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PI3K / Akt / mTOR

PI3K / Akt / mTOR

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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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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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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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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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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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OTSSP167

Catalog No. A12851
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MELK 抑制剂

OTSSP167是一种高效的MELK（母体亮氨酸拉链激酶）抑制剂，IC50为0.41 nM。了解更多

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- Yubao Wang ,etc. Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival. Proc Natl Acad Sci USA. 2016 Aug 30; 113(35): 9810–9815.
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MELK-IN-1

Catalog No. A12675
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MELK inhibitor

MELK-IN-1 is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK) with an IC50 and a Ki of 3 nM and 0.39 nM, respectively. 了解更多

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JNJ-47117096 hydrochloride

Catalog No. A21542
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MELK inhibitor

JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM. 了解更多

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MELK-8a hydrochloride

Catalog No. A21751
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MELK inhibitor

MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM. 了解更多

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KU-55933

Catalog No. A10506
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ATM 抑制剂

KU-55933是ATM抑制剂，通过抑制细胞增殖，并通过阻断Akt过度激活的癌细胞中的Akt诱导凋亡。了解更多

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- Mariko Shikata, .et al. 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced Histone Acetylation via α7nAChR-Mediated PI3K/Akt Activation and Its Impact on γ-H2AX Generation, Chem Res Toxicol, 2021, Dec 20;34(12):2512-2521 PMID: 34784199
- Masaya Igase, .et al. Combination Therapy with Reovirus and ATM Inhibitor Enhances Cell Death and Virus Replication in Canine Melanoma, Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- Hayakawa K, .et al. Planar compression of extracellular substrates induces S phase arrest via ATM-independent CHK2 activation, Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
- Chwastek J, .et al. The ATM kinase inhibitor KU-55933 provides neuroprotection against hydrogen peroxide-induced cell damage via a γH2AX/p-p53/caspase-3-independent mechanism: Inhibition of calpain and cathepsin D, Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
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KU-60019

Catalog No. A10507
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ATM 抑制剂

KU-60019是一种强效特异性ATM抑制剂，IC50为6.3 nM。了解更多

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- Fu-Xing Gong, .et al. De-dimerization of PTB is catalyzed by PDI and is involved in the regulation of p53 translation, Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
- Hegedus C, .et al. PARP1 Inhibition Augments UVB-Mediated Mitochondrial Changes-Implications for UV-Induced DNA Repair and Photocarcinogenesis, Cancers (Basel), 2019, Dec 18;12(1) PMID: 31861350
- Masaya Igase, .et al. Combination Therapy with Reovirus and ATM Inhibitor Enhances Cell Death and Virus Replication in Canine Melanoma, Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- CHENGHUA LOU, .et al. Targeting the ataxia telangiectasia mutated pathway for effective therapy against hirsutine-resistant breast cancer cells, Oncol Lett, 2016, Jul; 12(1): 295-300 PMID: 27347141
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Chloroquine Phosphate

Catalog No. A16445
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Chloroquine Phosphate是一种4-氨基喹啉抗疟和抗类风湿药，也可作为ATM活化剂。了解更多

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- Egawa Y, .et al. Therapeutic potential of CPI-613 for targeting tumorous mitochondrial energy metabolism and inhibiting autophagy in clear cell sarcoma, PLoS One, 2018, Jun 7;13(6):e0198940 PMID: 29879220
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AZD6738 (Ceralasertib)

Catalog No. A15794
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ATR 抑制剂

AZD6738是一种有效的ATR激酶抑制剂，对分离的酶的IC50为1 nM，对细胞中ATR激酶依赖性CHK1磷酸化的IC50为74 nM。了解更多

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- Brian F Kiesel, .et al. Dose-dependent bioavailability and tissue distribution of the ATR inhibitor AZD6738 (ceralasertib) in mice, Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. The POLD1 R689W variant increases the sensitivity of colorectal cancer cells to ATR and CHK1 inhibitors, Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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AZD0156

Catalog No. A16419
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ATM 抑制剂

AZD0156是有效且选择性的ATM激酶抑制剂，具有潜在的化学/放射致敏和抗肿瘤活性。了解更多

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- Yi-Ru Pan, .et al. ATM Inhibitor Suppresses Gemcitabine-Resistant BTC Growth in a Polymerase θ Deficiency-Dependent Manner, Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
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CP-466722

Catalog No. A11086
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ATM 抑制剂

CP-466722是一种特殊的ATM抑制剂，可抑制细胞依赖ATM的磷酸化事件，并且ATM功能的破坏会导致特征性的细胞周期检查点缺陷。了解更多

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Schisandrin B

Catalog No. A11991
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Schisandrin B是从五味子五味子或五味子的果实中分离出的最丰富的二苯并环辛二烯，它是一种安全的ATR和P-gp抑制剂。了解更多

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CGK 733

Catalog No. A13191
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ATM/ATR 抑制剂

CGK733是ATR和ATM激酶的选择性抑制剂。在过早衰老的乳腺癌细胞中诱导细胞死亡。了解更多

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AZ-20

Catalog No. A13205
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ATR kinase 抑制剂

AZ20是一种有效的选择性ATR抑制剂，IC50值为5 nM。了解更多

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VE-822

Catalog No. A13289
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ATR 抑制剂

VE-822是有效的ATR抑制剂。了解更多

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Mirin

Catalog No. A15842
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ATM 抑制剂

Mirin可防止ATM激活以响应双链断裂（IC50 = 12 uM），并诱导G2细胞周期停滞。了解更多

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AZ32

Catalog No. A16814
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ATM 抑制剂

AZ32是ATM激酶的特异性抑制剂，对小鼠具有良好的BBB渗透性，ATM酶的IC50值<0.0062 uM。它对ATR有足够的选择性，并且具有较高的细胞通透性。了解更多

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AZ31

Catalog No. A16813
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ATM 抑制剂

AZ31是一种新的选择性ATM抑制剂，IC50<0.0012 uM，对密切相关的酶具有良好的选择性（对DNA-PK和PI3Kα的选择性大于500倍，对mTOR、PI3Kβ和PI3Kγ的选择性大于1000倍）。了解更多

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AZD1390

Catalog No. A16798
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ATM 抑制剂

AZD1390是一流的口服中枢神经渗透性ATM抑制剂，在细胞中的IC50为0.78 nM，对PIKK酶家族中密切相关的成员具有10,000倍以上的选择性，并且在多种激酶中均具有出色的选择性。了解更多

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KU 59403

Catalog No. A20928
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ATM inhibitor

KU 59403 is a potent ATM inhibitor, with an IC50 of 3 nM. 了解更多

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