PI3K/Akt/mTOR Signaling

Everolimus (RAD001) is an orally effective second-generation mTOR inhibitor.

CC-223 (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. CC-223 inhibits both mTORC1 and mTORC2.

GSK690693 is a potent and selective, ATP-competitive, pan-Akt kinase inhibitor with IC 50 values of 2nM, 13nM, and 9nM for Akt1, Akt2, and Akt3, respectively.

A dual PDK1 and class I PI3K inhibitor

MHY1485 is a cell-permeable mTOR activator.

A chalcone and flavonoid with diverse biological activities

Torin 2 is an orally active mTOR inhibitor (EC 50 =0.25nM).

PI3Kδ inhibitor

PS 48 is a PDK1 (phosphoinositide-dependent kinase-1) activator with an AC 50 of 8μM. PS 48 can bind to the HM/PIF binding pocket of PDK1, targeting the protein kinase catalytic domain without affecting the ATP binding site.

RGX-202 (3-Guanidinopropionic acid) is an oral small-molecule SLC6A8 transporter inhibitor. RGX-202 robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. RGX-202 can be used for the research of cancer and duchenne muscular dystrophy.

An inhibitor of RSK2

CK2 inhibitor

CDK1/cyclin B and GSK-3β inhibitor

GSK-3α/β inhibitor

GSK-3β inhibitor

LY3023414 (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. LY3023414 potently inhibits mTORC1/2 at low nanomolar concentrations.

Tideglusib is a potent, selective, and irreversible non-ATP competitive glycogen synthase kinase-3 (GSK-3) inhibitor. The IC 50 values for GSK-3βWT and GSK-3βC199A are 5nM and 60nM, respectively.

An inhibitor of class I PI3K isoforms

PIK-III is a potent and selective inhibitor of VPS34 with an IC50 of 18 nM.

GSK-3 inhibitor,potent and selective

A PI3Kγ inhibitor

Rapamycin (Sirolimus) is a macrolide mTOR inhibitor (IC 50 =0.1nM).

TG100-115 is an orally active selective inhibitor of PI3Kγ (IC 50 =83nM) and PI3Kδ (IC 50 =235nM).