PI3K/Akt/mTOR Signaling

Selective oral PI3K inhibitor

PI3K/PLK1 inhibitor

INK1117 (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.

Potent and selective PI 3-Kγ inhibitor

A pan Akt inhibitor

CHPG is a selective metabotropic glutamate receptor 5 (mGlu5) agonist.

Temsirolimus (CCI-779), an ester of rapamycin, inhibits the activity of mTOR kinase activity with an IC 50 value of 1.76 ± 0.15μM.

Potent and selective inhibitor of PI3Kβ and PI3Kδ

Indirubin-3'-oxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 μM, respectively; Indirubin-3'-oxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.

XL147 (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.

PX 866 (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.

Akt inhibitor

A selective inhibitor of GSK-3

CX-4945 (Silmitasertib) is a potent and orally active casein kinase 2 (CK2) inhibitor with an IC 50 of 1nM for CK2α.

GSK3β inhibitor

HTH-01-015 is a potent and selective inhibitor of NUAK1 with a IC 50 value of 100nM and does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.

MTOR inhibitor,ATP-competitive and selective

CAL-101 (Idelalisib, GS-1101) is a phosphatidylinositol 3-kinase δ (PI3Kδ/p110δ) inhibitor (IC 50 =2.5nM).

TRPC activator

PI3K and endogenous midkine (MDK) expression inhibitor

GSK-3β inhibitor

Non-ATP-competitive inhibitor of PLK1