PI3K/Akt/mTOR

GDC-0032 is a potent, next-generation PI3 inhibitor targeting PI3 alpha.

KP372-1 is a synthetic small molecule AKT inhibitor.

BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM).

PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.

PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor.

GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis.

Afuresertib, also known as GSK2110183, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. It binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.

AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.

CC-223 is a potent mTOR kinase inhibitor (IC50=16 nM), with >150-fold sensitivity over the related lipid kinase PI3K-alpha (IC50=4uM).

CGK733 is a selective inhibitor of ATR and ATM kinases. Induces cell death in prematurely senescent breast cancer cells.

AZ20 is a potent and selective inhibitor of ATR with an IC50 value of 5 nM.

Triciribine, also known as API-2, suppresses the phosphorylation level and kinase activity of Akt.

KU0060648 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. KU-0060648 enhances HDR efficiency and attenuates NHEJ frequency.

Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt.

BX-912 is an inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1).

NVP-BGT226, novel phosphoinositide 3-kinase/mTOR dual inhibitor, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo.

CH5132799 is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM).

WYE-687 is a novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin(mTOR).

WAY-600 is a single digit nanomolar inhibitor of the mTOR kinases, with significant selectivity for these enzymes over phosphatidylinositol 3-kinase (PI3K) isofoms (>100-fold).

CAY10505 is a potent inhibitor of PI3K, selectively inhibiting the γ isoform (IC50 = 30 nM) better than the α, β, and δ isoforms (IC50 = 0.94, 20, and 20 μM, respectively).

AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.

D-106669 is a highly potent and selective PI3K inhibitor, (PI3Kα IC50 <10 nM, >3 log selectivity against tyrosine or serine/threonine kinases, except ERK1 and 2).

The S-enantiomer of A66 is a potent inhibitor of the p110alpha isoform of PI 3-kinase (PIK3CA).

PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR).

TWS119 is a 4,6 disubstituted pyrrolopyrimidine that potently inhibits GSK3β with an IC50 value of 30 nM.1 At 400 nM.

GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays

PX-866 is a small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity.

Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3.

AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.

A-443654, a specific Akt inhibitor with Ki value of 160 pM, interferes with mitotic progression and bipolar spindle formation.

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.

CMK is a RSK2 kinase inhibitor which exhibits similar potency but less chemical stability compared with FMK.

GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases.

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).

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).

NVP-BAG956 acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor, displaying much reduced potency against VEGFR1 (IC50 = 2.56 uM) and little or no activity toward a panel of 15 other kinases (IC50 >10 uM).

PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent.

QL-IX-55 is a selective ATP-competitive inhibitor of mTORC1/2 with IC50s of 50/50/10-50 nM for Human mTORC1/Yeast mTORC1/Yeast mTORC2, respectively.

Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 μM).

TDZD-8 protects the brain against I/R injury by inhibiting GSK-3beta activity

Zotarolimus is an immunosuppressant. It is a semi-synthetic derivative of rapamycin. It was designed for use in stents with phosphorylcholine as a carrier.

TG 100713 is an inhibitor of PI3-kinase that inhibits endothelial cell proliferation.

Schisandrin B is the most abundant dibenzocyclooctadiene isolated from the fruit of Schisandra chinensis (Turcz) Baillon or Wu-Wei-Zi (transliterally meaning "the fruit of five tastes" in Chinese), which is a commonly used tonic herb in Chinese medicine, particularly for the treatment of liver ailments.

SC 66 is an allosteric inhibitor of Akt that facilitates both ubiquitination and deactivation of Akt. It exhibits anticancer activity in vitro and in vivo.

MK8722 is a potent and systemic pan-AMPK activator.

HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies.

SF1670 is a selective PTEN inhibitor (IC50=2 uM). As PTEN-mTOR pathway is critical for controlling the regenerative capacity of corticospinal neurons, PTEN deletion or its inhibitor enhances the regenerative ability of adult corticospinal neurons. Pretreatment with SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model.

PS 48 is an allosteric phosphoinositide-dependent protein kinase-1 (PDK1) activator (Kd = 10.3 μM).

AP1903 is a lipid-permeable tacrolimus analogue with homodimerizing activity. Dimerizer drug AP1903 homodimerizes an analogue of human protein FKBP12 (Fv) which contains a single acid substitution (Phe36Val) so that AP1903 binds to wild-type FKBP12 with 1000-fold lower affinity.