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Akt

Isoform-selective Products

Akt1 Akt2 Akt3

Signaling Pathway

Akt Products

All (73)
Akt Inhibitors (59)
Akt Activators (7)
Akt Modulators (6)
New Akt Products

Catalog No.	Product Name	Information	Product Use Citations
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.	Nat Cancer, 2024, Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0 Nat Commun, 2024, 15(1):2132
S1037	Perifosine	Perifosine is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.	Exp Cell Res, 2024, 436(2):113978 Sci Rep, 2023, 13(1):12424 Sci Rep, 2023, 13(1):12424
S7863	SC79	SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.	Signal Transduct Target Ther, 2024, 9(1):109 Signal Transduct Target Ther, 2024, 9(1):109 J Exp Clin Cancer Res, 2024, 43(1):56
S8019	Capivasertib (AZD5363)	Capivasertib (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.	Nat Neurosci, 2024, 10.1038/s41593-024-01604-8 Mol Cell, 2024, S1097-2765(24)00865-7 Cell Rep Med, 2024, 5(10):101752
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9 CNS Neurosci Ther, 2024, 30(8):e14913
S2808	Ipatasertib (GDC-0068)	Ipatasertib (GDC-0068, RG7440) 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, 2024, 10.1038/s41586-024-08031-6 Cell Rep Med, 2024, S2666-3791(24)00179-4 Cancer Lett, 2024, 604:217219
S1117	Triciribine (API-2)	Triciribine (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.	J Cell Sci, 2023, 136(4)jcs259788 Exp Gerontol, 2023, 173:112091 EJHaem, 2023, 4(3):631-638
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.	Exp Gerontol, 2024, 186:112359 iScience, 2023, 26(9):107734 Exp Gerontol, 2023, 173:112091
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.	Nat Commun, 2024, 15(1):2089 Environ Mol Mutagen, 2024, 10.1002/em.22604 Cancer Cell, 2022, 40(7):754-767.e6
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.	Nat Commun, 2024, 15(1):6150 Cell Rep, 2024, 43(4):114108 Nat Commun, 2023, 14(1):886
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.	Int J Nanomedicine, 2023, 18:4313-4327 Exp Gerontol, 2023, 173:112091 Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
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.	Cell Rep, 2024, 43(9):114728 Oncogene, 2024, 43(19):1411-1430 Heliyon, 2024, 10(1):e23945
S2670	A-674563 HCl	A-674563 HCl 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.	J Biol Chem, 2024, 300(2):105641 Nat Commun, 2023, 14(1):886 Exp Gerontol, 2023, 173:112091
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.	Exp Gerontol, 2023, 173:112091 Cancers (Basel), 2022, 14(21)5215 Oncoimmunology, 2021, 10(1):1943234
S2335	Oridonin	Oridonin, 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.	Inflammopharmacology, 2023, 31(4):1993-2005 J Immunol Res, 2023, 2023:5293677 J Immunother Cancer, 2022, 10(9)e005116
S7776	Akti-1/2	Akti-1/2 (Akt Inhibitor VIII) 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 Exp Clin Cancer Res, 2024, 43(1):56 iScience, 2024, 27(4):109580 Sci Rep, 2024, 14(1):11174
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.	Exp Gerontol, 2023, 173:112091 Cancer Cell, 2022, S1535-6108(22)00312-9 Nucleic Acids Res, 2022, gkac179
S3056	Miltefosine	Miltefosine (Hexadecylphosphocholine) 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.	Environ Toxicol Pharmacol, 2024, S1382-6689(24)00205-9 PLoS Negl Trop Dis, 2024, 18(3):e0011976 Evid Based Complement Alternat Med, 2022, 2022:4388919
S8339	Miransertib (ARQ 092) HCl	Miransertib (ARQ 092) HCl is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors.	World J Oncol, 2024, 15(2):192-208 Chemistry, 2023, e202203959. Nat Commun, 2022, 13(1):2111
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.	Neoplasia, 2023, 10.1016/j.neo.2023.100948 Cancers (Basel), 2022, 14(23)5943 Br J Cancer, 2021, 10.1038/s41416-021-01442-6
S7492	Uprosertib (GSK2141795)	Uprosertib (GSK2141795, GSK795) 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.	Nat Commun, 2022, 13(1):245 Bone Res, 2022, 10(1):27 Front Oncol, 2022, 12:905665
S6811	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.	World J Oncol, 2024, 15(3):492-505 World J Oncol, 2024, 15(2):192-208 Commun Biol, 2023, 6(1):916
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.	Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110725 J Cell Mol Med, 2021, 10.1111/jcmm.17005 Oncol Lett, 2020,
S5144	Neferine	Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.	Bone Res, 2022, 10(1):27 Cell Death Dis, 2022, 13(11):1000 iScience, 2022, 25(11):105394
S3901	Astragaloside IV	Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.	Cell Transplant, 2023, 32:9636897231198167 Cell Transplant, 2023, 32:9636897231198167 Cell Cycle, 2022, 1-14
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 are downregulated, while PTEN is upregulated after Oroxin B treatment.	Environ Pollut, 2023, 323:121306 Theranostics, 2022, 12(2):910-928 J Cancer, 2021, 12(7):2140-2150
S8132	Deguelin	Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.	Cell, 2023, 186(13):2929-2949.e20 Cell Death Dis, 2020, 11(2):143 Oncotarget, 2020, 11(46):4224-4242
S6847	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.	PLoS Pathog, 2023, 19(3):e1011295 J Mol Endocrinol, 2019, 63(3):199-213
S3238	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.	Research Square, 2024, 10.21203/rs.3.rs-3790060/v1 Phytomedicine, 2022, 102:154182
S3296	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.	Evid Based Complement Alternat Med, 2023, 2023:9428241
E2384	(E)-Akt inhibitor-IV	(E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic.	Eur J Pharmacol, 2022, 931:175186
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.	Food Sci Nutr, 2023, 11(12):7791-7802 J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3810	Scutellarin	Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide), 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.	Biomed Pharmacother, 2022, 155:113781
S3220	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.	Biomed Pharmacother, 2021, 143:112204
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.
S3294	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.	Signal Transduct Target Ther, 2024, 9(1):243
E2947	Recilisib	Recilisib (ON01210, EX-RAD) is a radioprotectant that activates the activity of AKT and PI3K in cells. It has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug.
S4572	Homosalate	Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways.
S3289	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.
S9514	Rotundic acid	Rotundic acid (Rutundic 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.
S3224	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.
S8961	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.
S8839	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.
S5554	Lanatoside C	Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S3243	Zeaxanthin	Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
E1125	A-443654	A-443654, a derivative of indazole–pyridine compounds, is a pan Akt (Akt1, 2, & 3 isoforms) inhibitor which binds to the ATP-binding site of Akt. It is an ATP competitive and reversible inhibitor.
E3656	Dichroa febrifuga Extract	Dichroa Febrifuga Extract is extracted from Dichroa Febrifuga, which can Suppress PI3K/AKT and MAPK Signaling Pathways.
S0765	MAZ51	MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
S4953	Usnic acid	Usnic acid (Usniacin) 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.
E3106	Dioscoreae Nipponicae Rhizoma Extract	Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
E1710^New	LY2780301	LY2780301 is a highly selective adenosine triphosphate (ATP)-competitive dual inhibitor of p70S6K and Akt. LY2780301 binds to Akt, inhibiting its activity, which consequently blocks the PI3K/Akt signaling pathway which leads to reduced cell proliferation and the initiation of apoptosis in tumor cells.
E3241	Cinnamomi Ramulus Extract	Cinnamomi Ramulus Extract is extracted from Cinnamomi Ramulus, which can inhibit the growth of colon cancer cells via Akt/ERK signaling pathways.
E0020	Lupenone	Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway.
E3041	Alpiniae Katsumadai Extract	Alpiniae Katsumadai Extract is extracted from Alpiniae Katsumadai, which can induce growth inhibition and autophagy‑related apoptosis by regulating the AMPK and Akt/mTOR/p70S6K signaling pathways in cancer cells.
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.
E3365	Weigela Grandiflora Fortune Extract	Weigela Grandiflora Fortune Extract is extracted from Weigela Grandiflora Fortune, which decreases the infection-mediated expression of inflammatory mediators by inhibiting the AKT/NF-κB and MAPK signaling pathways.
S6760	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.	Theranostics, 2024, 14(4):1561-1582 Int J Mol Sci, 2024, 25(4)2408 Sci Rep, 2024, 14(1):12090
S3309	Solasodine	Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21.
S9054	Pectolinarin	Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway.
E2391	α-Linolenic acid	α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties.
E0945	BIA	BIA (TMBIM6 antagonist BIA), a potential TMBIM6 antagonist, is an inhibitor of the interaction between TMBIM6 (Transmembrane B cell lymphoma 2-associated X protein (BAX) inhibitor motif-containing 6) and mTORC2, which ultimately blocks AKT activation and cancer progression.
S6885	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.	Theranostics, 2024, 14(4):1371-1389
S2323	Methyl-Hesperidin	Methyl Hesperidin is a flavanone glycoside (flavonoid) (C28H34O15) found abundantly in citrus fruits. Its aglycone form is called hesperetin.
E2682	RPI-1	RPI-1 inhibits proliferation of human papillary thyroid carcinoma cell line TPC-1 by inducing accumulation of cells at the G2 cell cycle phase, abolishes Ret/Ptc1 tyrosine phosphorylation along with its binding to Shc and phospholipase Cg, also abolishes the activation of JNK2 and AKT.
S8500	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).
E2826	Hematein	Hematein inhibits casein kinase II activity in a selective, dose-dependent and ATP non-competitive manner in vitro, with IC50 of 0.55 μM in the presence of 10 μM ATP.
S9611	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.
E2401	SPP-86	SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
S1321	Urolithin B	Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S1273	Amarogentin	Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.
S3241	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.
E0785	YS-49	YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.	Signal Transduct Target Ther, 2024, 9(1):243
E1604^New	Vevorisertib trihydrochloride	Vevorisertib trihydrochloride(ARQ 751 trihydrochloride) is a selective, allosteric inhibitor of pan-AKT and AKT1-E17K mutant with Kd values of 1.2 nM and 8.6 nM, respectively. It also has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively and can be used for the research of cancer.
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.	Nat Cancer, 2024, Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0 Nat Commun, 2024, 15(1):2132
S1037	Perifosine	Perifosine is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.	Exp Cell Res, 2024, 436(2):113978 Sci Rep, 2023, 13(1):12424 Sci Rep, 2023, 13(1):12424
S8019	Capivasertib (AZD5363)	Capivasertib (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.	Nat Neurosci, 2024, 10.1038/s41593-024-01604-8 Mol Cell, 2024, S1097-2765(24)00865-7 Cell Rep Med, 2024, 5(10):101752
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9 CNS Neurosci Ther, 2024, 30(8):e14913
S2808	Ipatasertib (GDC-0068)	Ipatasertib (GDC-0068, RG7440) 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, 2024, 10.1038/s41586-024-08031-6 Cell Rep Med, 2024, S2666-3791(24)00179-4 Cancer Lett, 2024, 604:217219
S1117	Triciribine (API-2)	Triciribine (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.	J Cell Sci, 2023, 136(4)jcs259788 Exp Gerontol, 2023, 173:112091 EJHaem, 2023, 4(3):631-638
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.	Exp Gerontol, 2024, 186:112359 iScience, 2023, 26(9):107734 Exp Gerontol, 2023, 173:112091
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.	Nat Commun, 2024, 15(1):2089 Environ Mol Mutagen, 2024, 10.1002/em.22604 Cancer Cell, 2022, 40(7):754-767.e6
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.	Nat Commun, 2024, 15(1):6150 Cell Rep, 2024, 43(4):114108 Nat Commun, 2023, 14(1):886
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.	Int J Nanomedicine, 2023, 18:4313-4327 Exp Gerontol, 2023, 173:112091 Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
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.	Cell Rep, 2024, 43(9):114728 Oncogene, 2024, 43(19):1411-1430 Heliyon, 2024, 10(1):e23945
S2670	A-674563 HCl	A-674563 HCl 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.	J Biol Chem, 2024, 300(2):105641 Nat Commun, 2023, 14(1):886 Exp Gerontol, 2023, 173:112091
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.	Exp Gerontol, 2023, 173:112091 Cancers (Basel), 2022, 14(21)5215 Oncoimmunology, 2021, 10(1):1943234
S2335	Oridonin	Oridonin, 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.	Inflammopharmacology, 2023, 31(4):1993-2005 J Immunol Res, 2023, 2023:5293677 J Immunother Cancer, 2022, 10(9)e005116
S7776	Akti-1/2	Akti-1/2 (Akt Inhibitor VIII) 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 Exp Clin Cancer Res, 2024, 43(1):56 iScience, 2024, 27(4):109580 Sci Rep, 2024, 14(1):11174
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.	Exp Gerontol, 2023, 173:112091 Cancer Cell, 2022, S1535-6108(22)00312-9 Nucleic Acids Res, 2022, gkac179
S3056	Miltefosine	Miltefosine (Hexadecylphosphocholine) 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.	Environ Toxicol Pharmacol, 2024, S1382-6689(24)00205-9 PLoS Negl Trop Dis, 2024, 18(3):e0011976 Evid Based Complement Alternat Med, 2022, 2022:4388919
S8339	Miransertib (ARQ 092) HCl	Miransertib (ARQ 092) HCl is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors.	World J Oncol, 2024, 15(2):192-208 Chemistry, 2023, e202203959. Nat Commun, 2022, 13(1):2111
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.	Neoplasia, 2023, 10.1016/j.neo.2023.100948 Cancers (Basel), 2022, 14(23)5943 Br J Cancer, 2021, 10.1038/s41416-021-01442-6
S7492	Uprosertib (GSK2141795)	Uprosertib (GSK2141795, GSK795) 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.	Nat Commun, 2022, 13(1):245 Bone Res, 2022, 10(1):27 Front Oncol, 2022, 12:905665
S6811	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.	World J Oncol, 2024, 15(3):492-505 World J Oncol, 2024, 15(2):192-208 Commun Biol, 2023, 6(1):916
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.	Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110725 J Cell Mol Med, 2021, 10.1111/jcmm.17005 Oncol Lett, 2020,
S3901	Astragaloside IV	Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.	Cell Transplant, 2023, 32:9636897231198167 Cell Transplant, 2023, 32:9636897231198167 Cell Cycle, 2022, 1-14
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 are downregulated, while PTEN is upregulated after Oroxin B treatment.	Environ Pollut, 2023, 323:121306 Theranostics, 2022, 12(2):910-928 J Cancer, 2021, 12(7):2140-2150
S8132	Deguelin	Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.	Cell, 2023, 186(13):2929-2949.e20 Cell Death Dis, 2020, 11(2):143 Oncotarget, 2020, 11(46):4224-4242
S6847	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.	PLoS Pathog, 2023, 19(3):e1011295 J Mol Endocrinol, 2019, 63(3):199-213
S3238	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.	Research Square, 2024, 10.21203/rs.3.rs-3790060/v1 Phytomedicine, 2022, 102:154182
S3296	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.	Evid Based Complement Alternat Med, 2023, 2023:9428241
E2384	(E)-Akt inhibitor-IV	(E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic.	Eur J Pharmacol, 2022, 931:175186
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.	Food Sci Nutr, 2023, 11(12):7791-7802 J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3810	Scutellarin	Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide), 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.	Biomed Pharmacother, 2022, 155:113781
S3220	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.	Biomed Pharmacother, 2021, 143:112204
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.
S3224	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.
S8839	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.
S5554	Lanatoside C	Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S3243	Zeaxanthin	Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
E1125	A-443654	A-443654, a derivative of indazole–pyridine compounds, is a pan Akt (Akt1, 2, & 3 isoforms) inhibitor which binds to the ATP-binding site of Akt. It is an ATP competitive and reversible inhibitor.
E3656	Dichroa febrifuga Extract	Dichroa Febrifuga Extract is extracted from Dichroa Febrifuga, which can Suppress PI3K/AKT and MAPK Signaling Pathways.
S4953	Usnic acid	Usnic acid (Usniacin) 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.
E3106	Dioscoreae Nipponicae Rhizoma Extract	Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
E1710^New	LY2780301	LY2780301 is a highly selective adenosine triphosphate (ATP)-competitive dual inhibitor of p70S6K and Akt. LY2780301 binds to Akt, inhibiting its activity, which consequently blocks the PI3K/Akt signaling pathway which leads to reduced cell proliferation and the initiation of apoptosis in tumor cells.
E3241	Cinnamomi Ramulus Extract	Cinnamomi Ramulus Extract is extracted from Cinnamomi Ramulus, which can inhibit the growth of colon cancer cells via Akt/ERK signaling pathways.
E0020	Lupenone	Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway.
E3041	Alpiniae Katsumadai Extract	Alpiniae Katsumadai Extract is extracted from Alpiniae Katsumadai, which can induce growth inhibition and autophagy‑related apoptosis by regulating the AMPK and Akt/mTOR/p70S6K signaling pathways in cancer cells.
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.
E3365	Weigela Grandiflora Fortune Extract	Weigela Grandiflora Fortune Extract is extracted from Weigela Grandiflora Fortune, which decreases the infection-mediated expression of inflammatory mediators by inhibiting the AKT/NF-κB and MAPK signaling pathways.
S3309	Solasodine	Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21.
S9054	Pectolinarin	Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway.
E0945	BIA	BIA (TMBIM6 antagonist BIA), a potential TMBIM6 antagonist, is an inhibitor of the interaction between TMBIM6 (Transmembrane B cell lymphoma 2-associated X protein (BAX) inhibitor motif-containing 6) and mTORC2, which ultimately blocks AKT activation and cancer progression.
E2682	RPI-1	RPI-1 inhibits proliferation of human papillary thyroid carcinoma cell line TPC-1 by inducing accumulation of cells at the G2 cell cycle phase, abolishes Ret/Ptc1 tyrosine phosphorylation along with its binding to Shc and phospholipase Cg, also abolishes the activation of JNK2 and AKT.
S8500	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).
E2826	Hematein	Hematein inhibits casein kinase II activity in a selective, dose-dependent and ATP non-competitive manner in vitro, with IC50 of 0.55 μM in the presence of 10 μM ATP.
S9611	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.
E2401	SPP-86	SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
S1321	Urolithin B	Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S1273	Amarogentin	Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.
S3241	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.
E1604^New	Vevorisertib trihydrochloride	Vevorisertib trihydrochloride(ARQ 751 trihydrochloride) is a selective, allosteric inhibitor of pan-AKT and AKT1-E17K mutant with Kd values of 1.2 nM and 8.6 nM, respectively. It also has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively and can be used for the research of cancer.
S7863	SC79	SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.	Signal Transduct Target Ther, 2024, 9(1):109 Signal Transduct Target Ther, 2024, 9(1):109 J Exp Clin Cancer Res, 2024, 43(1):56
S5144	Neferine	Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.	Bone Res, 2022, 10(1):27 Cell Death Dis, 2022, 13(11):1000 iScience, 2022, 25(11):105394
S3294	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.	Signal Transduct Target Ther, 2024, 9(1):243
E2947	Recilisib	Recilisib (ON01210, EX-RAD) is a radioprotectant that activates the activity of AKT and PI3K in cells. It has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug.
S0765	MAZ51	MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
S6760	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.	Theranostics, 2024, 14(4):1561-1582 Int J Mol Sci, 2024, 25(4)2408 Sci Rep, 2024, 14(1):12090
E0785	YS-49	YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.	Signal Transduct Target Ther, 2024, 9(1):243
S4572	Homosalate	Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways.
S3289	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.
S9514	Rotundic acid	Rotundic acid (Rutundic 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.
S8961	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.
E2391	α-Linolenic acid	α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties.
S6885	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.	Theranostics, 2024, 14(4):1371-1389
E1710^New	LY2780301	LY2780301 is a highly selective adenosine triphosphate (ATP)-competitive dual inhibitor of p70S6K and Akt. LY2780301 binds to Akt, inhibiting its activity, which consequently blocks the PI3K/Akt signaling pathway which leads to reduced cell proliferation and the initiation of apoptosis in tumor cells.
E1604^New	Vevorisertib trihydrochloride	Vevorisertib trihydrochloride(ARQ 751 trihydrochloride) is a selective, allosteric inhibitor of pan-AKT and AKT1-E17K mutant with Kd values of 1.2 nM and 8.6 nM, respectively. It also has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively and can be used for the research of cancer.

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