AMPK
AMPK产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) 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。 |
![]() ![]() 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. |
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S1113 |
GSK690693GSK690693 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。 |
![]() ![]() 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. |
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E0022New |
Ophiopogonin DOphiopogonin D (OJV-VI, Deacetylophiopogonin C) 是一种从中草药麦冬中分离得到的甾体糖苷,具有抗肿瘤作用。Ophiopogonin D 可通过调节 ITGB1/FAK/Src/AKT/β-catenin/MMP-9 信号轴抑制TGF-β1介导的MDA-MB-231细胞转移行为。Ophiopogonin D 还通过抑制小鼠肺上皮细胞中的 AMPK/NF-κB 通路来减轻 PM2.5 诱导的炎症。 |
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S7306 |
Dorsomorphin (Compound C) 2HClDorsomorphin 2HCl (BML-275, Compound C) 是一种有效的,可逆的,选择性AMPK抑制剂,在无细胞试验中Ki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。 |
![]() ![]() 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. |
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S7317 |
WZ4003WZ4003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。 |
![]() ![]() 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) |
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S7318 |
HTH-01-015HTH-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。 |
![]() ![]() 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).
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S8274 |
STO-609STO-609 是特异性的CaM-KK的抑制剂,抑制CaM-KKα和CaM-KKβ的活性,Ki值分别为80 ng/ml和15 ng/ml,并抑制其自身磷酸化活性。STO-609 可抑制 AMPKK 活性并抑制自噬。 |
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S8161 |
ON123300ON123300是有效的多靶点激酶抑制剂,对CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。 |
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S0177 |
XMD-17-51XMD-17-51 (XMD17-51)是一种有效的具有高度选择性的 NUAK1 的抑制剂。 |
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S7840 |
Dorsomorphin (Compound C)Dorsomorphin (Compound C, BML-275)是一种有效的,可逆选择性 AMPK 抑制剂,无细胞试验中 Ki 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。如需进行动物实验,建议选择可水溶产品 S7306 Dorsomorphin (Compound C) 2HCl。 |
![]() ![]() 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. |
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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。 |
![]() ![]() 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. |
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S2697 |
A-769662A-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。 |
![]() ![]() 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. |
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S1802 |
AICAR (Acadesine)AICAR (Acadesine, NSC105823, AICA Riboside)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。 |
![]() ![]() 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). |
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E0653New |
Trans-ferulic acidTrans-ferulic acid是高糖条件下AMPK的强效激活剂。 |
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E0204New |
Poricoic acid APoricoic acid A 是从茯苓的表层中分离出来的 Poricic acid A 激活 AMPK 以减弱肾纤维化中的成纤维细胞活化和异常细胞外基质重塑。Poricic acid A 也是色氨酸羟化酶-1 (tryptophan hydroxylase-1, TPH-1) 的调节剂。 |
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E1031New |
MK-8722MK-8722 是一种有效的、直接的、所有 12 种哺乳动物 泛AMPK 复合物的变构激活剂。 |
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S9860New |
BC1618BC1618 是一种口服活性的 Fbxo48 的抑制剂,可刺激adenosine monophosphate (AMP)-activated protein kinase (Ampk)依赖性信号传导。BC1618 可促进线粒体分裂,促进自噬并提高肝胰岛素敏感性。 |
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S1396 |
Resveratrol (SRT501)Resveratrol (SRT501, trans-Resveratrol)具有广泛靶点,包括环氧酶(如COX, IC50=1.1 μM)、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素,具有抗癌,抗炎,降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
![]() ![]() Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
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S2542 |
Phenformin (NSC-756501) HClPhenformin HCl (NSC-756501, Phenethylbiguanide)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。 |
![]() ![]() 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.
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S4895 |
Nilotinib hydrochloride monohydrateNilotinib (AMN-107, Tasigna) hydrochloride monohydrate 是一种选择性的 Bcr-Abl 的口服生物利用抑制剂,在鼠骨髓祖细胞中的IC50值小于30 nM。Nilotinib 通过 AMPK 激活来诱导自噬。 |
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S5284 |
Adenosine 5'-monophosphate monohydrateAdenosine 5'-monophosphate monohydrate (5'-Adenylic acid, 5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK). |
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S3296 |
HispidulinHispidulin (Dinatin) 是一种在许多传统中草药中存在的天然活性成分,对癌蛋白激酶 Pim-1 具有抑制活性,其IC50值为2.71 μM。Hispidulin 通过 mitochondrial dysfunction 来诱导凋亡,并可抑制HepG2癌细胞中的 P13k/Akt 的信号通路。Hispidulin 通过激活 AMPK 信号通路发挥抗骨质疏松和骨吸收减弱的作用。 |
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S8335 |
PF-06409577PF-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)。 |
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S3832 |
EuphorbiasteroidEuphorbiasteroid (Euphorbia factor L1)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。 |
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S8953 |
ASP4132ASP4132 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。 |
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S7898 |
GSK621GSK621是一种特异性且有效的AMPK激活剂。 |
![]() ![]() 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.
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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。 |
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S5958 |
MetforminMetformin (1,1-Dimethylbiguanide) 是一种广泛用于治疗2型糖尿病的药物,可激活肝细胞中的 AMP-activated protein kinase (AMPK)。Metformin 可促进单核细胞中的线粒体自噬。Metformin 可通过激活 JNK/p38 MAPK 途径和GADD153来诱导肺癌细胞凋亡。 |
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S0795 |
O-304O-304 (O-304X) 是一种口服活性的 AMPK activated protein kinase (AMPK) 的泛激活剂。O-304 (O-304X) 作为治疗2型糖尿病(T2D)和相关心血管并发症的新型药物具有巨大潜力。 |
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S3341 |
Palmitoleic acidPalmitoleic acid (POA, Palmitoleate) 可通过依赖于PPARα的 AMPK 和 FGF-21 活化来刺激肝脏中葡萄糖的摄取。 |
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S8803 |
MK-3903MK-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。 |
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S0411 |
BAM 15BAM 15 是一种新型的 mitochondrial protonophore 的解偶联剂,能够保护哺乳动物免受急性肾缺血-再灌注损伤和冷诱导的微管损伤。BAM 15 也是一种有效的 AMPK 激活剂。BAM 15 可减轻iPS分化的视网膜组织中运输引起的凋亡。 |
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S9096 |
ligustroflavoneLigustroflavone (Nuezhenoside), isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator. |
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S2942 |
EB-3DEB-3D 是一种有效的 choline kinase α (ChoKα) 的选择性抑制剂,对ChoKα1的IC50值为1 μM。EB-3D 可在白血病T细胞中诱导 AMPK-mTOR 通路失调和凋亡。 |
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S7953 |
ETC-1002ETC-1002 (Bempedoic acid, ESP-55016)是一种可用于口服、降低LDL-C的小分子,是肝脏AMPK的激活剂。ETC-1002 对肝ATP-citrate lyase具有有效的抑制作用(IC50 = 29 uM)。 |
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S4460 |
IMM-H007IMM-H007 是一种腺苷衍生物,是 AMP-Activated Protein Kinase (AMPK) 的激活剂。IMM-H007 是一种治疗心功能不全的潜在药物。IMM-H007 可通过钝化 NF-κB 和 JNK/AP1 信号传导负向调节内皮炎症。IMM-H007 可抑制 ABCA1 (ATP binding cassette subfamily a member 1) 的降解并促进其在巨噬细胞中的细胞表面定位,从而促进胆固醇外流。 |
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S9604 |
IM156IM156 (HL156A),一种二甲双胍衍生物,也是 AMPK 的有效激活剂,可增强AMPK磷酸化。IM156 可通过抑制 complex I 来阻止 oxidative phosphorylation (OXPHOS),并增加细胞凋亡。IM156 可改善各种类型的纤维化并抑制肿瘤。 |
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S9116 |
Chikusetsusaponin IVaChikusetsusaponin IVa (Calenduloside F) 是三萜类皂苷的主要活性成分,具有多种药理活性,包括对各种癌细胞的细胞毒活性,抗炎活性,预防龋齿和诱导人五味子霉素肾毒性。Chikusetsusaponin IVa 也是一种新型的 AMPK 激活剂。 |
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S1323 |
7-Methoxyisoflavone7-Methoxyisoflavone (MIF) 是一种 adenosine monophosphate-activated protein kinase (AMPK) 的有效激活剂。 |
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S1321 |
Urolithin BUrolithin B 通过减少 IκBα 的磷酸化和降解来抑制 NF-κB 活性。Urolithin B 可抑制 JNK、ERK 和 Akt 的磷酸化,并增强 AMPK 的磷酸化。Urolithin B 也是 skeletal muscle mass 的调节剂。 |
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S1273 |
AmarogentinAmarogentin (AG) 是一种主要从 Swertia 和 Gentiana 根中提取的裂环烯醚苷,具有抗氧化、抗肿瘤和抗糖尿病的作用。Amarogentin 是苦味受体 TAS2R1 的激动剂,可抑制LAD-2细胞中substance P诱导的新合成的 TNF-α 的产生。Amarogentin 通过 G2/M 细胞周期的阻滞和 PI3K/Akt 信号通路诱导人胃癌细胞(SNU-16)的凋亡。Amarogentin (AG) 可与 AMP-activated protein kinase (AMPK) 的α2亚基相互作用,并激活三聚体激酶,其EC50值为277 pM。 |
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S4561 |
DanthronDanthron (Chrysazin, Antrapurol) 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。 |
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S6221 |
Methyl cinnamateMethyl 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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S3299 |
DemethyleneberberineDemethyleneberberine (DMB) 是黄柏Cortex Phellodendri Chinensis (CPC) 的成分,可显著地缓解体重减轻并降低 myeloperoxidase (MPO) 活性,同时显著地减少促炎细胞因子的生成,例如 interleukin (IL)-6 和 tumor necrosis factor-α (TNF-α),并抑制 NF-κB 信号通路的激活。Demethyleneberberine (DMB) 可以通过激活 AMPK 途径改善NAFLD (非酒精性脂肪肝疾病)。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) 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。 |
![]() ![]() 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. |
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S1113 |
GSK690693GSK690693 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。 |
![]() ![]() 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. |
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E0022New |
Ophiopogonin DOphiopogonin D (OJV-VI, Deacetylophiopogonin C) 是一种从中草药麦冬中分离得到的甾体糖苷,具有抗肿瘤作用。Ophiopogonin D 可通过调节 ITGB1/FAK/Src/AKT/β-catenin/MMP-9 信号轴抑制TGF-β1介导的MDA-MB-231细胞转移行为。Ophiopogonin D 还通过抑制小鼠肺上皮细胞中的 AMPK/NF-κB 通路来减轻 PM2.5 诱导的炎症。 |
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S7306 |
Dorsomorphin (Compound C) 2HClDorsomorphin 2HCl (BML-275, Compound C) 是一种有效的,可逆的,选择性AMPK抑制剂,在无细胞试验中Ki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。 |
![]() ![]() 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. |
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S7317 |
WZ4003WZ4003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。 |
![]() ![]() 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) |
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S7318 |
HTH-01-015HTH-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。 |
![]() ![]() 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).
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S8274 |
STO-609STO-609 是特异性的CaM-KK的抑制剂,抑制CaM-KKα和CaM-KKβ的活性,Ki值分别为80 ng/ml和15 ng/ml,并抑制其自身磷酸化活性。STO-609 可抑制 AMPKK 活性并抑制自噬。 |
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S8161 |
ON123300ON123300是有效的多靶点激酶抑制剂,对CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。 |
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S0177 |
XMD-17-51XMD-17-51 (XMD17-51)是一种有效的具有高度选择性的 NUAK1 的抑制剂。 |
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S7840 |
Dorsomorphin (Compound C)Dorsomorphin (Compound C, BML-275)是一种有效的,可逆选择性 AMPK 抑制剂,无细胞试验中 Ki 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。如需进行动物实验,建议选择可水溶产品 S7306 Dorsomorphin (Compound C) 2HCl。 |
![]() ![]() 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 |
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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。 |
![]() ![]() 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. |
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S2697 |
A-769662A-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。 |
![]() ![]() 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. |
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S1802 |
AICAR (Acadesine)AICAR (Acadesine, NSC105823, AICA Riboside)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。 |
![]() ![]() 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). |
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E0653New |
Trans-ferulic acidTrans-ferulic acid是高糖条件下AMPK的强效激活剂。 |
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E0204New |
Poricoic acid APoricoic acid A 是从茯苓的表层中分离出来的 Poricic acid A 激活 AMPK 以减弱肾纤维化中的成纤维细胞活化和异常细胞外基质重塑。Poricic acid A 也是色氨酸羟化酶-1 (tryptophan hydroxylase-1, TPH-1) 的调节剂。 |
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E1031New |
MK-8722MK-8722 是一种有效的、直接的、所有 12 种哺乳动物 泛AMPK 复合物的变构激活剂。 |
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S9860New |
BC1618BC1618 是一种口服活性的 Fbxo48 的抑制剂,可刺激adenosine monophosphate (AMP)-activated protein kinase (Ampk)依赖性信号传导。BC1618 可促进线粒体分裂,促进自噬并提高肝胰岛素敏感性。 |
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S1396 |
Resveratrol (SRT501)Resveratrol (SRT501, trans-Resveratrol)具有广泛靶点,包括环氧酶(如COX, IC50=1.1 μM)、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素,具有抗癌,抗炎,降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
![]() ![]() Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
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S2542 |
Phenformin (NSC-756501) HClPhenformin HCl (NSC-756501, Phenethylbiguanide)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。 |
![]() ![]() 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.
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S4895 |
Nilotinib hydrochloride monohydrateNilotinib (AMN-107, Tasigna) hydrochloride monohydrate 是一种选择性的 Bcr-Abl 的口服生物利用抑制剂,在鼠骨髓祖细胞中的IC50值小于30 nM。Nilotinib 通过 AMPK 激活来诱导自噬。 |
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S5284 |
Adenosine 5'-monophosphate monohydrateAdenosine 5'-monophosphate monohydrate (5'-Adenylic acid, 5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK). |
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S3296 |
HispidulinHispidulin (Dinatin) 是一种在许多传统中草药中存在的天然活性成分,对癌蛋白激酶 Pim-1 具有抑制活性,其IC50值为2.71 μM。Hispidulin 通过 mitochondrial dysfunction 来诱导凋亡,并可抑制HepG2癌细胞中的 P13k/Akt 的信号通路。Hispidulin 通过激活 AMPK 信号通路发挥抗骨质疏松和骨吸收减弱的作用。 |
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S8335 |
PF-06409577PF-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)。 |
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S3832 |
EuphorbiasteroidEuphorbiasteroid (Euphorbia factor L1)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。 |
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S8953 |
ASP4132ASP4132 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。 |
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S7898 |
GSK621GSK621是一种特异性且有效的AMPK激活剂。 |
![]() ![]() 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.
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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。 |
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S5958 |
MetforminMetformin (1,1-Dimethylbiguanide) 是一种广泛用于治疗2型糖尿病的药物,可激活肝细胞中的 AMP-activated protein kinase (AMPK)。Metformin 可促进单核细胞中的线粒体自噬。Metformin 可通过激活 JNK/p38 MAPK 途径和GADD153来诱导肺癌细胞凋亡。 |
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S0795 |
O-304O-304 (O-304X) 是一种口服活性的 AMPK activated protein kinase (AMPK) 的泛激活剂。O-304 (O-304X) 作为治疗2型糖尿病(T2D)和相关心血管并发症的新型药物具有巨大潜力。 |
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S3341 |
Palmitoleic acidPalmitoleic acid (POA, Palmitoleate) 可通过依赖于PPARα的 AMPK 和 FGF-21 活化来刺激肝脏中葡萄糖的摄取。 |
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S8803 |
MK-3903MK-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。 |
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S0411 |
BAM 15BAM 15 是一种新型的 mitochondrial protonophore 的解偶联剂,能够保护哺乳动物免受急性肾缺血-再灌注损伤和冷诱导的微管损伤。BAM 15 也是一种有效的 AMPK 激活剂。BAM 15 可减轻iPS分化的视网膜组织中运输引起的凋亡。 |
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S9096 |
ligustroflavoneLigustroflavone (Nuezhenoside), isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator. |
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S2942 |
EB-3DEB-3D 是一种有效的 choline kinase α (ChoKα) 的选择性抑制剂,对ChoKα1的IC50值为1 μM。EB-3D 可在白血病T细胞中诱导 AMPK-mTOR 通路失调和凋亡。 |
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S7953 |
ETC-1002ETC-1002 (Bempedoic acid, ESP-55016)是一种可用于口服、降低LDL-C的小分子,是肝脏AMPK的激活剂。ETC-1002 对肝ATP-citrate lyase具有有效的抑制作用(IC50 = 29 uM)。 |
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S4460 |
IMM-H007IMM-H007 是一种腺苷衍生物,是 AMP-Activated Protein Kinase (AMPK) 的激活剂。IMM-H007 是一种治疗心功能不全的潜在药物。IMM-H007 可通过钝化 NF-κB 和 JNK/AP1 信号传导负向调节内皮炎症。IMM-H007 可抑制 ABCA1 (ATP binding cassette subfamily a member 1) 的降解并促进其在巨噬细胞中的细胞表面定位,从而促进胆固醇外流。 |
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S9604 |
IM156IM156 (HL156A),一种二甲双胍衍生物,也是 AMPK 的有效激活剂,可增强AMPK磷酸化。IM156 可通过抑制 complex I 来阻止 oxidative phosphorylation (OXPHOS),并增加细胞凋亡。IM156 可改善各种类型的纤维化并抑制肿瘤。 |
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S9116 |
Chikusetsusaponin IVaChikusetsusaponin IVa (Calenduloside F) 是三萜类皂苷的主要活性成分,具有多种药理活性,包括对各种癌细胞的细胞毒活性,抗炎活性,预防龋齿和诱导人五味子霉素肾毒性。Chikusetsusaponin IVa 也是一种新型的 AMPK 激活剂。 |
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S1323 |
7-Methoxyisoflavone7-Methoxyisoflavone (MIF) 是一种 adenosine monophosphate-activated protein kinase (AMPK) 的有效激活剂。 |
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S1321 |
Urolithin BUrolithin B 通过减少 IκBα 的磷酸化和降解来抑制 NF-κB 活性。Urolithin B 可抑制 JNK、ERK 和 Akt 的磷酸化,并增强 AMPK 的磷酸化。Urolithin B 也是 skeletal muscle mass 的调节剂。 |
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S1273 |
AmarogentinAmarogentin (AG) 是一种主要从 Swertia 和 Gentiana 根中提取的裂环烯醚苷,具有抗氧化、抗肿瘤和抗糖尿病的作用。Amarogentin 是苦味受体 TAS2R1 的激动剂,可抑制LAD-2细胞中substance P诱导的新合成的 TNF-α 的产生。Amarogentin 通过 G2/M 细胞周期的阻滞和 PI3K/Akt 信号通路诱导人胃癌细胞(SNU-16)的凋亡。Amarogentin (AG) 可与 AMP-activated protein kinase (AMPK) 的α2亚基相互作用,并激活三聚体激酶,其EC50值为277 pM。 |
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S4561 |
DanthronDanthron (Chrysazin, Antrapurol) 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。 |
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S6221 |
Methyl cinnamateMethyl 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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S3299 |
DemethyleneberberineDemethyleneberberine (DMB) 是黄柏Cortex Phellodendri Chinensis (CPC) 的成分,可显著地缓解体重减轻并降低 myeloperoxidase (MPO) 活性,同时显著地减少促炎细胞因子的生成,例如 interleukin (IL)-6 和 tumor necrosis factor-α (TNF-α),并抑制 NF-κB 信号通路的激活。Demethyleneberberine (DMB) 可以通过激活 AMPK 途径改善NAFLD (非酒精性脂肪肝疾病)。 |