PI3K/Akt/mTOR Signaling

VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively.

VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively.

YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells.

YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells.

An allosteric activator of AMPK

KDU731, an orally active C.

A selective inhibitor of PI3Kγ

Demethyleneberberine (DMB), as a natural active component of medicinal plant Cortex phellodendri chinensis, has favorable bioactivity.

Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla. Heterophyllin B provides a novel strategy for the treatment of esophageal cancer.

A natural diterpene with antiinflammatory and antiangiogenic properties

A coumarin with diverse actions

Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.

rac-AZD 6482 ((Rac)-KIN-193) is the racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.

An alkaloid with diverse biological activities

A tricyclic diterpene

WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.

Desmethylglycitein, a metabolite of daidzein, is a potent tyrosinase inhibitor with an IC 50 value of 9.2μM for mushroom tyrosinase.

A naphthol with diverse biological activities

KPT-6566 is a selective, covalent PIN1 (peptidyl-prolyl cis-trans isomerase) inhibitor (IC 50 =640nM; K i =625.2nM).

A PI3K inhibitor