Akt

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Akt	Akt1	Akt2	Akt3	Other Targets
A10003	MK-2206 2HCl		***	***	**
A10709	Perifosine	*
A11030	GSK690693		****	***	***	PKCθ,PKCη,PrkX
A11246	Ipatasertib		****	**	***
A11759	AZD5363		****	***	***	ROCK2
A11024	PF-04691502	****				PI3Kδ,PI3Kα,PI3Kγ
A10094	AT7867		**	***	**	PKA,p70 S6K
A13210	Triciribine	*				HIV-1
A11031	CCT128930			****		p70 S6K,PKA
A11034	A-674563		***			PKA,CDK2,GSK-3β
A11032	PHT-427	*				PDK-1
A11286	Akti-1/2		**	*	*
A15809	Uprosertib		*	*	**
A16392	Afuresertib		****	****	****
A12464	AT13148		**	*	**	PKA,ROCK2,ROCK1
A14138	Miltefosine					PI3K,PKC
A10453	Honokiol					MEK
A12720	TIC10 Analogue					ERK
A13460	Deguelin					PI3K
A15903	TIC10					ERK
A11287	A-443654		****
A13590	10-DEBC HCl	*
A16286	ARQ-092 (Miransertib)		****	****	***

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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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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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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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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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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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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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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Akt-l-1

Catalog No. A12435
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AKT1 抑制剂

Akt-I-1是Akt1（IC50为4.6 μM）的特异性抑制剂，不抑制AKT2或AKT3。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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