AMPK

Inhibitory Selectivity

Catalog No.	Inhibitor Name	AMPK
A13720	Dorsomorphin 2HCl	**
A14312	WZ4003	****
A11970	Dorsomorphin	**
A16281	HTH-01-015	***
A11071	A 769662	*
A15815	ETC-1002

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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A-769662

Catalog No. A11071
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AMPK 激活剂

A-769662是AMP激活的蛋白激酶（AMPK）的新激活剂。了解更多

Product Citations (4)

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- Daniel Missailidis, .et al. Dysregulated Provision of Oxidisable Substrates to the Mitochondria in ME/CFS Lymphoblasts, Int J Mol Sci., 2021, Feb; 22(4): 2046 PMID: 33669532
- Lieberthal W, .et al. AMPK-mediated activation of Akt protects renal tubular cells from stress-induced apoptosis in vitro and ameliorates ischemic AKI in vivo, Am J Physiol Renal Physiol, 2019, 2019 PMID: 30995114
- Kikuchi H, .et al. Failure to sense energy depletion may be a novel therapeutic target in chronic kidney disease, Kidney Int, 2018, Nov 13. pii: S0085-2538(18)30635-5 PMID: 30455054
- Schneider H, .et al. AMPK Dilates Resistance Arteries via Activation of SERCA and BKCa Channels in Smooth Muscle, Hypertension, 2015, Jul;66(1):108-16 PMID: 26034200
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Acadesine (Aicar,NSC 105823)

Catalog No. A10028
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AMPK 激活剂

Acadesine (Aicar,NSC 105823)是肝细胞和脂肪细胞中AMPK的选择性激活剂。了解更多

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- R. Lim, .et al. Activation of AMPK in human fetal membranes alleviates infection-induced expression of pro-inflammatory and pro-labour mediators., Placenta, 2015, Apr;36(4):454-62 PMID: 25659498
- Stella Liong, .et al. Activation of AMPK improves inflammation and insulin resistance in adipose tissue and skeletal muscle from pregnant women., J Physiol Biochem, 2015, Dec;71(4):703-17 PMID: 26407807
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BML-275 (Dorsomorphin)

Catalog No. A11970
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AMPK 抑制剂

BML-275 (Dorsomorphin)是一种可渗透细胞的吡唑并嘧啶化合物，显示为AMP激活的蛋白激酶（AMPK）和脂肪酸合酶抑制剂。了解更多

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- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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Dorsomorphin 2HCl

Catalog No. A13720
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BMP 抑制剂

Dorsomorphin 2HCl (BML-275)是BMP信号传导的选择性小分子抑制剂，可促进胚胎干细胞的心肌发生。Dorsomorphin通过抑制骨形态发生蛋白信号转导逆转乳腺癌起始细胞的间质表型。了解更多

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- Kameshima S, .et al. Eukaryotic elongation factor 2 (eEF2) kinase/eEF2 plays protective roles against glucose deprivation-induced cell death in H9c2 cardiomyoblasts, Apoptosis, 2019, Feb 8 PMID: 30737648
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ETC-1002

Catalog No. A15815
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ACL 抑制剂 and AMPK 激活剂

ETC-1002是一种新颖的，一流的可以降低LDL-C的小分子；肝AMP激活的蛋白激酶（AMPK）的激活剂;对肝ATP-柠檬酸裂解酶也具有有效的抑制活性（IC50 = 29 uM）。了解更多

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GSK621

Catalog No. A15896
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AMPK 激活剂

GSK621是有效的选择性AMPK激动剂。了解更多

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- Harvey W. Smith, .et al. An ErbB2/c-Src axis links bioenergetics with PRC2 translation to drive epigenetic reprogramming and mammary tumorigenesis, Nat Commun, 2019, 10, 2901(2019) PMID: 31263101
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YLF-466D

Catalog No. A16284
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AMPK 激活剂

YLF-466D是一种变构AMPK激活剂。了解更多

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ex229 (compound 991)

Catalog No. A16795
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AMPK 激活剂

ex229 (compound 991)是一种有效的AMPK活化剂，在活化AMPK方面比A769662的效力高5-10倍。了解更多

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- CN Koyani, .et al. Empagliflozin Protects Heart From Inflammation and Energy Depletion via AMPK Activation, Pharmacol Res, 2020, May 17;158:104870 PMID: 32434052
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MK8722

Catalog No. A13392
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pan-AMPK activator

MK8722 is a potent and systemic pan-AMPK activator. 了解更多

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ZLN024

Catalog No. A21963
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AMPK allosteric activator

ZLN024 is an AMPK allosteric activator. 了解更多

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Phenformin hydrochloride

Catalog No. A10717
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Phenformin hydrochloride是双胍类药物中苯乙双胍的盐酸盐，具有抗糖尿病活性。了解更多

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WZ4003

Catalog No. A14312
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NUAK kinase 抑制剂

WZ4003是一种高度特异性的NUAK激酶抑制剂，对于NUAK1和NUAK2的IC50为20 nM和100 nM。了解更多

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HTH-01-015

Catalog No. A16281
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NUAK1 抑制剂

HTH-01-015是NUAK1的有效和选择性抑制剂（IC50 = 100 nM），并且不影响包括其他AMPK家族成员在内的139种其他激酶的活性。了解更多

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PF-06409577

Catalog No. A16801
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AMPK 激活剂

PF-06409577是口服生物可利用的AMPK激活剂，在TR-FRET试验中，对AMPK α1β1γ1的EC50为7 nM。在膜片钳试验（100 uM）中没有检测到对hERG的抑制作用，也不是人类主要细胞色素P450亚型微粒体活性的抑制剂（IC50>100 uM）。了解更多

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MK-3903

Catalog No. A17063
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AMPK 激活剂

MK-3903是有效的选择性AMPK激活剂（EC50 = 8 nM）。口服给药后，MK-3903在小鼠肝脏中表现出强大的靶标参与性，从而改善了小鼠的脂质代谢和胰岛素敏感性。了解更多

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