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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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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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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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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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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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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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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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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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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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

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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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Miltefosine

Catalog No. A14138
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PI3K/Akt 抑制剂

Miltefosine在癌细胞系A431和HeLa中抑制PI3K/Akt活性，ED50为17.2μM和8.1μM。了解更多

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AT13148

Catalog No. A12464
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multi-AGC kinase 抑制剂

AT13148是一种新型多AGC激酶抑制剂，具有强大的药效和抗肿瘤活性，与其他AKT抑制剂相比，具有独特的作用机理。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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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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KP372-1

Catalog No. A12877
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Akt 抑制剂

KP372-1是合成的小分子AKT抑制剂。了解更多

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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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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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AT7867

Catalog No. A10094
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AKT 抑制剂

AT7867是AKT和下游激酶p70 S6激酶（p70S6K）以及蛋白激酶A的新型有效抑制剂。了解更多

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PF-04691502

Catalog No. A11024
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PI3K/mTOR 抑制剂

PF-04691502是PI3K/mTOR激酶抑制剂，也是在PI3K/mTOR信号传导途径中靶向磷脂酰肌醇3激酶（PI3K）和雷帕霉素（mTOR）哺乳动物靶标的药物。了解更多

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