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
S1362	Rigosertib (ON-01910)	95 mg/mL	95 mg/mL	'<1 mg/mL
S2808	Ipatasertib (GDC-0068)	<1 mg/mL	92 mg/mL	92 mg/mL
S3296	Hispidulin	-1 mg/mL	100 mg/mL	'''-1 mg/mL
S3220	Trigonelline	-1 mg/mL	50 mg/mL	''-1 mg/mL
S3241	Loureirin A	-1 mg/mL	100 mg/mL	''-1 mg/mL
S6847	ML-9 HCl	10 mg/mL	72 mg/mL	'''6 mg/mL
S6885	Ailanthone	-1 mg/mL	100 mg/mL	'-1 mg/mL
S6811	Miransertib (ARQ-092)	<1 mg/mL	8 mg/mL	''''<1 mg/mL
S9611	ABTL-0812			' mg/mL
S8961	Alobresib (GS-5829)	˂1 mg/mL	87 mg/mL	'''11 mg/mL
S8500	BAY1125976	<1 mg/mL	11 mg/mL	<1 mg/mL
S8839	Borussertib	<1 mg/mL	100 mg/mL	<1 mg/mL
S8019	Capivasertib (AZD5363)	<1 mg/mL	86 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
S9190	Oroxin B	-1 mg/mL	100 mg/mL	-1 mg/mL
S7492	Uprosertib (GSK2141795)	<1 mg/mL	85 mg/mL	85 mg/mL
S7963	TIC10 (ONC201)	<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
S3785	Notoginsenoside R1	-1 mg/mL	100 mg/mL	-1 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
S2335	Oridonin	<1 mg/mL	72 mg/mL	28 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
S3224	Cinobufagin	-1 mg/mL	100 mg/mL	''-1 mg/mL
S3238	Resibufogenin	-1 mg/mL	100 mg/mL	'''-1 mg/mL
S3289	Daphnoretin	-1 mg/mL	100 mg/mL	'''-1 mg/mL
S6760	LM22B-10	<1 mg/mL	97 mg/mL	''97 mg/mL
S7863	SC79	<1 mg/mL	72 mg/mL	72 mg/mL
S3294	Demethyl-Coclaurine	-1 mg/mL	100 mg/mL	''-1 mg/mL
S9514	Rotundic acid	-1 mg/mL	98 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 (47) Akt阻害剤(39) Akt活性剤(5) Akt作動薬(1) Aktモジュレータ(1)

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. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.	Cell, 2020, 25;181(7):1596-1611.e27. Cell, 2020, 182(3):685-712.e19 Cell Stem Cell, 2020, 27(1):50-63.e5	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, NSC639966) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.	Aging (Albany NY), 2020, 18;12(10):9489-9499 Cancer Cell Int, 2020, 25;20:134 J Cell Biochem, 2020, 121(1):723-734	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. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.	Cell, 2020, 25;181(7):1596-1611.e27. J Clin Invest, 2020, 1;130(5):2422-2434 Biomaterials, 2020, 239:119839	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.
S1362	Rigosertib (ON-01910) Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.	Mol Cell, 2020, 79(1):191-198.e3 Biology (Basel), 2020, 15;9(5):E99 Nature, 2019, 10.1038/s41586-019-1607-3	Along with cell death, immunoblotting shows ON 01910.Na induces hyperphosphorylation of RanGAP1, increased expression of RanGAP1.SUMO1 but decreased expression of free unmodified RanGAP1. No viable SU-DHL-5 cells were available for immunoblotting at 0.5 uM of ON 01910.Na.
S2808	Ipatasertib (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.	Nature, 2020, 583(7817):620-624 Cell, 2020, 182(3):685-712.e19 Nat Commun, 2020, 8;11(1):2291	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.
S3296^新	Hispidulin Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.
S3220^新	Trigonelline Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells.
S3241^新	Loureirin A Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation.
S6847^新	ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.
S6885^新	Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
S6811^新	Miransertib (ARQ-092) Miransertib (ARQ-092) is a potent, selective and orally bioavailable allosteric inhibitor of Akt with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.	Int J Biol Sci, 2020, 16(14):2559-2579
S9611^新	ABTL-0812 ABTL0812 (α-Hydroxylinoleic acid, LP-10218, SCLN-0812) inhibits Akt/mTOR axis by inducing the overexpression of TRIB3 and activating autophagy in lung squamous carcinoma cell lines. ABTL0812 also induces AMPK activation and ROS accumulation.
S8961^新	Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
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.
S8019	Capivasertib (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.	Nature, 2020, 583(7817):620-624 Cell, 2020, 182(3):685-712.e19 Genome Med, 2020, 18;12(1):17	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.
S2743	PF-04691502 PF-04691502 (PF4691502) 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. PF-04691502 induces apoptosis. Phase 2.	Mol Cancer, 2019, Cancer Biol Med, 2019, 16(2):264-275 PLoS One, 2018, 13(8):e0200725	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 (NSC 154020, VD-0002, vqd-002, API-2) 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.	Cell Oncol (Dordr), 2020, 8 Int J Biol Sci, 2020, 16(13):2382-2391 Biol Pharm Bull, 2020, 10.1248	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. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.	Biomed Pharmacother, 2020, 130:110544 Sci Transl Med, 2019, 11(501) Cancers (Basel), 2019, 11(8)	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.	Sci Signal, 2020, 13(619) Cancers (Basel), 2020, 12(9)E2668 Biomolecules, 2020, 10(2)	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 (CS-0223) 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.	Cell Oncol (Dordr), 2020, 8 J Clin Med, 2019, 8(6) mBio, 2018, 9(5)	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. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.	Cancers (Basel), 2020, 12(7):E1782 Int J Nanomedicine, 2020, 15:17-29 Radiat Environ Biophys, 2020,	(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.
S9190	Oroxin B Oroxin B (Hypocretin-2), 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.
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 Cell Oncol (Dordr), 2020, 8 Sci Rep, 2020, 10(1):12644	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 (ONC201) TIC10 (ONC201) inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.	ACS Chem Biol, 2019, 14(5):1020-1029 Eur J Pharmacol, 2019, 857:172423 J Cancer, 2018, 9(8):1486-1499	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. Akti-1/2 induces apoptosis.	J Cell Physiol, 2020, 235(2):1051-1064 Mol Ther Oncolytics, 2020, 18:282-294 Int J Cancer, 2019, 145(6):1690-1700	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.	Oncol Lett, 2020, Cancers (Basel), 2019, 11(9) Sci Rep, 2019, 9(1):10933
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. Usnic acid inhibits breast tumor angiogenesis and growth by suppressing VEGFR2-mediated AKT and ERK1/2 signaling pathways.
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.	Dev Dyn, 2020, 10.1002/dvdy.231 Int J Biol Sci, 2020, 16(14):2559-2579 Cancer Res, 2019, 79(9):2367-2378	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.)
S3785	Notoginsenoside R1 Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways.
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, 2020, 11(1):4629 Cell Oncol (Dordr), 2020, 8 Cancer Sci, 2020, 111(5):1663-1675	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. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S2335	Oridonin Oridonin (Isodonol, Rubescenin, NSC-250682), a diterpenoid purified from Rabdosia rubescens, is a traditional agent with antitumor, anti-bacterial and anti-inflammatory effects. Oridonin inhibits AKT1 and AKT2 kinase activity with IC50 of 8.4 μM and 8.9 μM, respectively.	Protein Sci, 2020, 29(6):1366-1372 Mediators Inflamm, 2019, 2019:7634761 Biochem Biophys Res Commun, 2019, 513(3):594-601	Histopathological analysis of H460 tumors following combination treatment with oridonin and radiation. Hematoxylin and eosin (H-E) staining and immunohistochemistry for cleaved caspase-3 and γ-H2AX were performed on tumors harvested at 14 days after IR. Representative images of H-E-stained tumors (upper images) and cleaved caspase-3- and γ-H2AX-positive cells (middle images, brown staining) and quantification of cleaved caspase-3 and γ-H2AX-positive staining with six mice in each group (lower plots, means ± SEM) are shown; * p < 0.05.
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. Scutellarin can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.
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.	Cell, 2020, 182(3):685-712.e19 Cancer Cell, 2020, 37(1):85-103 Nat Cell Biol, 2019, 21(6):778-790	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
S3224^新	Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238^新	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S3289^新	Daphnoretin Daphnoretin (Dephnoretin, Thymelol), a biologically active compound isolated from Wikstroemia indica C.A. Mey., is a protein kinase C (PKC) activator. Daphnoretin inhibits the proliferation, invasion, and migration of tumor cells and promote its apoptosis by regulating the activity of Akt signal pathway.
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.	Proc Natl Acad Sci U S A, 2020, 117(40):25104-25115 Biomaterials, 2020, 237:119793 Cell Rep, 2020, 30(5):1400-1416	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.
S3294^新	Demethyl-Coclaurine Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
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.
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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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. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.	Cell, 2020, 25;181(7):1596-1611.e27. Cell, 2020, 182(3):685-712.e19 Cell Stem Cell, 2020, 27(1):50-63.e5	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, NSC639966) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.	Aging (Albany NY), 2020, 18;12(10):9489-9499 Cancer Cell Int, 2020, 25;20:134 J Cell Biochem, 2020, 121(1):723-734	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. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.	Cell, 2020, 25;181(7):1596-1611.e27. J Clin Invest, 2020, 1;130(5):2422-2434 Biomaterials, 2020, 239:119839	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.
S1362	Rigosertib (ON-01910) Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.	Mol Cell, 2020, 79(1):191-198.e3 Biology (Basel), 2020, 15;9(5):E99 Nature, 2019, 10.1038/s41586-019-1607-3	Along with cell death, immunoblotting shows ON 01910.Na induces hyperphosphorylation of RanGAP1, increased expression of RanGAP1.SUMO1 but decreased expression of free unmodified RanGAP1. No viable SU-DHL-5 cells were available for immunoblotting at 0.5 uM of ON 01910.Na.
S2808	Ipatasertib (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.	Nature, 2020, 583(7817):620-624 Cell, 2020, 182(3):685-712.e19 Nat Commun, 2020, 8;11(1):2291	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.
S3296^新	Hispidulin Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.
S3220^新	Trigonelline Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells.
S3241^新	Loureirin A Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation.
S6847^新	ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.
S6885^新	Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
S6811^新	Miransertib (ARQ-092) Miransertib (ARQ-092) is a potent, selective and orally bioavailable allosteric inhibitor of Akt with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.	Int J Biol Sci, 2020, 16(14):2559-2579
S9611^新	ABTL-0812 ABTL0812 (α-Hydroxylinoleic acid, LP-10218, SCLN-0812) inhibits Akt/mTOR axis by inducing the overexpression of TRIB3 and activating autophagy in lung squamous carcinoma cell lines. ABTL0812 also induces AMPK activation and ROS accumulation.
S8961^新	Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
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.
S8019	Capivasertib (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.	Nature, 2020, 583(7817):620-624 Cell, 2020, 182(3):685-712.e19 Genome Med, 2020, 18;12(1):17	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.
S2743	PF-04691502 PF-04691502 (PF4691502) 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. PF-04691502 induces apoptosis. Phase 2.	Mol Cancer, 2019, Cancer Biol Med, 2019, 16(2):264-275 PLoS One, 2018, 13(8):e0200725	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 (NSC 154020, VD-0002, vqd-002, API-2) 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.	Cell Oncol (Dordr), 2020, 8 Int J Biol Sci, 2020, 16(13):2382-2391 Biol Pharm Bull, 2020, 10.1248	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. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.	Biomed Pharmacother, 2020, 130:110544 Sci Transl Med, 2019, 11(501) Cancers (Basel), 2019, 11(8)	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.	Sci Signal, 2020, 13(619) Cancers (Basel), 2020, 12(9)E2668 Biomolecules, 2020, 10(2)	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 (CS-0223) 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.	Cell Oncol (Dordr), 2020, 8 J Clin Med, 2019, 8(6) mBio, 2018, 9(5)	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. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.	Cancers (Basel), 2020, 12(7):E1782 Int J Nanomedicine, 2020, 15:17-29 Radiat Environ Biophys, 2020,	(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.
S9190	Oroxin B Oroxin B (Hypocretin-2), 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.
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 Cell Oncol (Dordr), 2020, 8 Sci Rep, 2020, 10(1):12644	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 (ONC201) TIC10 (ONC201) inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.	ACS Chem Biol, 2019, 14(5):1020-1029 Eur J Pharmacol, 2019, 857:172423 J Cancer, 2018, 9(8):1486-1499	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. Akti-1/2 induces apoptosis.	J Cell Physiol, 2020, 235(2):1051-1064 Mol Ther Oncolytics, 2020, 18:282-294 Int J Cancer, 2019, 145(6):1690-1700	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.	Oncol Lett, 2020, Cancers (Basel), 2019, 11(9) Sci Rep, 2019, 9(1):10933
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. Usnic acid inhibits breast tumor angiogenesis and growth by suppressing VEGFR2-mediated AKT and ERK1/2 signaling pathways.
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.	Dev Dyn, 2020, 10.1002/dvdy.231 Int J Biol Sci, 2020, 16(14):2559-2579 Cancer Res, 2019, 79(9):2367-2378	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.)
S3785	Notoginsenoside R1 Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways.
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, 2020, 11(1):4629 Cell Oncol (Dordr), 2020, 8 Cancer Sci, 2020, 111(5):1663-1675	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. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S2335	Oridonin Oridonin (Isodonol, Rubescenin, NSC-250682), a diterpenoid purified from Rabdosia rubescens, is a traditional agent with antitumor, anti-bacterial and anti-inflammatory effects. Oridonin inhibits AKT1 and AKT2 kinase activity with IC50 of 8.4 μM and 8.9 μM, respectively.	Protein Sci, 2020, 29(6):1366-1372 Mediators Inflamm, 2019, 2019:7634761 Biochem Biophys Res Commun, 2019, 513(3):594-601	Histopathological analysis of H460 tumors following combination treatment with oridonin and radiation. Hematoxylin and eosin (H-E) staining and immunohistochemistry for cleaved caspase-3 and γ-H2AX were performed on tumors harvested at 14 days after IR. Representative images of H-E-stained tumors (upper images) and cleaved caspase-3- and γ-H2AX-positive cells (middle images, brown staining) and quantification of cleaved caspase-3 and γ-H2AX-positive staining with six mice in each group (lower plots, means ± SEM) are shown; * p < 0.05.
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. Scutellarin can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.
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.	Cell, 2020, 182(3):685-712.e19 Cancer Cell, 2020, 37(1):85-103 Nat Cell Biol, 2019, 21(6):778-790	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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S3224^新	Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238^新	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S3289^新	Daphnoretin Daphnoretin (Dephnoretin, Thymelol), a biologically active compound isolated from Wikstroemia indica C.A. Mey., is a protein kinase C (PKC) activator. Daphnoretin inhibits the proliferation, invasion, and migration of tumor cells and promote its apoptosis by regulating the activity of Akt signal pathway.
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.	Proc Natl Acad Sci U S A, 2020, 117(40):25104-25115 Biomaterials, 2020, 237:119793 Cell Rep, 2020, 30(5):1400-1416	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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S3294^新	Demethyl-Coclaurine Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.

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S3294^新

Demethyl-Coclaurine

Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.

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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

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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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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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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