PI3K/Akt/mTOR Signaling

Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.

Rotundic acid, a triterpenoid obtained from I.

A metabolite of ellagic acid

A 22carbon monounsaturated fatty acid

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6?nM and 16?nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66?μM for mouse β (R7T1) cells).

Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound.

BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively.

9-ING-41 is a selective and potent GSK-3β inhibitor with an IC 50 value of 0.71μM.

PI-273 is a substrate-competitive and specific phosphatidylinositol 4-kinase IIα (PI4KIIα) inhibitor (IC 50= 0.47μM).

BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.

Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.

Rheb inhibitor NR1 is a small molecule that inhibits the monomeric protein Rheb with an IC 50 value of 2.1μM.

EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.

M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.

DNA-PK inhibitor IV is an inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 value of 400 nM for the DNA-PK-dependent phosphorylation of a p53 peptide substrate.

CAY10706 is a ligustrazine-curcumin hybrid that promotes intracellular reactive oxygen species accumulation preferentially in lung cancer cells.

2,3-Dimethoxy-5-methyl-p-benzoquinone (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea.

Viridiol is a fungal steroid that demonstrates phytotoxic activity.

Theaflavin 3,3'-digallate (TF-3; ZP10) is a potent inhibitor of Zika virus (ZIKV) protease with an IC 50 value of 2.3μM.

17β-hydroxy Wortmannin is an analog of wortmannin.

1-Deoxynojirimycin (1-dNM) (hydrochloride), produced by Bacillus species, is a glucose analog that potently inhibits α-glucosidase I and II.

1-O-Octadecyl-2-O-methyl-sn-glycerol is a metabolite of a phosphotidylinositol ether lipid analog (PIA).

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN.

Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively.