PKG

抑制剂选择性比较

PKG产品

所有产品(6) 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, AT-877)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 Cell Regen, 2021, 10(1):8 Int J Neurosci, 2021, 1-7	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。	Theranostics, 2021, 11(10):4975-4991 Front Aging Neurosci, 2021, 13:660249 FEBS J, 2021, 10.1111/febs.15763	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 (AM-2282) Staurosporine (AM-2282, Antibiotic AM-2282, STS)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 STAR Protoc, 2021, 2(2):100391 J Immunother Cancer, 2021, 9(2)e001906
S0378	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。
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。
S0152	PKG drug G1 PKG drug G1 是靶向C42的 Protein Kinase G Iα (PKG Iα) 的激活剂，可导致血管舒张和血压下降。

目录号	产品描述	文献引用	实验数据
S1573	Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877)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 Cell Regen,2021, 10(1):8 Int J Neurosci,2021, 1-7	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。	Theranostics,2021, 11(10):4975-4991 Front Aging Neurosci,2021, 13:660249 FEBS J,2021, 10.1111/febs.15763	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 (AM-2282) Staurosporine (AM-2282, Antibiotic AM-2282, STS)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 STAR Protoc,2021, 2(2):100391 J Immunother Cancer,2021, 9(2)e001906
S0378	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。
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。

目录号

产品描述

文献引用

实验数据

S0152

PKG drug G1

PKG drug G1 是靶向C42的 Protein Kinase G Iα (PKG Iα) 的激活剂，可导致血管舒张和血压下降。