PI3K/Akt/mTOR

Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).

AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.

AZD1080 is a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.

AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor.

Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.

FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells.

BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

OSU-03012 is a novel celecoxib derivative, without cyclooxygenase-2 inhibitory activity, capable of inducing apoptosis in various cancer cells types.

Tideglusib is a GSK-3 inhibitor currently in phase II clinical trials for the treatment of Alzheimer disease and progressive supranuclear palsy

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively.

BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and fatty acid synthase inhibitor.

VE-821 is a potent and selective inhibitor of protein kinase ATR.

BI-D1870 is a potent and specific inhibitor of the p90 ribosomal S6 kinase (RSK) isoforms in vitro and in vivo, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of 10?€?30 nM.

OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.

XL147 is a potent, selective and orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K) with potential antineoplastic activity.

PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.

Gedatolisib (PKI-587) is a highly potent PI3K/mTOR kinase inhibitor that inhibits PI3K-α,β,γ, δ isoforms and mTOR with IC50 of 0.4, 6.0, 5.4, 6.0 and 1.6 nM respectively.

Shikonin, a component of chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1.

Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242).

AS-605240 is an orally active inhibitor of PI3-kinase γ that inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

AT7867 is a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A.

Deforolimus (Ridaforolimus) is an investigational targeted and small-molecule inhibitor of the protein mTOR. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis.

IC-87114 was the first isoform-selective PI3K inhibitor :p110M-NM-4(IC50 = 0.13 M-BM-5M) vs. p110M-NM-1(IC50 = 200 M-BM-5M), p110M-NM-2(IC50 = 16 M-BM-5M) and p110M-NM-3(IC50 = 61 M-BM-5M).

Indirubin, the active constituent of a Chinese antileukaemia medicine, is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.

KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively).

Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/mTOR pathway having broad activity in angiogenesis and cellular proliferation.

PIK-293 is a PI3-K inhibitor. PIK-293 inhibits the p110α, p110β, p110δ. PIK-293 is the parent compound of PIK-294.

PIK-294 is a PI3 Kinase inhibitor that is 20- to 60-fold more potent than the parent compound, PIK-293. It is one of the most potent p110δ-selective inhibitors that has been reported.

PIK-90 is a synthetic phosphoinositide 3-kinase (PI3K) inhibitor with IC50 values (nM) of 11, 350, 18, and 58 for p110 α, β, γ and δ isoforms, low mTOR activity.

Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.

SB 216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).

Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.

Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells.

TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively).

XL765 is a PI3K/mTOR dual kinase inhibitor and it is more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone.

CCT128930 is an ATP-competitive AKT inhibitor that is a potent, advanced lead pyrrolopyrimidine compound exhibiting selectivity for AKT over PKA, achieved by targeting a single amino acid difference.

PHT-427 is a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor.

Triciribine phosphate inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation.

GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.

WYE-125132 is an ATP-competitive and specific inhibitor of mTORC1 and mTORC2 (IC50 = 0.19 nM; >5,000-fold selective versus PI3Ks).

OSI-027 is a potent, selective and orally bioavailable mTOR kinase inhibitor that inhibits the kinase activity associated with both the TORC1 and TORC2 complexes of mTOR.

SB 415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM.

CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3.

CP-466722 is a specific ATM inhibitor that inhibits cellular ATM-dependent phosphorylation events and disruption of ATM function resulted in characteristic cell cycle checkpoint defects.

PKI-402 is a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor.

AS-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000, and 20,000 nM respectively.

Camonsertib is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays.