数据
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。	Nat Cell Biol, 2020, 25 Nat Commun, 2020, 11(1):71 Cell Rep, 2020, 30(11):3864-3874	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.
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 Cell Death Dis, 2020, 6;11(4):221	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。	EMBO J, 2020, 39(5):e102608 Genes Dev, 2020, 34(7-8):526-543 Cell Rep, 2020, 10;30(10):3411-3423 e7
S0378^New	MBP146-78 MBP146-78 是一种有效的、选择性的 cyclic GMP(cGMP)-dependent protein kinases/Protein Kinase G (PKG) 抑制剂，对弓形虫Toxoplasma gondii表现出细胞抑制活性。
S6861^New	KT5823 KT5823 is a selective inhibitor of cGMP-dependent protein kinase (PKG) with Ki of 0.23 μM. KT5823 also inhibits PKA and PKC with Ki of 10 μM and 4 μM, respectively.
S0152^New	PKG drug G1 PKG drug G1 is an inducer targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

目录号	产品描述	文献引用	实验数据
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。	Nat Cell Biol,2020, 25 Nat Commun,2020, 11(1):71 Cell Rep,2020, 30(11):3864-3874	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.
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 Cell Death Dis,2020, 6;11(4):221	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。	EMBO J,2020, 39(5):e102608 Genes Dev,2020, 34(7-8):526-543 Cell Rep,2020, 10;30(10):3411-3423 e7
S0378^New	MBP146-78 MBP146-78 是一种有效的、选择性的 cyclic GMP(cGMP)-dependent protein kinases/Protein Kinase G (PKG) 抑制剂，对弓形虫Toxoplasma gondii表现出细胞抑制活性。
S6861^New	KT5823 KT5823 is a selective inhibitor of cGMP-dependent protein kinase (PKG) with Ki of 0.23 μM. KT5823 also inhibits PKA and PKC with Ki of 10 μM and 4 μM, respectively.

目录号

产品描述

文献引用

实验数据

S0152^New

PKG drug G1

PKG drug G1 is an inducer targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.