AMPK

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抑制剂选择性比较

AMPK产品

所有产品 AMPK抑制剂(6) AMPK激活剂(15)

目录号	产品描述	文献引用	实验数据
S1208	Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin) HCl是一种抗生素类试剂，可抑制DNA topoisomerase II，并在肿瘤细胞中诱导DNA损伤、线粒体自噬和凋亡。Doxorubicin 可降低 AMPK的基础磷酸化。Doxorubicin 可应用于HIV感染病人的联合治疗，但是在免疫治疗中有将HBV重活化的风险。	Nat Commun, 2020, 24;11(1):1972 PLoS Biol, 2020, 23;18(3):e3000666 Cancer Res, 2020, 10.1158/0008-5472.CAN-19-2069	Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05.
S1113	GSK690693 GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。	Cell, 2020, 25;181(7):1596-1611.e27. J Clin Invest, 2020, 1;130(5):2422-2434 Biomaterials, 2020, 239:119839	UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
S7306	Dorsomorphin (Compound C) 2HCl Dorsomorphin 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。Dorsomorphin 可诱导癌细胞系的自噬。	Cell Stem Cell, 2020, 2 pii: S1934-5909(20)30098-9 Cell Metab, 2020, 5;31(5):892-908 e11 PLoS Biol, 2020, 9;18(6):e3000288	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。	Mol Cell, 2020, 77(6):1322-1339 J Cell Biochem, 2019, 120(8):12989-13000 Evid Based Complement Alternat Med, 2019, 2019:3648685	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。	Mol Cell, 2020, 77(6):1322-1339 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 receptors ALK2，ALK3和ALK6 的活性。Dorsomorphin被应用于促进特定细胞分化和诱导癌细胞自噬。	Nat Commun, 2020, 11(1):382 PLoS Biol, 2020, 9;18(6):e3000288 Antioxid Redox Signal, 2020, 7	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.
S1033	Nilotinib (AMN-107) Nilotinib (AMN-107)是一种特异性BCR-ABL抑制剂，在小鼠骨髓祖细胞中IC50低于30 nM。Nilotinib (AMN-107)可通过激活AMPK来诱导自噬。	Blood, 2020, 8 pii: blood Mol Cell, 2020, 9 pii: S1097-2765(20)30189-1 Genome Med, 2020, 18;12(1):17	Effect of nilotinib on Bcr-Abl kinase activity in ABCB1- and ABCG2- overexpressing CD34⁺CD38^- cells. K562 parental cells and CD34⁺CD38^- subpopulation isolated from K562 cells were treated with nilotinib at 0.01, 0.1 and 1.0 umol/L for 12 h. Equal amount of protein was loaded for western blot analysis as described in the Experimental section. The experiments were repeated at least three times independently, and a representative experiment is shown.
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。	FASEB J, 2020, 34(3):4702-4717 J Lipid Res, 2020, 10.1194/jlr.RA119000542 Am J Physiol Cell Physiol, 2020, 1;318(5):C1018-C1029	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。AICAR (Acadesine)可诱导线粒体自噬。Phase 3。	Cell Death Dis, 2020, 8;11(6):427 Cell Microbiol, 2020, 22(2):e13131 Cell Biosci , 2020, 20;10:43	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).
S8953^New	ASP4132 ASP4132 是一种 Adenosine Monophosphate-Activated Protein Kinase (AMPK) 的有效口服活性激活剂，其对应的EC50值为0.018 μM。ASP4132 可用作治疗人类癌症的临床候选药物。
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.
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）。
S3832	Euphorbiasteroid Euphorbiasteroid是Euphorbia lathyris L.的成分之一，通过激活AMPK信号通路抑制3T3-L1细胞的脂肪形成，并通过促进Bcl-2/Bax信号通路诱导HL-60细胞凋亡。
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。	Cell Rep, 2019, 29(10):3331-3348
S8803	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。
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。	J Cell Mol Med, 2020, 25
S4561	Danthron Danthron通过激活 AMPK 来调节葡萄糖和脂质代谢。Danthron是从传统中药大黄中提取的天然产物。Danthron曾经是一种泻药，现在被用作合成润滑剂中的抗氧化剂，实验抗肿瘤剂的合成，杀真菌剂和制造染料的中间体。
S6221	Methyl cinnamate Methyl cinnamate 是花椒(Zanthoxylum armatum)的活性成分，是一种广泛使用的具有抗菌和 tyrosinase 抑制剂活性的天然香料化合物。Methyl cinnamate 通过激活3T3-L1前脂肪细胞中的 CaMKK2--AMPK 信号通路来抑制脂肪细胞分化。

目录号	产品描述	文献引用	实验数据
S1208	Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin) HCl是一种抗生素类试剂，可抑制DNA topoisomerase II，并在肿瘤细胞中诱导DNA损伤、线粒体自噬和凋亡。Doxorubicin 可降低 AMPK的基础磷酸化。Doxorubicin 可应用于HIV感染病人的联合治疗，但是在免疫治疗中有将HBV重活化的风险。	Nat Commun,2020, 24;11(1):1972 PLoS Biol,2020, 23;18(3):e3000666 Cancer Res,2020, 10.1158/0008-5472.CAN-19-2069	Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05.
S1113	GSK690693 GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。	Cell,2020, 25;181(7):1596-1611.e27. J Clin Invest,2020, 1;130(5):2422-2434 Biomaterials,2020, 239:119839	UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
S7306	Dorsomorphin (Compound C) 2HCl Dorsomorphin 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。Dorsomorphin 可诱导癌细胞系的自噬。	Cell Stem Cell,2020, 2 pii: S1934-5909(20)30098-9 Cell Metab,2020, 5;31(5):892-908 e11 PLoS Biol,2020, 9;18(6):e3000288	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。	Mol Cell,2020, 77(6):1322-1339 J Cell Biochem,2019, 120(8):12989-13000 Evid Based Complement Alternat Med,2019, 2019:3648685	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。	Mol Cell,2020, 77(6):1322-1339 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 receptors ALK2，ALK3和ALK6 的活性。Dorsomorphin被应用于促进特定细胞分化和诱导癌细胞自噬。	Nat Commun,2020, 11(1):382 PLoS Biol,2020, 9;18(6):e3000288 Antioxid Redox Signal,2020, 7	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.

目录号	产品描述	文献引用	实验数据
S1033	Nilotinib (AMN-107) Nilotinib (AMN-107)是一种特异性BCR-ABL抑制剂，在小鼠骨髓祖细胞中IC50低于30 nM。Nilotinib (AMN-107)可通过激活AMPK来诱导自噬。	Blood, 2020, 8 pii: blood Mol Cell, 2020, 9 pii: S1097-2765(20)30189-1 Genome Med, 2020, 18;12(1):17	Effect of nilotinib on Bcr-Abl kinase activity in ABCB1- and ABCG2- overexpressing CD34⁺CD38^- cells. K562 parental cells and CD34⁺CD38^- subpopulation isolated from K562 cells were treated with nilotinib at 0.01, 0.1 and 1.0 umol/L for 12 h. Equal amount of protein was loaded for western blot analysis as described in the Experimental section. The experiments were repeated at least three times independently, and a representative experiment is shown.
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。	FASEB J, 2020, 34(3):4702-4717 J Lipid Res, 2020, 10.1194/jlr.RA119000542 Am J Physiol Cell Physiol, 2020, 1;318(5):C1018-C1029	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。AICAR (Acadesine)可诱导线粒体自噬。Phase 3。	Cell Death Dis, 2020, 8;11(6):427 Cell Microbiol, 2020, 22(2):e13131 Cell Biosci , 2020, 20;10:43	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).
S8953^New	ASP4132 ASP4132 是一种 Adenosine Monophosphate-Activated Protein Kinase (AMPK) 的有效口服活性激活剂，其对应的EC50值为0.018 μM。ASP4132 可用作治疗人类癌症的临床候选药物。
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.
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）。
S3832	Euphorbiasteroid Euphorbiasteroid是Euphorbia lathyris L.的成分之一，通过激活AMPK信号通路抑制3T3-L1细胞的脂肪形成，并通过促进Bcl-2/Bax信号通路诱导HL-60细胞凋亡。
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。	Cell Rep, 2019, 29(10):3331-3348
S8803	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。
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。	J Cell Mol Med, 2020, 25
S4561	Danthron Danthron通过激活 AMPK 来调节葡萄糖和脂质代谢。Danthron是从传统中药大黄中提取的天然产物。Danthron曾经是一种泻药，现在被用作合成润滑剂中的抗氧化剂，实验抗肿瘤剂的合成，杀真菌剂和制造染料的中间体。
S6221	Methyl cinnamate Methyl cinnamate 是花椒(Zanthoxylum armatum)的活性成分，是一种广泛使用的具有抗菌和 tyrosinase 抑制剂活性的天然香料化合物。Methyl cinnamate 通过激活3T3-L1前脂肪细胞中的 CaMKK2--AMPK 信号通路来抑制脂肪细胞分化。

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AMPK

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研究领域

抑制剂选择性比较

AMPK产品