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PI3K / Akt / mTOR

PI3K / Akt / mTOR

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AT7867 2HCl

Catalog No. A15006
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Akt 抑制剂

AT7867 dihydrochloride是一种有效的ATP竞争性Akt1/2/3和p70S6K/PKA抑制剂，IC50分别为32 nM/17 nM/47 nM和85 nM/20 nM，在AGC激酶家族之外几乎没有活性。了解更多

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Tomatidine

Catalog No. A16233
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ERK/Akt/NF-kB 抑制剂

Tomatidine抑制ERK，Akt的磷酸化以及NF-kB的核含量。具有抗炎特性。了解更多

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Afuresertib

Catalog No. A16392
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Akt 抑制剂

Afuresertib是一种有效的口服生物利用性Akt抑制剂，对于Akt1，Akt2和Akt3，Ki分别为0.08 nM，2 nM和2.6 nM。了解更多

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Borussertib

Catalog No. A13364
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Akt inhibitor

Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt. 了解更多

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AKT Kinase Inhibitor

Catalog No. A11285
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Akt kinase inhibitor

AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity. 了解更多

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Isobavachalcone

Catalog No. A11453
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Akt inhibitor

Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). 了解更多

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3CAI

Catalog No. A20924
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AKT1/AKT2 inhibitor

3CAI is a potent and specific AKT1 and AKT2 inhibitor. 了解更多

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Solenopsin

Catalog No. A21087
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ATP-competitive AKT inhibitor

Solenopsin is an ATP-competitive AKT inhibitor with IC50 value of 10 μM . 了解更多

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YS-49

Catalog No. A21198
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PI3K/Akt activator

YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. 了解更多

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Ipatasertib dihydrochloride

Catalog No. A21734
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pan-Akt inhibitor

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA. 了解更多

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PF-AKT400

Catalog No. A21991
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Akt inhibitor

PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM). 了解更多

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AKT-IN-1

Catalog No. A21009
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AKT inhibitor

AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM. 了解更多

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Palomid 529 (P529)

Catalog No. A10693
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AKT 抑制剂

Palomid 529是PI3K/Akt/mTOR途径的双重TORC1/2抑制剂，在血管生成和细胞增殖中具有广泛的活性。了解更多

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GDC-0068 (Ipatasertib, RG-7440)

Catalog No. A11246
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Akt 抑制剂

GDC-0068 (Ipatasertib,RG-7440)是一种选择性的，具有ATP竞争性的pan-Akt抑制剂，在无细胞试验中，其靶向Akt1、2和3的IC50值分别为5、18和8 nM。了解更多

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TIC10 isomer

Catalog No. A12720
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AKT 抑制剂?

TIC10通过Foxo3a使Akt和ERK失活，从而诱导TRAIL，具有优越的药物特性：跨血脑屏障传递，优异的稳定性和改善的药代动力学。了解更多

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10-DEBC HCl

Catalog No. A13590
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AKT/PKB 抑制剂?

10-DEBC HCl是Akt/PKB的选择性抑制剂。它抑制IGF-1刺激的磷酸化和Akt的激活（在2.5μM时完全抑制），抑制mTOR，p70 S6激酶的下游激活。了解更多

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SR-13668

Catalog No. A13554
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AKT 抑制剂?

SR-136683是一种口服制剂，其中含有血管内皮生长因子受体（VEGFR）和血小板衍生生长因子受体（PDGFR）的小分子受体酪氨酸激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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Afuresertib HCl

Catalog No. A13030
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AKT 抑制剂?

Afuresertib HCl，也称为GSK2110183，是具有潜在抗肿瘤活性的丝氨酸/苏氨酸蛋白激酶Akt（蛋白激酶B）的生物利用抑制剂。它结合并抑制Akt的活性，这可能导致PI3K/Akt信号传导途径的抑制和肿瘤细胞的增殖以及肿瘤细胞凋亡的诱导.PI3K/Akt信号传导途径的激活通常与肿瘤发生有关，PI3K/Akt信号传导失调可能有助于肿瘤对多种抗肿瘤药的耐药性。了解更多

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SC79

Catalog No. A15541
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Akt phosphorylation activator

SC79是AKT激活剂。SC79绑定到模仿PtdIns（3,4,5）P3的结合的Akt的plecktrin同源（PH）域，以诱导Akt的构象变化，从而增强磷酸化和激活。了解更多

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GSK2141795 (Uprosertib, GSK795)

Catalog No. A15809
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Akt 抑制剂

GSK2141795 (Uprosertib,GSK795)结合并抑制Akt的活性，这可能导致PI3K/Akt信号传导途径的抑制和肿瘤细胞的增殖以及肿瘤细胞凋亡的诱导。了解更多

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SC 66

Catalog No. A12081
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Akt 抑制剂

SC 66是Akt的变构抑制剂，促进Akt的泛素化和失活。它在体外和体内显示抗癌活性。了解更多

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TIC10

Catalog No. A15903
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Akt 抑制剂?

TIC10通过Foxo3a使Akt和ERK失活，从而诱导TRAIL，具有优越的药物特性：跨血脑屏障传递，优异的稳定性和改善的药代动力学。了解更多

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Akt1 and Akt2-IN-1

Catalog No. A16285
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AKT 1/2 抑制剂

Akt1 and Akt2-IN-1是Akt1（IC50 = 3.5 nM）和Akt2（IC50 = 42 nM）的变构抑制剂，具有有效且平衡的活性。了解更多

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ARQ-092 (Miransertib)

Catalog No. A16286
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AKT 抑制剂

ARQ 092是一种口服活化，有效和选择性的AKT抑制剂，IC50值：5.0 nM（AKT1）；4.5 nM（AKT2）；16 nM（AKT3）。了解更多

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GSK690693

Catalog No. A11030
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AKT 抑制剂

GSK690693是一种新型的ATP竞争性低纳摩尔泛Akt激酶抑制剂（IC50值分别为Akt1、2和3的2、13和9 nM）。了解更多

Product Citations (1)

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- Khan MI, .et al. Thalidomide attenuates development of m0rphine dependence in mice by inhibiting PI3K/Akt and nitric oxide signaling pathways, Prog Neuropsychopharmacol Biol Psychiatry, 2018, Mar 2;82:39-48 PMID: 9223784
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AZD5363

Catalog No. A11759
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AKT 抑制剂

AZD5363是有效的AKT抑制剂，在体内具有药效学活性，有潜力作为单一疗法或联合用药来治疗一系列实体瘤和血液肿瘤。了解更多

Product Citations (3)

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- Giri R. Gnawali, .et al. Synthesis of 2-oxoquinoline derivatives as dual pim and mTORC protein kinase inhibitors, Medicinal Chemistry Research, 2022, 31: 1154-1175
- Jeremiah J Bearss, .et al. EDC3 phosphorylation regulates growth and invasion through controlling P-body formation and dynamics, EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
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AKT inhibitor VIII (AKTI-1/2)

Catalog No. A11286
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AKT 抑制剂

AKT inhibitor VIII (AKTI-1/2)是一种细胞可渗透且可逆的喹喔啉化合物，在体外激酶测定中，该化合物有效和选择性地抑制Akt1/Akt2活性（对于Akt1，Akt2和Akt3，IC50分别为58 nM，210 nM和2.12μM）。了解更多

Product Citations (2)

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- Bjune K, .et al. Inhibitors of AKT kinase increase LDL receptor mRNA expression by two different mechanisms, PLoS One, 2019, Jun 19;14(6):e0218537 PMID: 31216345
- Hoshiba T, .et al. Decellularized matrices as in vitro models of extracellular matrix in tumor tissues at different malignant levels: Mechanism of 5-fluorouracil resistance in colorectal tumor cells, Biochim Biophys Acta, 2016, Nov;1863(11):2749-2757 PMID: 27558478
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A-674563

Catalog No. A11034
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Akt 抑制剂

A-674563是一种B/Akt抑制剂，IC50为14 nM，并且还显示出对PKA和CDK2的抑制活性，IC50分别为16和46 nM。了解更多

Product Citations (3)

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- Kobayashi T, .et al. A-674563 increases chondrocyte marker expression in cultured chondrocytes by inhibiting Sox9 degradation, Biochem Biophys Res Commun, 2018, Jan 1;495(1):1468-1475 PMID: 29196261
- Lin Xu, .et al. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells, Biochem Biophys Res Commun, 2016, Apr 15;472(4):662-8 PMID: 26920060
- Zou Y, .et al. Pre-clinical assessment of A-674563 as an anti-melanoma agent, Biochem Biophys Res Commun, 2016, Aug 12;477(1):1-8 PMID: 26970307
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Perifosine (NSC-639966)

Catalog No. A10709
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Akt 抑制剂

Perifosine (也为KRX-0401) 充当Akt抑制剂和PI3K抑制剂。了解更多

Product Citations (4)

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- Bjune K, .et al. Inhibitors of AKT kinase increase LDL receptor mRNA expression by two different mechanisms, PLoS One, 2019, Jun 19;14(6):e0218537 PMID: 31216345
- Kyoung-Jae Won, .et al. Stability of the cancer target DDIAS is regulated by the CHIP/HSP70 pathway in lung cancer cells, Cell Death Dis, 2017, Jan; 8(1): e2554 PMID: 28079882
- Zhipeng Li, .et al. A positive feedback loop involving EGFR/Akt/mTORC1 and IKK/NF-κB regulates head and neck squamous cell carcinoma proliferation, Oncotarget, 2016, May 31; 7(22): 31892–31906 PMID: 26895469
- Won KJ, .et al. NSC126188 induces apoptosis of prostate cancer PC-3 cells through inhibition of Akt membrane translocation, FoxO3a activation, and RhoB transcription., Apoptosis., 2014, Jan;19(1):179-90 PMID: 24085402
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MK-2206 2HCl

Catalog No. A10003
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AKT 抑制剂

MK-2206 2HCl是Akt1/2/3的高选择性抑制剂，IC50分别为8 nM/12 nM/65 nM。了解更多

Product Citations (17)

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Ali Nasrollahzadeh, .et al. Anti-proliferative activity of disulfiram through regulation of the AKT-FOXO axis: A proteomic study of molecular targets, Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Rona Aviram, .et al. Ultradian rhythms of AKT phosphorylation and gene expression emerge in the absence of the circadian clock components Per1 and Per2, PLoS Biol, 2021, Dec 30;19(12):e3001492 PMID: 34968386
- Cristina Rosell??-Busquets, .et al. Nystatin Regulates Axonal Extension and Regeneration by Modifying the Levels of Nitric Oxide, Front Mol Neurosci, 2020, 13: 56 PMID: 32317932
- Dai-Chi Liu, .et al. Chronic Activation of Gp1 mGluRs Leads to Distinct Refinement of Neural Network Activity Through Non-Canonical p53 and Akt Signaling, eNeuro, 2020, Mar 27;7(2):ENEURO.0438-19.2020 PMID: 32161037
- Nishihama K, .et al. Anti-apoptotic activity of human matrix metalloproteinase-2 attenuates diabetes mellitus, Metabolism, 2018, May;82:88-99 PMID: 29366755
- J Wei, .et al. Profiling the surface proteome identifies actionable biology for TSC1 mutant cells beyond mTORC1 signaling, bioRxiv, 2018, 2018
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
- Wan-Ting Hu, .et al. The O-glycosylating enzyme GALNT2 suppresses the malignancy of gastric adenocarcinoma by reducing EGFR activities, Am J Cancer Res, 2018, 8(9): 1739-1751 PMID: 30323967
- Angela M. Gocher, .et al. Akt activation by Ca2+/calmodulin-dependent protein kinase kinase 2 (CaMKK2) in ovarian cancer cells, J Biol Chem, 2017, Aug 25; 292(34): 14188-14204 PMID: 28634229
- Kusuyama J, .et al. Constitutive activation of p46JNK2 is indispensable for C/EBPδ induction in the initial stage of adipogenic differentiation, Biochem J, 2017, Oct 5;474(20):3421-3437 PMID: 28887384
- Pi-Lin Sung, .et al. Periostin in tumor microenvironment is associated with poor prognosis and platinum resistance in epithelial ovarian carcinoma, Oncotarget, 2016, Jan 26; 7(4): 4036-4047 PMID: 26716408
- Mikaël M. Martino, .et al. Inhibition of IL-1R1/MyD88 signalling promotes mesenchymal stem cell-driven tissue regeneration, Nat Commun, 2016, 7: 11051 PMID: 27001940
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
- Jewett KA, .et al. The tumor suppressor p53 guides GluA1 homeostasis through Nedd4-2 during chronic elevation of neuronal activity., J Neurochem., 2015, Oct;135(2):226-33 PMID: 26250624

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