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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
BCC1163 PIK-75 PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
BCC3906 TIC10 TIC10 isomer is the isomer of TIC10. TIC10 isomer does not possess the reported biological activity of inducing TRIAL expression.
BCC1442 CAL-130 Racemate CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.
BCC3657 ZSTK474 ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
BCN2385 Indirubin Indirubin (Couroupitine B) is a purple 3,2- bisindole and a stable isomer of indigo isolated from Indigo naturalis (Apiaceae); anti-inflammatory and anticancer activities.
BCC1805 Nordihydroguaiaretic acid Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC50=8 μM) and tyrosine kinase inhibitor.
BCC5030 BI-D1870 BI-D1870 is an ATP-competitive, cell permeable inhibitor of RSK isoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively.
BCC3679 NU7441 (KU-57788) KU-57788 is a potent and selective inhibitor of DNA-PK with an IC50 of 13 nM, with selectivity over a range of kinases including mTOR, PI 3-K, ATM and ATR.
BCC3592 Rapamycin (Sirolimus) Rapamycin (Sirolimus) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
BCC7873 PIT 1
BCC1321 A-443654 A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
BCC3903 A-674563 A-674563 is a potent and selective Akt1 inhibitor with a Ki of 11 nM.
BCC4605 Ridaforolimus (Deforolimus, MK-8669) Deforolimus (AP23573; MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
BCC4360 Miltefosine Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).
BCC2519 PIK-93 PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
BCC4512 TWS119 TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
BCC4126 GSK-3 inhibitor 1 GSK-3 inhibitor 1 is an inhibitor of GSK-3.
BCC1717 LY2090314 LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
BCC4508 AZD1080 AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
BCC1334 AKT inhibitor VIII AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.
BCC4989 AS-604850 AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively.
BCC2495 AS-605240 AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
BCC1244 TGX-221 TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.
BCC4510 GSK-3 Inhibitor IX (BIO) GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
BCC5332 1-Azakenpaullone 1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM.
BCC1247 TG100-115 TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.
BCC1248 PIK-90 PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
BCC4220 AICAR phosphate AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AMPK Activator.
BCC1250 BX-912 BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
BCC3635 BX795 BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
BCC5527 ZLN024 ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
BCC1255 OSU-03012 (AR-12) PDPK1 (PDK1) inhibitor; inhibits Akt signaling,OSU-03012 (AR-12) is a potent inhibitor of recombinant PDK-1(phosphoinositide-dependent kinase 1) with IC50 of 5 μM in a cell-free assay and 2-fold increase in potency over OSU-02067.
BCC1533 DMAT DMAT is a potent and specific CK2 inhibitor with an IC₅₀ value of 130 nM.
BCC4085 Imeglimin hydrochloride Imeglimin hydrochloride (EMD 387008) is an oral glucose-lowering agent. Imeglimin also reduces reactive oxygen species (ROS) production, increases mitochondrial DNA and improves mitochondrial function.
BCC4221 Imeglimin Imeglimin (EMD 387008) is an oral glucose-lowering agent. Imeglimin improves insulin sensitivity. Imeglimin also reduces reactive oxygen species (ROS) production, increases mitochondrial DNA and improves mitochondrial function.
BCC1489 CMK CMK is a RSK2 kinase inhibitor which exhibits similar potency but less chemical stability compared with FMK.
BCC1580 FMK FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
BCC1335 AKT Kinase Inhibitor AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
BCC6391 BX517(PDK1 inhibitor2) BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
BCC1813 NVP-BAG956 NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
BCC2536 AT7867 AT7867 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.
BCC4511 Tideglusib Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3βWT (1 h preincubation) and GSK-3βC199A (1 h preincubation), respectively.
BCC5131 Dorsomorphin Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
BCC6384 Acalisib (GS-9820) Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.
BCC1270 CAL-101 (Idelalisib, GS-1101) Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
BCC6160 SC 66 SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
BCC1110 KU-0060648 KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively.
BCC3904 CCT128930 CCT128930 is a potent and selective inhibitor of Akt2 (IC50 6 nM) with 28-fold selectivity over the closely related PKA kinase (IC50 168 nM), as well as 20-fold selectivity over p70S6K (IC50 120 nM).
BCC4994 PIK-293 PIK-293, an analog of IC87114, is a PI3K inhibitor, with IC50 values of 0.24 μM, 10 μM, 25 μM and 100 μM for p110δ, p110β, p110γ and p110α, respectively.
BCC4995 PIK-294 PIK-294 is a potent p110δ-selective inhibitor with an IC50 of 10 nM.
BCC4988 AS-252424 AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.
BCC7518 FPA 124 FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis.
BCC3905 Palomid 529 Palomid 529 is a potent inhibitor of mTORC1 and mTORC2 complexes.
BCC3655 BEZ235 (NVP-BEZ235) Dactolisib (BEZ235) is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
BCC7409 10-DEBC hydrochloride Selective Akt/PKB inhibitor
BCC4985 TG100713 PI 3-kinase inhibitor,TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
BCC4603 OSI-027 OSI-027 is an ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively.
BCC2483 GSK690693 GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2, 13, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693, an AMP-activated protein kinase (AMPK) inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
BCC2484 KU-0063794 KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC50s of 10 nM.
BCC1279 BKM120 Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
BCC5379 PI-3065 PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
BCC2487 XL147 Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
BCC3626 GDC-0941 Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
BCC1590 GDC-0941 dimethanesulfonate Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
BCC4181 NVP-QAV-572 NVP-QAV-572 is a PI3K inhibitor extracted from patent US7998990B2, Compound Example 8, has an IC50 of 10 nM.
BCC4984 GSK1059615 GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.