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搜索结果：“akt”

“akt”的搜索结果

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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

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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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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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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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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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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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Triciribine

Catalog No. A13210
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AKT 抑制剂

Triciribine，也称为API-2，可抑制Akt的磷酸化水平和激酶活性。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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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

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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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A-443654

Catalog No. A11287
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Akt 抑制剂

A-443654是Ki值为160 pM的特异Akt抑制剂，可干扰有丝分裂进程和双极纺锤体形成。了解更多

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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

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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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Triciribine phosphate (NSC-280594)

Catalog No. A11033
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AKT 抑制剂

Triciribine phosphate是一种DNA synthesis抑制剂，也抑制PC3细胞系中的Akt和CEM-SS，H9，H9IIIB，U1细胞中的HIV-1，IC50分别为130 nM和20 nM；对PI3K/PDK1没有抑制作用；作用于缺乏腺苷激酶的细胞，活性降低5000 了解更多

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PHT-427

Catalog No. A11032
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AKT 抑制剂

PHT-427是一种新型的Akt/磷脂酰肌醇依赖性蛋白激酶1 pleckstrin同源域抑制剂。了解更多

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CCT128930

Catalog No. A11031
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AKT 抑制剂

CCT128930是一种具有ATP竞争性的AKT抑制剂，是一种有效的高级吡咯并嘧啶铅化合物，相对于PKA表现出对AKT的选择性，可通过靶向单个氨基酸差异实现。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

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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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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

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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

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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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ON-01910 (rigosertib)

Catalog No. A10673
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PLK 抑制剂

ON-01910 (rigosertib)通过涉及PI3K/AKT抑制和氧化应激诱导的双重作用机制对慢性淋巴细胞白血病细胞具有选择性的细胞毒性。了解更多

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SNX-2112

Catalog No. A11189
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Hsp90 抑制剂

SNX-2112是目前在临床试验中具有抗癌特性的热激蛋白90（Hsp90）抑制剂。SNX-2112通过Akt/mTOR/p70S6K抑制以时间和剂量依赖的方式诱导自噬。SNX-2112在人黑素瘤A-375细胞中诱导明显的凋亡和自噬，可能是有效的靶向治疗剂。了解更多

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- Michael Heider, .et al. The IMiD target CRBN determines HSP90 activity toward transmembrane proteins essential in multiple myeloma, Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
- Hiroki Murano, .et al. A purine-type heat shock protein 90 inhibitor promotes the heat shock response in Arabidopsis, Plant Biotechnol Rep, 2017, 11:107-113
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Artesunate

Catalog No. A10087
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cytochrome oxidase 抑制剂

Artesunate是用于治疗疟疾的青蒿素的半合成衍生物。它也被证明可以有效对抗其他寄生虫，例如肝吸虫。青蒿琥酯还显示出针对不同肿瘤类型的癌细胞系的细胞毒性作用。青蒿琥酯已显示出通过抑制类风湿关节炎成纤维细胞样滑膜细胞中的NF-B和PI3激酶/ Akt信号通路来抑制TNF诱导的促炎细胞因子的产生。了解更多

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BX-795

Catalog No. A11148
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PDK-1 抑制剂

BX-795是有效的PDK1抑制剂，可阻断肿瘤细胞中的PDK1/Akt信号传导并抑制培养物中多种肿瘤细胞系的锚定依赖性生长或诱导凋亡。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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TAK-733

Catalog No. A11040
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MEK 抑制剂

TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1，AKT3，c-RAF，CamK1，CDK2及c-Met等活性。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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