Akt

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1078	MK-2206 2HCl	<1 mg/mL	14 mg/mL	<1 mg/mL
S1037	Perifosine (KRX-0401)	8 mg/mL	<1 mg/mL	15 mg/mL
S1113	GSK690693	<1 mg/mL	39 mg/mL	<1 mg/mL
S2808	GDC-0068	<1 mg/mL	92 mg/mL	92 mg/mL
S8019	AZD5363	<1 mg/mL	86 mg/mL	<1 mg/mL
S8500	BAY1125976	<1 mg/mL	11 mg/mL	<1 mg/mL
S8839	Borussertib	<1 mg/mL	100 mg/mL	<1 mg/mL
S2743	PF-04691502	<1 mg/mL	14 mg/mL	<1 mg/mL
S1558	AT7867	<1 mg/mL	68 mg/mL	5 mg/mL
S1117	Triciribine	<1 mg/mL	64 mg/mL	<1 mg/mL
S2635	CCT128930	<1 mg/mL	68 mg/mL	6 mg/mL
S2670	A-674563	72 mg/mL	72 mg/mL	18 mg/mL
S1556	PHT-427	<1 mg/mL	82 mg/mL	60 mg/mL
S3056	Miltefosine	81 mg/mL	<1 mg/mL	81 mg/mL
S2310	Honokiol	<1 mg/mL	53 mg/mL	<1 mg/mL
S7127	TIC10 Analogue	<1 mg/mL	11 mg/mL	<1 mg/mL
S7492	Uprosertib (GSK2141795)	<1 mg/mL	85 mg/mL	85 mg/mL
S7963	TIC10	<1 mg/mL	77 mg/mL	77 mg/mL
S7776	Akti-1/2	<1 mg/mL	22 mg/mL	<1 mg/mL
S5313	SC66	-1 mg/mL	55 mg/mL	-1 mg/mL
S4953	Usnic acid	-1 mg/mL	4 mg/mL	-1 mg/mL
S8339	Miransertib (ARQ 092) HCl	<1 mg/mL	75 mg/mL	4 mg/mL
S7521	Afuresertib (GSK2110183)	<1 mg/mL	85 mg/mL	85 mg/mL
S9315	Praeruptorin A	-1 mg/mL	77 mg/mL	-1 mg/mL
S3810	Scutellarin	-1 mg/mL	50 mg/mL	-1 mg/mL
S7563	AT13148	<1 mg/mL	62 mg/mL	<1 mg/mL
S8132	Deguelin	<1 mg/mL	78 mg/mL	78 mg/mL
S7863	SC79	<1 mg/mL	72 mg/mL	72 mg/mL
S9514	Rotundic acid	-1 mg/mL	98 mg/mL	-1 mg/mL
S9190	Oroxin B	-1 mg/mL	100 mg/mL	-1 mg/mL
S2323	Methyl-Hesperidin	100 mg/mL	100 mg/mL	<1 mg/mL

亜型選択性的な製品

Akt製品

All (32) Akt阻害剤(27) Akt活性剤(2) Aktモジュレータ(1) Akt化学物質(2) 新Akt製品

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1078	MK-2206 2HCl MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.	Genes Dev, 2020, 10.1101/gad.332494.119 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2485 Mol Syst Biol, 2020, 16(2):e8664	VE-cadherin-induced Akt activation mediates YAP phosphorylation and translocation in ECs. HUVECs were starved for 1h and treated with thrombin (1U) for 1h. Total cell lysates were probed with anti-pAkt, Akt or b-actin antibody. The representative blots of three independent experiments are depicted, and the normalized values for p-Akt are shown. HUVECs were cultured and starved as described as in d and incubated for 8h in complete medium with the Akt inhibitor, MK-2206 (1 uM). pAkt, Akt, pYAP and YAP were detected by western blotting using specific antibodies.
S1037	Perifosine (KRX-0401) Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.	J Cell Biochem, 2020, 121(1):723-734 Transl Oncol, 2020, 13(2):355-364 Chin J Integr Med, 2020, 10.1007	Tumor growth of 827 GSC-derived xenografts treated with an AKT inhibitor perifosine (30 mg/kg body weight). Twenty-three days after tumor implantation in mice, perifosine was administered by intraperitoneal injection (daily for 5 days). Error bars represent SD. Five mice per group, *p < 0.01.
S1113	GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.	Biomaterials, 2020, 239:119839 Cell Cycle, 2020, 19(1):53-66 Cell, 2019, 176(6):1379-1392	UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
S2808	GDC-0068 Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.	Eur J Med Chem, 2020, 189:112076 Cancer Discov, 2019, 10.1158/2159-8290.CD-18-0830 Nat Commun, 2019, 10(1):2532	Inhibition of AKT signaling abolishes MKK4 phosphorylation on Ser78 in injured axons. Cultures of sensory neurons were treated with 5 µM MK-2206 or 5 µM GDC-0068 for 1 hr prior to axotomy. Axonal proteins harvested at indicated time points after axotomy were subjected to immunoblot analysis.
S8019	AZD5363 AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.	Cells, 2020, 9(3) FASEB Bioadv, 2020, 2(2):126-144 Cancer Res, 2019, 79(9):2367-2378	Inhibition of PI3K and Akt by LY294002 and AZD5363 was confirmed by analyzing expression and activation status of the ribosomal protein S6 by Western blot analysis of PC-3 clone #14 cells treated with 0.5 or 5 uM AZD5363 (AZD) and 10 uM LY294002 (LY). Tubulin was used as a loading control.
S8500^新	BAY1125976 BAY 1125976 is a selective allosteric AKT1/2 inhibitor,exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY1125976 inhibits the activity of AKT1 (IC50 = 5.2 nM at 10 µM ATP and 44 nM at 2 mM ATP) and AKT2 (IC50 = 18 nM at 10 µM ATP and 36 nM at 2 mM ATP) very potently.Whereas BAY1125976 is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP).
S8839^新	Borussertib Borussertib is a covalent-allosteric inhibitor of protein kinase Akt with an IC50 of 0.8 nM and a Ki of 2.2 nM for WT Akt.
S2743	PF-04691502 PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with K_i of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.	Cancer Biol Med, 2019, 16(2):264-275 PLoS One, 2018, 13(8):e0200725 Onco Targets , 2018, 11:943-953	BMDMs from WT animals were treated with different concentrations of PI3K inhibitors (500 nmol/L PF4691502, PI-103, BKM120 and 25 μmol/L SF1126) followed by hypoxia for 4 hours for Western blots. These macrophages were either used for lysate preparation (nuclear extracts for HIFα or WCE for pAKT and AKT) and Western blot analysis.
S1558	AT7867 AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM in cell-free assays, respectively; little activity outside the AGC kinase family.	FEBS J, 2019, 10.1111/febs.15112 FEBS Lett, 2019, 593(2):175-186 PLoS One, 2019, 14(6):e0218537	UMUC-6 cells were treated with the indicated concentrations of AT7867 for 72 hours. Relative cytotoxicity compared to untreated control cells was assessed by alamarBlue. Each data points represents the mean of three independent experiments and the error bars represent the standard error of the mean.
S1117	Triciribine Triciribine is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.	Biol Pharm Bull, 2020, 10.1248 Front Endocrinol (Lausanne), 2020, 10:915 Neuron, 2019, 101(1):32-44	Effect of triciribine on the migration of (A) FaDu and (B) Hep2 cells. The cells were treated with 5 µM triciribine for different periods of time. *P<0.05 vs. control. Hpf, high-power field.
S2635	CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.	Sci Transl Med, 2019, 11(501) Cancers (Basel), 2019, 11(8) Cell Death Dis, 2019, 9(10):1013	PI3K/AKT were involved in the E2 induced decrease of Caov-3 cell anoikis. Caov-3 cells were pretreated by different signaling pathway inhibitors and Bit1 expression was determined by western blotting.
S2670	A-674563 A-674563 is an Akt1 inhibitor with K_i of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.	Biomolecules, 2020, 10(2) J Immunother Cancer, 2019, 7(1):33 Cell Death Dis, 2019, 9(10):1013	B cells were pre-treated with the indicated concentrations of A-674563 for 1h prior to R848 treatment (500 ng/ml). Thymidine incorporation was analyzed 24h later.
S1556	PHT-427 PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with K_i of 2.7 μM and 5.2 μM, respectively.	Mol Syst Biol, 2020, 16(2):e8664 FEBS J, 2019, 10.1111/febs.15112 FEBS Lett, 2019, 593(2):175-186	The inhibition of PI3K/Akt pathway is involved in ATG-induced FOXO3a dephosphorylation in PDGF-BB-activated HSCs. Serum-starved LX-2 human HSCs were pretreated with or without DMSO (vehicle) or ATG (0.5 uM) for 4 h, in the absence or presence of PI3K inhibitor LY294002 (20 uM) or Akt inhibitor PHT-427 (20 uM), and then incubated with or without 50 ng/ml PDGF-BB for 4 h. After treatment, aliquots of whole cell lysates were collected and subjected to Western blotting analysis. The experiments were repeated three times with similar results and a representative blot was shown for each protein. Total protein levels of Akt and FOXO3a served as internal controls.
S3056	Miltefosine Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.	J Clin Med, 2019, 8(6) mBio, 2018, 9(5) Antimicrob Agents Chemother, 2015, 59(2):1088-99	Effects of a miltefosine co-treatment with celecoxib on steatohepatitis, hepatocyte apoptosis, Akt activation and p53 expression in the liver of MCD-diet fed mice. Mice were fed the control diet, an MCD diet, an MCD diet with celecoxib (20 mg/kg/day) treatment, or an MCD diet co-treatment with celecoxib and miltefosine (50 mg/kg/day) for 3 weeks. (C) TUNEL-stained sections of liver samples are representative of the indicated groups (magnification×400). Abbreviations: MCD, methionine and choline deficient; CON, control; CEL, celecoxib; MTF, miltefosine.
S2310	Honokiol Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.	Antioxidants (Basel), 2019, 8(10) Int J Mol Med, 2019, 44(1):227-239 Front Pharmacol, 2018, 9:357	(B) Cleaved PARP, Bax and Bcl2 protein expression was evaluated by immunoblotting of KRAS mutant cells lysates after 48 h of honokiol (10, 20, 40, and 60 μM) treatment. ∗∗P < 0.01 and ∗∗∗P < 0.001 for comparison between control group and honokiol-treated group.
S7127	TIC10 Analogue TIC10 Analogue is an analogue of TIC10, which inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
S7492	Uprosertib (GSK2141795) Uprosertib (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.	Br J Cancer, 2020, 10.1038/s41416-020-0777-y Stem Cell Res Ther, 2019, 10(1):345 Toxicol Appl Pharmacol, 2019, 381:114729	Parental cell line wastreated with Akt inhibitor (GSK2141795) and BGJ398. The 5 uM BGJ398 resistant cell line was treated with GSK2141795, BGJ398, and 2 concentrations of GSK2141795 and varying dosages of BGJ398. The parental cell line treated with GSK2141795, the dark green line, indicates minimal effect of the inhibitor compared to the resistant cell line treated GSK2141795, the light purple line. However, when the resistant cell line is treated with both GSK2141795 and BGJ398 there is a greater decrease in cell viability compared to the resistant cell line that is treated only with GSK2141795.
S7963	TIC10 TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.	Eur J Pharmacol, 2019, 857:172423 J Cancer, 2018, 9(8):1486-1499 Oncotarget, 2017, 8(9):15775-15788	Established HCC cell lines, HepG2 (A-C) and Huh-7 (D), primary human HCC cells (D, "Pri_1/Pri _2"), as well as HL-7702 human hepatocytes (D) and primary human adult hepatocytes ("Hepatocytes", D), were either left untreated ("C", same for all figures), or treated with applied concentration of TIC10 (0.1-30 μM), cells were then cultured in conditional medium for applied time; Cell proliferation was tested by MTT assay (A and D), clonogenicity assay (B) and [H3] Thymidine incorporation assay (C). Experiments in this figure were repeated for five times, with similar results obtained. n = 5 for each repeat. Bars stand for mean ± SD. *p < 0.05 vs. group "C".
S7776	Akti-1/2 Akti-1/2 is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3.	Int J Cancer, 2019, 145(6):1690-1700 Xenotransplantation, 2019, doi: 10 Nat Immunol, 2019, 20(1):10-17	AKTi-1/2 inhibits human HCC cells in vitro. Human HCC HepG2 cells (A–F), Huh-7 cells (G), primary human HCC cells (“Pri HCC”, G) or the primary liver cells (“Pri liver cells”, G) were treated with/out applied concentrations of AKTi-1/2 for indicated time; Cell survival (A, B and G), proliferation (C and D) and apoptosis (E and F) were tested by the listed assays. Data were shown as the mean (n = 5) with the standard deviation (SD). Experiments in this figure were repeated three times, with similar results were obtained. *P < 0.05 vs. “C” (untreated control) group.
S5313	SC66 SC66 is an allosteric inhibitor which displays a dual-inhibitory function toward AKT activity with IC50 values of 0.77, 2.85 and 0.47 μg/ml in HepG2, Huh7 and Hep3B cells after 72 h treatment, respectively.	Cancers (Basel), 2019, 11(9) Sci Rep, 2019, 9(1):10933 Cancer Cell Int, 2019, 19:124
S4953	Usnic acid Usnic acid is a furandione found uniquely in lichen that is used widely in cosmetics, deodorants, toothpaste and medicinal creams as well as some herbal products. It exhibits antiviral, antiprotozoal, antiproliferative, anti-inflammatory and analgesic activity.
S8339	Miransertib (ARQ 092) HCl ARQ 092 is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors.	Cancer Res, 2019, 79(9):2367-2378 Toxicol Appl Pharmacol, 2019, 381:114729 PLoS One, 2019, 14(6):e0218537	ARQ-092, a novel pan-AKT inhibitor, promotes axonal recovery when applied pre- and post-OGD. ARQ-092, which is an inhibitor of activated AKT, promoted axon function recovery when applied as a pre-treatment and as a post-treatment. A) Pre-treatment with ARQ-092 (500 nM, dark blue) applied before OGD promoted consistent and sustained CAP area recovery. B) ARQ-092 improved CAP area recovery at 250 nM and 500 nM when compared to control CAP area recovery. C) ARQ-092 (500 nM, brown) applied after OGD promoted consistent and sustained CAP area recovery. D) ARQ-092 improved CAP area recovery at 250 and 500 nM compared to control CAP area recovery. p < 0.05 and *p < 0.01, one-way ANOVA with Newman-Keuls post hoc test. (For interpretation of the references to color in this figure legend, the reader is referred to the web version of this article.)
S7521	Afuresertib (GSK2110183) Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with K_i of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.	Nat Commun, 2019, 10(1):95 Toxicol Appl Pharmacol, 2019, 381:114729 J Clin Invest, 2018, 128(10):4604-4621	Analysis of the mechanism of action of the enhanced anti‑tumor effect of the combination therapy of suboptimal doses of pomalidomide plus dexamethasone and afuresertib in MM cells. (A‑C) The altered expression of protein substrates was analyzed in two MM cell lines that were treated with suboptimal doses of PD, or AFU, or the PD and AFU combination. The XG‑7 and U266 cell lines were subjected to the indicated treatments for 48 and 72 h, respectively. (A) Caspases, (B) substrates related mainly to the working mechanism of IMiDs, (C) substrates mainly related to the working mechanism of afuresertib, and (D) two primary MM cell cultures, were subjected to the analysis in the same manner as the two MM cell lines. In the expression panel of p‑FoxO3a/FoxO1, the upper band represents p‑FoxO3a and the lower band represents p‑FOXO1. PD, pomalidomide plus dexamethasone; AFU, Afuresertib; MM, multiple myeloma; IMiDs, immunomodulatory drugs.
S9315	Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. It is reported to induce apoptosis in human multidrug resistant (MDR) KB-V1 cells.
S3810	Scutellarin Scutellarin, the major active principal flavonoids extracted from the Chinese herbal medicines Scutellaria baicalensis and Erigeron breviscapus (Vant.) Hand-Mazz, has many pharmacological effects, such as antioxidant, antitumor, antiviral, and antiinflammatory activities.
S7563	AT13148 AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.	Nat Cell Biol, 2019, 21(6):778-790 Cancer Sci, 2016, 107(11):1563-1571 Biochem Biophys Res Commun, 2016, 478(1):330-6	AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
S8132	Deguelin Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.	Cell Death Dis, 2020, 11(2):143
S6760^新	LM22B-10 LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator, LM22B-10 selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro.
S7863	SC79 SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.	Biochem Biophys Res Commun, 2020, 522(2):518-524 J Hematol Oncol, 2020, 13(1):11 BMC Complement Med Ther, 2020, 20(1):13	Cells with OGN over-expression were challenged with EGF (100 ng/mL) and pretreated with SC79 (constitutive Akt activator) for 24 h. Western blotting with the significantly altered markers was performed.
S9514	Rotundic acid Rotundic acid, a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.
S9190	Oroxin B Oroxin B, one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment.
S2323	Methyl-Hesperidin Methyl Hesperidin is a flavanone glycoside (flavonoid) (C28H34O15) found abundantly in citrus fruits. Its aglycone form is called hesperetin.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1078	MK-2206 2HCl MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.	Genes Dev, 2020, 10.1101/gad.332494.119 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2485 Mol Syst Biol, 2020, 16(2):e8664	VE-cadherin-induced Akt activation mediates YAP phosphorylation and translocation in ECs. HUVECs were starved for 1h and treated with thrombin (1U) for 1h. Total cell lysates were probed with anti-pAkt, Akt or b-actin antibody. The representative blots of three independent experiments are depicted, and the normalized values for p-Akt are shown. HUVECs were cultured and starved as described as in d and incubated for 8h in complete medium with the Akt inhibitor, MK-2206 (1 uM). pAkt, Akt, pYAP and YAP were detected by western blotting using specific antibodies.
S1037	Perifosine (KRX-0401) Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.	J Cell Biochem, 2020, 121(1):723-734 Transl Oncol, 2020, 13(2):355-364 Chin J Integr Med, 2020, 10.1007	Tumor growth of 827 GSC-derived xenografts treated with an AKT inhibitor perifosine (30 mg/kg body weight). Twenty-three days after tumor implantation in mice, perifosine was administered by intraperitoneal injection (daily for 5 days). Error bars represent SD. Five mice per group, *p < 0.01.
S1113	GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.	Biomaterials, 2020, 239:119839 Cell Cycle, 2020, 19(1):53-66 Cell, 2019, 176(6):1379-1392	UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
S2808	GDC-0068 Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.	Eur J Med Chem, 2020, 189:112076 Cancer Discov, 2019, 10.1158/2159-8290.CD-18-0830 Nat Commun, 2019, 10(1):2532	Inhibition of AKT signaling abolishes MKK4 phosphorylation on Ser78 in injured axons. Cultures of sensory neurons were treated with 5 µM MK-2206 or 5 µM GDC-0068 for 1 hr prior to axotomy. Axonal proteins harvested at indicated time points after axotomy were subjected to immunoblot analysis.
S8019	AZD5363 AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.	Cells, 2020, 9(3) FASEB Bioadv, 2020, 2(2):126-144 Cancer Res, 2019, 79(9):2367-2378	Inhibition of PI3K and Akt by LY294002 and AZD5363 was confirmed by analyzing expression and activation status of the ribosomal protein S6 by Western blot analysis of PC-3 clone #14 cells treated with 0.5 or 5 uM AZD5363 (AZD) and 10 uM LY294002 (LY). Tubulin was used as a loading control.
S8500^新	BAY1125976 BAY 1125976 is a selective allosteric AKT1/2 inhibitor,exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY1125976 inhibits the activity of AKT1 (IC50 = 5.2 nM at 10 µM ATP and 44 nM at 2 mM ATP) and AKT2 (IC50 = 18 nM at 10 µM ATP and 36 nM at 2 mM ATP) very potently.Whereas BAY1125976 is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP).
S8839^新	Borussertib Borussertib is a covalent-allosteric inhibitor of protein kinase Akt with an IC50 of 0.8 nM and a Ki of 2.2 nM for WT Akt.
S2743	PF-04691502 PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with K_i of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.	Cancer Biol Med, 2019, 16(2):264-275 PLoS One, 2018, 13(8):e0200725 Onco Targets , 2018, 11:943-953	BMDMs from WT animals were treated with different concentrations of PI3K inhibitors (500 nmol/L PF4691502, PI-103, BKM120 and 25 μmol/L SF1126) followed by hypoxia for 4 hours for Western blots. These macrophages were either used for lysate preparation (nuclear extracts for HIFα or WCE for pAKT and AKT) and Western blot analysis.
S1558	AT7867 AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM in cell-free assays, respectively; little activity outside the AGC kinase family.	FEBS J, 2019, 10.1111/febs.15112 FEBS Lett, 2019, 593(2):175-186 PLoS One, 2019, 14(6):e0218537	UMUC-6 cells were treated with the indicated concentrations of AT7867 for 72 hours. Relative cytotoxicity compared to untreated control cells was assessed by alamarBlue. Each data points represents the mean of three independent experiments and the error bars represent the standard error of the mean.
S1117	Triciribine Triciribine is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.	Biol Pharm Bull, 2020, 10.1248 Front Endocrinol (Lausanne), 2020, 10:915 Neuron, 2019, 101(1):32-44	Effect of triciribine on the migration of (A) FaDu and (B) Hep2 cells. The cells were treated with 5 µM triciribine for different periods of time. *P<0.05 vs. control. Hpf, high-power field.
S2635	CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.	Sci Transl Med, 2019, 11(501) Cancers (Basel), 2019, 11(8) Cell Death Dis, 2019, 9(10):1013	PI3K/AKT were involved in the E2 induced decrease of Caov-3 cell anoikis. Caov-3 cells were pretreated by different signaling pathway inhibitors and Bit1 expression was determined by western blotting.
S2670	A-674563 A-674563 is an Akt1 inhibitor with K_i of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.	Biomolecules, 2020, 10(2) J Immunother Cancer, 2019, 7(1):33 Cell Death Dis, 2019, 9(10):1013	B cells were pre-treated with the indicated concentrations of A-674563 for 1h prior to R848 treatment (500 ng/ml). Thymidine incorporation was analyzed 24h later.
S1556	PHT-427 PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with K_i of 2.7 μM and 5.2 μM, respectively.	Mol Syst Biol, 2020, 16(2):e8664 FEBS J, 2019, 10.1111/febs.15112 FEBS Lett, 2019, 593(2):175-186	The inhibition of PI3K/Akt pathway is involved in ATG-induced FOXO3a dephosphorylation in PDGF-BB-activated HSCs. Serum-starved LX-2 human HSCs were pretreated with or without DMSO (vehicle) or ATG (0.5 uM) for 4 h, in the absence or presence of PI3K inhibitor LY294002 (20 uM) or Akt inhibitor PHT-427 (20 uM), and then incubated with or without 50 ng/ml PDGF-BB for 4 h. After treatment, aliquots of whole cell lysates were collected and subjected to Western blotting analysis. The experiments were repeated three times with similar results and a representative blot was shown for each protein. Total protein levels of Akt and FOXO3a served as internal controls.
S3056	Miltefosine Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.	J Clin Med, 2019, 8(6) mBio, 2018, 9(5) Antimicrob Agents Chemother, 2015, 59(2):1088-99	Effects of a miltefosine co-treatment with celecoxib on steatohepatitis, hepatocyte apoptosis, Akt activation and p53 expression in the liver of MCD-diet fed mice. Mice were fed the control diet, an MCD diet, an MCD diet with celecoxib (20 mg/kg/day) treatment, or an MCD diet co-treatment with celecoxib and miltefosine (50 mg/kg/day) for 3 weeks. (C) TUNEL-stained sections of liver samples are representative of the indicated groups (magnification×400). Abbreviations: MCD, methionine and choline deficient; CON, control; CEL, celecoxib; MTF, miltefosine.
S2310	Honokiol Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.	Antioxidants (Basel), 2019, 8(10) Int J Mol Med, 2019, 44(1):227-239 Front Pharmacol, 2018, 9:357	(B) Cleaved PARP, Bax and Bcl2 protein expression was evaluated by immunoblotting of KRAS mutant cells lysates after 48 h of honokiol (10, 20, 40, and 60 μM) treatment. ∗∗P < 0.01 and ∗∗∗P < 0.001 for comparison between control group and honokiol-treated group.
S7127	TIC10 Analogue TIC10 Analogue is an analogue of TIC10, which inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
S7492	Uprosertib (GSK2141795) Uprosertib (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.	Br J Cancer, 2020, 10.1038/s41416-020-0777-y Stem Cell Res Ther, 2019, 10(1):345 Toxicol Appl Pharmacol, 2019, 381:114729	Parental cell line wastreated with Akt inhibitor (GSK2141795) and BGJ398. The 5 uM BGJ398 resistant cell line was treated with GSK2141795, BGJ398, and 2 concentrations of GSK2141795 and varying dosages of BGJ398. The parental cell line treated with GSK2141795, the dark green line, indicates minimal effect of the inhibitor compared to the resistant cell line treated GSK2141795, the light purple line. However, when the resistant cell line is treated with both GSK2141795 and BGJ398 there is a greater decrease in cell viability compared to the resistant cell line that is treated only with GSK2141795.
S7963	TIC10 TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.	Eur J Pharmacol, 2019, 857:172423 J Cancer, 2018, 9(8):1486-1499 Oncotarget, 2017, 8(9):15775-15788	Established HCC cell lines, HepG2 (A-C) and Huh-7 (D), primary human HCC cells (D, "Pri_1/Pri _2"), as well as HL-7702 human hepatocytes (D) and primary human adult hepatocytes ("Hepatocytes", D), were either left untreated ("C", same for all figures), or treated with applied concentration of TIC10 (0.1-30 μM), cells were then cultured in conditional medium for applied time; Cell proliferation was tested by MTT assay (A and D), clonogenicity assay (B) and [H3] Thymidine incorporation assay (C). Experiments in this figure were repeated for five times, with similar results obtained. n = 5 for each repeat. Bars stand for mean ± SD. *p < 0.05 vs. group "C".
S7776	Akti-1/2 Akti-1/2 is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3.	Int J Cancer, 2019, 145(6):1690-1700 Xenotransplantation, 2019, doi: 10 Nat Immunol, 2019, 20(1):10-17	AKTi-1/2 inhibits human HCC cells in vitro. Human HCC HepG2 cells (A–F), Huh-7 cells (G), primary human HCC cells (“Pri HCC”, G) or the primary liver cells (“Pri liver cells”, G) were treated with/out applied concentrations of AKTi-1/2 for indicated time; Cell survival (A, B and G), proliferation (C and D) and apoptosis (E and F) were tested by the listed assays. Data were shown as the mean (n = 5) with the standard deviation (SD). Experiments in this figure were repeated three times, with similar results were obtained. *P < 0.05 vs. “C” (untreated control) group.
S5313	SC66 SC66 is an allosteric inhibitor which displays a dual-inhibitory function toward AKT activity with IC50 values of 0.77, 2.85 and 0.47 μg/ml in HepG2, Huh7 and Hep3B cells after 72 h treatment, respectively.	Cancers (Basel), 2019, 11(9) Sci Rep, 2019, 9(1):10933 Cancer Cell Int, 2019, 19:124
S4953	Usnic acid Usnic acid is a furandione found uniquely in lichen that is used widely in cosmetics, deodorants, toothpaste and medicinal creams as well as some herbal products. It exhibits antiviral, antiprotozoal, antiproliferative, anti-inflammatory and analgesic activity.
S8339	Miransertib (ARQ 092) HCl ARQ 092 is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors.	Cancer Res, 2019, 79(9):2367-2378 Toxicol Appl Pharmacol, 2019, 381:114729 PLoS One, 2019, 14(6):e0218537	ARQ-092, a novel pan-AKT inhibitor, promotes axonal recovery when applied pre- and post-OGD. ARQ-092, which is an inhibitor of activated AKT, promoted axon function recovery when applied as a pre-treatment and as a post-treatment. A) Pre-treatment with ARQ-092 (500 nM, dark blue) applied before OGD promoted consistent and sustained CAP area recovery. B) ARQ-092 improved CAP area recovery at 250 nM and 500 nM when compared to control CAP area recovery. C) ARQ-092 (500 nM, brown) applied after OGD promoted consistent and sustained CAP area recovery. D) ARQ-092 improved CAP area recovery at 250 and 500 nM compared to control CAP area recovery. p < 0.05 and *p < 0.01, one-way ANOVA with Newman-Keuls post hoc test. (For interpretation of the references to color in this figure legend, the reader is referred to the web version of this article.)
S7521	Afuresertib (GSK2110183) Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with K_i of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.	Nat Commun, 2019, 10(1):95 Toxicol Appl Pharmacol, 2019, 381:114729 J Clin Invest, 2018, 128(10):4604-4621	Analysis of the mechanism of action of the enhanced anti‑tumor effect of the combination therapy of suboptimal doses of pomalidomide plus dexamethasone and afuresertib in MM cells. (A‑C) The altered expression of protein substrates was analyzed in two MM cell lines that were treated with suboptimal doses of PD, or AFU, or the PD and AFU combination. The XG‑7 and U266 cell lines were subjected to the indicated treatments for 48 and 72 h, respectively. (A) Caspases, (B) substrates related mainly to the working mechanism of IMiDs, (C) substrates mainly related to the working mechanism of afuresertib, and (D) two primary MM cell cultures, were subjected to the analysis in the same manner as the two MM cell lines. In the expression panel of p‑FoxO3a/FoxO1, the upper band represents p‑FoxO3a and the lower band represents p‑FOXO1. PD, pomalidomide plus dexamethasone; AFU, Afuresertib; MM, multiple myeloma; IMiDs, immunomodulatory drugs.
S9315	Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. It is reported to induce apoptosis in human multidrug resistant (MDR) KB-V1 cells.
S3810	Scutellarin Scutellarin, the major active principal flavonoids extracted from the Chinese herbal medicines Scutellaria baicalensis and Erigeron breviscapus (Vant.) Hand-Mazz, has many pharmacological effects, such as antioxidant, antitumor, antiviral, and antiinflammatory activities.
S7563	AT13148 AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.	Nat Cell Biol, 2019, 21(6):778-790 Cancer Sci, 2016, 107(11):1563-1571 Biochem Biophys Res Commun, 2016, 478(1):330-6	AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
S8132	Deguelin Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.	Cell Death Dis, 2020, 11(2):143

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S6760^新	LM22B-10 LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator, LM22B-10 selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro.
S7863	SC79 SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.	Biochem Biophys Res Commun, 2020, 522(2):518-524 J Hematol Oncol, 2020, 13(1):11 BMC Complement Med Ther, 2020, 20(1):13	Cells with OGN over-expression were challenged with EGF (100 ng/mL) and pretreated with SC79 (constitutive Akt activator) for 24 h. Western blotting with the significantly altered markers was performed.

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S6760^新

LM22B-10

LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator, LM22B-10 selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro.

S7863

SC79

SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.

Biochem Biophys Res Commun, 2020, 522(2):518-524

J Hematol Oncol, 2020, 13(1):11

BMC Complement Med Ther, 2020, 20(1):13

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S9514	Rotundic acid Rotundic acid, a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.

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S9514

Rotundic acid, a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.

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S9190	Oroxin B Oroxin B, one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment.
S2323	Methyl-Hesperidin Methyl Hesperidin is a flavanone glycoside (flavonoid) (C28H34O15) found abundantly in citrus fruits. Its aglycone form is called hesperetin.

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S9190

Oroxin B

Oroxin B, one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment.

S2323

Methyl-Hesperidin

Methyl Hesperidin is a flavanone glycoside (flavonoid) (C28H34O15) found abundantly in citrus fruits. Its aglycone form is called hesperetin.

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