|Description||GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR.|
CC-115, a DNA-PK and mTOR inhibitor, has been found to have probable anticarcinoma effect. IC50:13 nM and 21 nM for DNA-PK and mTOR respectively.
Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates in cells at concentrations of 2 and 10 nM, respectively.
PP242 is a novel potent and selective mTOR inhibitor with an IC50 of 8 nM. PP242 also shows residual (micromolar) activity against panel of tyrosine kinases. Bu...
WYE-687 is a potent and ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM.
The functional target of QL-IX-55 is the ATP-binding site of TOR2 as evidenced by the discovery of resistant alleles of TOR2 through rational design and unbiase...
NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) and is a highly potent mTOR inhibitor, with reasonable liver microsome stability.
Palomid 529, also known as P529, is a novel PI3K/Akt/mTOR inhibitor. Palomid 529 (P529) inhibits the TORC1 and TORC2 complexes and shows both inhibition of Akt ...
PI3K inhibitory activity. Inhibits voltage-gated Kv channel activity (IC50 = 64.6 μM). Various pharmacological effects including inhibition of LPS-stimulated FP...
Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM.
CC-223, a mTOR kinase inhibitor, has been found to be effective in inducing the apoptosis and reducing the proliferation of tumor cells. It is still under Phase...
WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.
mTOR activator with an inhibitory effect on autophagy. MHY1485 markedly increased the LC3II/LC3I ratio dose-dependently and time-dependently by inhibition of th...
Omipalisib, also known as GSK2126458, is asmall-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic acti...
GDC-0084, a PI3K inhibitor, has been found to have probable antineoplastic effect and could pass blood-brain barrier with favourable penetration. It was just li...
Torin 2 inhibits of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively.
MLN0128, also known as INK128, is a TORC1/2 inhibitor, is also an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR co...
GDC-0349 is a small molecule anticaner drug candidate, being developed by Genentech. As of July 2012, Genentech has filed phase I trial of GDC-0349 for evaluati...
Gedatolisib (PF-05212384, PKI-587)
Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Phase 2.
SMER18 is a small molecule enhancer of rapamycin. It act as a mTOR-independent autophagy inducer. It is a positive regulators of autophagy acting independently ...
PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR (Kis= 10.6 nM and 12.5 nM for mTOR and PI3Kα, respectively).