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PI3K/Akt/mTOR Signaling

The PI3K/AKT/mTOR pathway is an intracellular signaling pathway important in regulating the cell cycle. Therefore, it is directly related to cellular quiescence, proliferation, cancer, and longevity. PI3K activation phosphorylates and activates AKT, localizing it in the plasma membrane. AKT can have a number of downstream effects such as activating CREB, inhibiting p27, localizing FOXO in the cytoplasm, activating PtdIns-3ps, and activating mTOR which can affect transcription of p70 or 4EBP1. There are many known factors that enhance the PI3K/AKT pathway including EGF, shh, IGF-1, insulin, and CaM. The pathway is antagonized by various factors including PTEN, GSK3B, and HB9. In many cancers, this pathway is overactive, thus reducing apoptosis and allowing proliferation. This pathway is necessary, however, to promote growth and proliferation over differentiation of adult stem cells, neural stem cells specifically. It is the difficulty in finding an appropriate amount of proliferation versus differentiation that researchers are trying to determine in order to utilize this balance in the development of various therapies. Additionally, this pathway has been found to be a necessary component in neural long term potentiation.

Products for PI3K/Akt/mTOR Signaling

Cat.No. Product Name Information
BCC1271 GDC-0068 (RG7440) Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
BCC1843 PDK1 inhibitor MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
BCC4991 CH5132799 CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
BCC3629 AZD8055 AZD-8055 is a novel ATP-competitive inhibitor of mTOR kinase with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.
BCC3732 AZD2014 Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
BCC3837 PF-04691502 PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
BCC1416 BEZ235 Tosylate Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
BCC1274 MK-2206 dihydrochloride MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206 dihydrochloride. Anticancer activities.
BCC4986 BAY 80-6946 (Copanlisib) Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.
BCC8049 GNE-477 GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
BCC4992 GDC-0980 (RG7422) Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
BCC8048 GNE-493 GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
BCC5294 GSK2141795 Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
BCC5295 GSK2141795 hydrochloride GSK2141795 Hcl is a potent and selective pan-Akt inhibitor with IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3 respectively (Clinical phase 1).
BCC5502 Afuresertib Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.
BCC5360 AT13148 AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s 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.
BCC4607 WAY-600 WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
BCC4604 WYE-687 WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
BCC1059 WYE-354 WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2.
BCC6369 LY2584702 LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
BCC3884 GSK2126458 Omipalisib (GSK2126458) is a highly selective and potent inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively.
BCC3682 PP242 Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively.
BCC4980 PP121 PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.
BCC2060 XL765
BCC1073 AZD5363 Capivasertib (AZD5363) is a potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
BCC4608 WYE-125132 (WYE-132) WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.
BCC1507 CZC24832 CZC24832 is a highly selective and potent PI3Kγ inhibitor (IC50=27 nM) with apparent dissociation constants (Kdapp) of 19 nM.
BCC3715 A66 A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
BCC4180 PI3Kγ inhibitor 1 PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
BCC3843 PKI-402 PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
BCC2523 AZD6482 AZD 6482 (KIN-193) is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
BCC7859 PS 48
BCC2554 PHT-427 PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
BCC1104 IPI-145 (INK1197) Duvelisib is a selectivite p100δ inhibitor with
BCC1781 GDC-mTOR inhibitor mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
BCC1094 GDC-0349 GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a Ki of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.
BCC4363 WZ4003 WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2, without significant inhibition on other 139 kinases.
BCC3707 BYL-719 Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
BCC4990 CAY10505 CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.
BCC4361 Dorsomorphin 2HCl Dorsomorphin dihydrochloride (Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
BCC3676 Torin 1 Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy.
BCC4606 Torin 2 Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
BCC1876 QL-IX-55
BCC3880 INK 128 (MLN0128) Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.
BCC4982 GSK2334470 GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
BCC1310 PI4KIII beta inhibitor 3 PI4KIII beta inhibitor 3 is a novel and high effective ΡΙ4ΚΙΙΙβ inhibitor with IC₅₀ of 5.7 nM.
BCC3827 NVP-BGT226 BGT226 maleate (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.
BCC2047 VS-5584 (SB2343) VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.
BCC2059 XL388 XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.
BCC5031 PF-4708671 PF-4708671 is a potent cell-permeable S6K1 inhibitor with a Ki of 20 nM and IC50 of 160 nM.
BCC5745 SAMS Peptide SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).
BCC4086 YLF-466D YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
BCC6375 CNX1351 CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
BCC5363 HS-173 HS-173 is a novel PI3K inhibitor, that is used for cancer treatment.
BCC6468 PF-4989216 PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
BCC4066 GDC-0032 Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
BCC5586 CX-4945 sodium salt Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
BCC4303 BIX 02565 BIX 02565 is a potent ribosomal S6 kinase 2 (RSK2) inhibitor with IC50 of 1.1 nM.
BCC1861 PI3k-delta inhibitor 1 PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.
BCC3913 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
BCC6517 GSK621
BCC2534 SAR245409 Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
BCC4993 GSK2636771 GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
BCC5655 GNE-317 GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).
BCC8016 RSVA 405
BCC1440 CAL-130 CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
BCC1441 CAL-130 Hydrochloride CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
BCC1378 AT7867 dihydrochloride AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
BCC4314 OTSSP167 OTSSP167 is a highly potent MELK inhibitor with IC50 value of 0.41 nM.
BCC3933 NU 7026 NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
BCC3659 LY 294002 LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
BCC1715 LY 303511 LY303511 is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K+ currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
BCC3673 Perifosine Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
BCC6689 L-NIO dihydrochloride L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively. L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats.
BCC3594 Everolimus (RAD001) Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
BCC6510 AMG319 AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC50 of 18 nM.
BCC4010 HTH-01-015 HTH-01-015 is a selective NUAK1/ARK5 inhibitor (IC50 is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).
BCC3678 Temsirolimus Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM.
BCC6470 AZD8186 AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
BCC6538 LJI308 LJI308 is a new and potent pan-RSK inhibitor, with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.
BCC1988 TBB TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
BCC5582 Bikinin Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.
BCN5415 Isobavachalcone Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.
BCC1275 CHIR-99021 (CT99021) CHIR-99021 (CT99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 induces autophagy.
BCC3751 CHIR-98014 CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
BCC3606 AICAR AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy and mitophagy inhibitor.
BCC3651 SB 415286 Potent, selective GSK-3 inhibitor,SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β.
BCC3650 SB 216763 SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
BCC5402 3CAI 3CAI is a potent and specific AKT1 and AKT2 inhibitor.
BCC1518 Daun02 Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin.
BCC6246 SC 79 Akt activator,SC79 is a unique specific Akt activator that may be used to enhance Akt activity in various physiological and pathological conditions.
BCC6404 MHY1485 MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes
BCC4258 TDZD-8 TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
BCC2017 TTP 22 TTP 22 is a potent CK2 inhibitor, with an IC50 of 100 nM and a Ki of 40 nM.
BCC7846 PT 1 AMPK activator
BCC3872 Triciribine Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively.
BCC1161 IC-87114 IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.
BCC1162 PI-103 PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
BCC1860 PI-103 Hydrochloride PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
BCC4996 YM201636 YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with an IC50 of 3.3 μM. YM-201636 inhibits retroviral replication.