PKG
抑制剂选择性比较
PKG产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1573 |
Fasudil (HA-1077) HClFasudil(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。 |
![]() ![]() 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 2HClH 89 2HCl是一种有效的PKA抑制剂,无细胞试验中Ki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。 |
![]() ![]() 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 |
StaurosporineStaurosporine (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。 |
![]() ![]() |
|
S0378New |
MBP146-78MBP146-78 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。 |
||
S2964New |
HA-100 dihydrochlorideHA-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。 |
||
S0152New |
PKG drug G1PKG 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) HClFasudil(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。 |
![]() ![]() 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 2HClH 89 2HCl是一种有效的PKA抑制剂,无细胞试验中Ki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。 |
![]() ![]() 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 |
StaurosporineStaurosporine (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。 |
![]() ![]() |
|
S0378New |
MBP146-78MBP146-78 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。 |
||
S2964New |
HA-100 dihydrochlorideHA-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 |
---|---|---|---|
S0152New |
PKG drug G1PKG 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。 |