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抑制剂选择性比较

AMPK产品

所有产品 AMPK抑制剂(4) AMPK激活剂(10) 新AMPK产品

产品目录	产品描述	文献引用	实验数据
S7306	Dorsomorphin (Compound C) 2HCl Dorsomorphin (Compound C) 2HCl是一种有效的，可逆的，选择性AMPK抑制剂，在无细胞试验中K_i为109 nM，对一些结构相关的激酶，包括ZAPK， SYK， PKCθ，PKA和JAK3没有显著的抑制作用。也会抑制I型BMP受体。	Mol Cell, 2019, 10.1016/j.molcel.2019.09.007 Mol Cell, 2019, 76(1):148-162 Mol Cell, 2019, 76(1):148-162	AMPK inhibition by compound C(Dorsomorphin) inhibited autophagy activation and neuroprotection induced by IPC in PC12 cells. (A) Compound C (Comp C) abolished IPC induced neuroprotection in PC12 cells. Cells were incubated with compound C 5 μM 60 min before the onset of IPC. Twelve hours after IPC, the cells were subjected to OGD for 10 h and cell viability was examined with CCK-8 kit. (B) Compound C reduced LC3II/LC3I ratio. The cells were incubated with compound C 5 μM 60 min before the onset of IPC. Then the cells were harvested 12 h after IPC and subjected to Western blot analysis. Bar represents mean ± SD, n = 3. P < 0.05, **P < 0.001 compared with the control group; $$$ P < 0.001 compared with the OGD group; %%% P < 0.001 compared with the IPC + OGD group; # P < 0.05 compared with the IPC group.
S7317	WZ4003 WZ4003是高特异性的NUAK kinase抑制剂，细胞试验中作用于NUAK1和NUAK2的IC50分别为20 nM和100 nM，对其他139个激酶没有显著抑制作用。	Nat Commun, 2018, 9(1):4826 Brain Behav Immun, 2018, 72:89-100 J Cell Mol Med, 2017, 10.1111/jcmm.13070	The AMPK inhibitor, WZ4003, and the p38 MAPK inhibitor, SB203580, could inhibit the APN-induced overexpression of CXCL1 and CXCL8 and h-JBMMSCs chemotaxis. After treated with WZ4003 and SB203580, the expression of CXCL1 (A and B) and CXCL8 (C and D) in the cells and supernatants of h-JBMMSCs treated with or without APN was evaluated by the ELISA assay (n = 3; P < 0.05; *P < 0.01)
S7318	HTH-01-015 HTH-01-015 是一种有效的选择性 NUAK1 抑制剂，其IC50 为100 nM，比作用于NUAK2的选择性高100多倍。	Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.10.005	Mouse BMDMs and human THP1 cells were treated with LPS (200 ng/ml) in the absence or presence of indicated AMPK activators (metformin, quercetin, resveratrol, AICAR, A-769662, and salicylate), AMPK inhibitors (compound C, WZ4003, and HTH-01-015), or HMGB1 inhibitor (glycyrrhizin) for 24 h. HMGB1 release in cell medium was assayed using ELISA kit, respectively (n = 3, *p < .05 versus LPS or Escherichia coli group).
S7840	Dorsomorphin (Compound C) Dorsomorphin (Compound C)是一种有效的，可逆选择性 AMPK 抑制剂，无细胞试验中 K_i 为 109 nM，对几个结构相关的激酶，包括ZAPK，SYK，PKCθ，PKA，和 JAK3没有显著的抑制作用。也会抑制 I型 BMP receptor 活性。	Neural Regen Res, 2020, 15(3):473-481 Nat Cell Biol, 2019, 21(3):397-407 Mol Cell, 2019, 10.1016/j.molcel.2019.09.007	FGF21 activates myogenic and aerobic myofiber-associated genes expression via AMPK pathway. The activator (acadesine) or inhibitor (dorsomorphin) of AMPK pathway were used to treat the pcDNA3.1-21 or control transfected C2C12 myoblasts. For this experiment, four groups were set up: FGF21-ACA (pcDNA3.1-21‡acadesine), Control-ACA (control‡acadesine), FGF21-DOR (pcDNA3.1-21‡dorsomorphin), and Control-DOR(control‡dorsomorphin). The qRT-PCR was performed to detect the genes expression of FGF21 (A), AMPK (B), Sirt 1, Myoglobin(C), Desmin (D), MEF2c (E), a-actin (F). (G) The C2C12 myoblasts were transiently transfected with pCDNA3.1-21 or pCDNA3.1, Western blot showed FGF21 activated AMPK signal via FGF21-Sirt1-AMPK. For the phosphorylated AMPK (right), the intensity of band was normalized total AMPK, and then normalized by control. (H and I) FGF21, as well as AMPK activator acadesine (ACA), increased phosphorylation of AMPM, and myogenic genes expression, especially MyHC I, which was activated by ACA (FGF21‡ACA) and suppressed by AMPK inhibitor DOR(FGF21‡DOR). The data are presented as mean±SD (P<0.05, *P<0.01, and P<0.001), n=ˆ3.
S2697	A-769662 A-769662是一种有效的，可逆的AMPK激活剂，在无细胞试验中EC50为0.8 μM，对GPPase/FBPase活性几乎没有作用。	cell, 2019, 178(5):1102-1114 Cell Metab, 2019, 30(3):508-524 Cell Metab, 2019, 29(6):1350-1362	Cells were treated with CP, DOXO, SRT1720 (100 nM), EX527 (100 nM), A769662 (10 μM) and Compound C (1 μM) under normoxic or hypoxic conditions for 48 hours, and then their viabilities were measured by MTT.
S1802	AICAR (Acadesine) AICAR (Acadesine)是AMPK的激活剂，引起ZMP积累，模拟AMP对AMPK和AMPKK的刺激作用。Phase 3。	Cell Rep, 2019, 27(12):3413-3421 Br J Pharmacol, 2019, 176(20):3983-4001 Antioxid Redox Signal, 2019, 30(2):163-183	Cultured hepatocytes were treated with 10 μM Compound C (Comp.C) for 30 min before treatment with 10 μM SAL, 1 mM AICAR for 3 h. Cell lysates were immunoblotted for the phosphorylation of AMPK, ACC, Akt and GSK3β. P < 0.05, *P < 0.01 versus control; ##P < 0.01 versus SAL alone; †P < 0.05, ††P < 0.01 versus AICAR alone. Values are means ± SEM (n = 4).
S2542	Phenformin HCl Phenformin HCl是一种Phenformin的盐酸盐，是一种双胍类的抗糖尿病药。它能激活AMPK，提高其活性和磷酸化。	cell, 2019, 178(5):1102-1114 Nat Commun, 2019, 10(1):3856 J Biol Chem, 2017, 292(7):2830-2841	a set of RNAi-resistant rescue forms of Cdc37 plasmids were transfected into stable Cdc37-RNAi HCT116 cells. 24 h after transfection cells were treated with phenformin and then subjected to FLAG immunoprecipitation.
S8803^New	MK-3903 MK-3903是一种有效的选择性AMPK激活剂，对α1 β1 γ1亚基的EC50值为8 nM。它能激活12种pAMPK复合体中的10种，EC50值在8-40 nM。
S5284	Adenosine 5'-monophosphate monohydrate Adenosine 5'-monophosphate monohydrate (5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK).
S8335	PF-06409577 PF-06409577是具有口服活性的AMPK激活剂，在TR-FRET实验中，对AMPK α1β1γ1的EC50为7 nM。在patchBclamp实验中，100μM的PF-06409577对hERG没有可观测到的抑制作用，对主要的人源细胞色素P450亚型的微粒体活性也没有抑制活性（IC50 > 100 μM）。
S7898	GSK621 GSK621是一种特异性且有效的AMPK激活剂。	Nat Commun, 2019, 10(1-:2987 Cell Rep, 2019, 26(13):3613-3628 EBioMedicine, 2019, 40:92-105	GSK621 dose-dependent activation of AMPK in erythroblasts. Western Blot analysis of PT172 AMPKα1, PS79 ACC and PS555 ULK1 in primary erythroblasts incubated for 3 h with increasing doses of GSK621. Anti-HSC70 was used as a loading control.
S8654	ex229 (compound 991) EX229 (compound 991)是一种有效的AMPK激活剂，其效力是A769662的5-10倍。
S9096	ligustroflavone Ligustroflavone, isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator.
S7953	ETC-1002 ETC-1002是一种可用于口服、降低LDL-C的小分子，是肝脏AMPK的激活剂。

产品目录	产品描述	文献引用	实验数据
S7306	Dorsomorphin (Compound C) 2HCl Dorsomorphin (Compound C) 2HCl是一种有效的，可逆的，选择性AMPK抑制剂，在无细胞试验中K_i为109 nM，对一些结构相关的激酶，包括ZAPK， SYK， PKCθ，PKA和JAK3没有显著的抑制作用。也会抑制I型BMP受体。	Mol Cell,2019, 10.1016/j.molcel.2019.09.007 Mol Cell,2019, 76(1):148-162 Mol Cell,2019, 76(1):148-162	AMPK inhibition by compound C(Dorsomorphin) inhibited autophagy activation and neuroprotection induced by IPC in PC12 cells. (A) Compound C (Comp C) abolished IPC induced neuroprotection in PC12 cells. Cells were incubated with compound C 5 μM 60 min before the onset of IPC. Twelve hours after IPC, the cells were subjected to OGD for 10 h and cell viability was examined with CCK-8 kit. (B) Compound C reduced LC3II/LC3I ratio. The cells were incubated with compound C 5 μM 60 min before the onset of IPC. Then the cells were harvested 12 h after IPC and subjected to Western blot analysis. Bar represents mean ± SD, n = 3. P < 0.05, **P < 0.001 compared with the control group; $$$ P < 0.001 compared with the OGD group; %%% P < 0.001 compared with the IPC + OGD group; # P < 0.05 compared with the IPC group.
S7317	WZ4003 WZ4003是高特异性的NUAK kinase抑制剂，细胞试验中作用于NUAK1和NUAK2的IC50分别为20 nM和100 nM，对其他139个激酶没有显著抑制作用。	Nat Commun,2018, 9(1):4826 Brain Behav Immun,2018, 72:89-100 J Cell Mol Med,2017, 10.1111/jcmm.13070	The AMPK inhibitor, WZ4003, and the p38 MAPK inhibitor, SB203580, could inhibit the APN-induced overexpression of CXCL1 and CXCL8 and h-JBMMSCs chemotaxis. After treated with WZ4003 and SB203580, the expression of CXCL1 (A and B) and CXCL8 (C and D) in the cells and supernatants of h-JBMMSCs treated with or without APN was evaluated by the ELISA assay (n = 3; P < 0.05; *P < 0.01)
S7318	HTH-01-015 HTH-01-015 是一种有效的选择性 NUAK1 抑制剂，其IC50 为100 nM，比作用于NUAK2的选择性高100多倍。	Cell Chem Biol,2019, 10.1016/j.chembiol.2019.10.005	Mouse BMDMs and human THP1 cells were treated with LPS (200 ng/ml) in the absence or presence of indicated AMPK activators (metformin, quercetin, resveratrol, AICAR, A-769662, and salicylate), AMPK inhibitors (compound C, WZ4003, and HTH-01-015), or HMGB1 inhibitor (glycyrrhizin) for 24 h. HMGB1 release in cell medium was assayed using ELISA kit, respectively (n = 3, *p < .05 versus LPS or Escherichia coli group).
S7840	Dorsomorphin (Compound C) Dorsomorphin (Compound C)是一种有效的，可逆选择性 AMPK 抑制剂，无细胞试验中 K_i 为 109 nM，对几个结构相关的激酶，包括ZAPK，SYK，PKCθ，PKA，和 JAK3没有显著的抑制作用。也会抑制 I型 BMP receptor 活性。	Neural Regen Res,2020, 15(3):473-481 Nat Cell Biol,2019, 21(3):397-407 Mol Cell,2019, 10.1016/j.molcel.2019.09.007	FGF21 activates myogenic and aerobic myofiber-associated genes expression via AMPK pathway. The activator (acadesine) or inhibitor (dorsomorphin) of AMPK pathway were used to treat the pcDNA3.1-21 or control transfected C2C12 myoblasts. For this experiment, four groups were set up: FGF21-ACA (pcDNA3.1-21‡acadesine), Control-ACA (control‡acadesine), FGF21-DOR (pcDNA3.1-21‡dorsomorphin), and Control-DOR(control‡dorsomorphin). The qRT-PCR was performed to detect the genes expression of FGF21 (A), AMPK (B), Sirt 1, Myoglobin(C), Desmin (D), MEF2c (E), a-actin (F). (G) The C2C12 myoblasts were transiently transfected with pCDNA3.1-21 or pCDNA3.1, Western blot showed FGF21 activated AMPK signal via FGF21-Sirt1-AMPK. For the phosphorylated AMPK (right), the intensity of band was normalized total AMPK, and then normalized by control. (H and I) FGF21, as well as AMPK activator acadesine (ACA), increased phosphorylation of AMPM, and myogenic genes expression, especially MyHC I, which was activated by ACA (FGF21‡ACA) and suppressed by AMPK inhibitor DOR(FGF21‡DOR). The data are presented as mean±SD (P<0.05, *P<0.01, and P<0.001), n=ˆ3.

产品目录	产品描述	文献引用	实验数据
S2697	A-769662 A-769662是一种有效的，可逆的AMPK激活剂，在无细胞试验中EC50为0.8 μM，对GPPase/FBPase活性几乎没有作用。	cell, 2019, 178(5):1102-1114 Cell Metab, 2019, 30(3):508-524 Cell Metab, 2019, 29(6):1350-1362	Cells were treated with CP, DOXO, SRT1720 (100 nM), EX527 (100 nM), A769662 (10 μM) and Compound C (1 μM) under normoxic or hypoxic conditions for 48 hours, and then their viabilities were measured by MTT.
S1802	AICAR (Acadesine) AICAR (Acadesine)是AMPK的激活剂，引起ZMP积累，模拟AMP对AMPK和AMPKK的刺激作用。Phase 3。	Cell Rep, 2019, 27(12):3413-3421 Br J Pharmacol, 2019, 176(20):3983-4001 Antioxid Redox Signal, 2019, 30(2):163-183	Cultured hepatocytes were treated with 10 μM Compound C (Comp.C) for 30 min before treatment with 10 μM SAL, 1 mM AICAR for 3 h. Cell lysates were immunoblotted for the phosphorylation of AMPK, ACC, Akt and GSK3β. P < 0.05, *P < 0.01 versus control; ##P < 0.01 versus SAL alone; †P < 0.05, ††P < 0.01 versus AICAR alone. Values are means ± SEM (n = 4).
S2542	Phenformin HCl Phenformin HCl是一种Phenformin的盐酸盐，是一种双胍类的抗糖尿病药。它能激活AMPK，提高其活性和磷酸化。	cell, 2019, 178(5):1102-1114 Nat Commun, 2019, 10(1):3856 J Biol Chem, 2017, 292(7):2830-2841	a set of RNAi-resistant rescue forms of Cdc37 plasmids were transfected into stable Cdc37-RNAi HCT116 cells. 24 h after transfection cells were treated with phenformin and then subjected to FLAG immunoprecipitation.
S8803^New	MK-3903 MK-3903是一种有效的选择性AMPK激活剂，对α1 β1 γ1亚基的EC50值为8 nM。它能激活12种pAMPK复合体中的10种，EC50值在8-40 nM。
S5284	Adenosine 5'-monophosphate monohydrate Adenosine 5'-monophosphate monohydrate (5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK).
S8335	PF-06409577 PF-06409577是具有口服活性的AMPK激活剂，在TR-FRET实验中，对AMPK α1β1γ1的EC50为7 nM。在patchBclamp实验中，100μM的PF-06409577对hERG没有可观测到的抑制作用，对主要的人源细胞色素P450亚型的微粒体活性也没有抑制活性（IC50 > 100 μM）。
S7898	GSK621 GSK621是一种特异性且有效的AMPK激活剂。	Nat Commun, 2019, 10(1-:2987 Cell Rep, 2019, 26(13):3613-3628 EBioMedicine, 2019, 40:92-105	GSK621 dose-dependent activation of AMPK in erythroblasts. Western Blot analysis of PT172 AMPKα1, PS79 ACC and PS555 ULK1 in primary erythroblasts incubated for 3 h with increasing doses of GSK621. Anti-HSC70 was used as a loading control.
S8654	ex229 (compound 991) EX229 (compound 991)是一种有效的AMPK激活剂，其效力是A769662的5-10倍。
S9096	ligustroflavone Ligustroflavone, isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator.
S7953	ETC-1002 ETC-1002是一种可用于口服、降低LDL-C的小分子，是肝脏AMPK的激活剂。

Tags: AMPK inhibition | AMPK activation | AMPK phosphorylation | AMPK activity | AMP-activated protein kinase pathway | AMPK activity assay | AMPK activators review | AMPK activity assay | AMPK inhibitor cancer | AMPK agonists | AMPK antagonist | AMPK inhibitor review