mTOR

A butyrolactone derivative and autophagy inhibitor

PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.

A dual inhibitor of PI3K and mTOR

Pomiferin (NSC 5113) (NSC 5113) acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 μM).

FT-1518 is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor, and exhibits antitumor activity.

A dual inhibitor of PI3Kα and mTOR

CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.

JR-AB2-011 is an improved mTORC2 inhibitor identified through structure-activity relationship (SAR) studies with an IC 50 value of 0.36μM.

Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.

BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.

PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

A dual inhibitor of PI3K and mTORC

An alkaloid with diverse biological activities

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.

Rotundic acid, a triterpenoid obtained from I.

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

AR420626 is an oral active and selective agonist of free fatty acid receptor 3 (FFAR3) with an EC 50 value of 2.2µM.

eCF309 is an ATP-competitive inhibitor of mTOR (IC50 = 15 nM in vitro and in cells) with >65-fold selectivity over other kinases, including PI3Ks.

NVP-BEZ235 is a potent dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies.

An internal standard for the quantification of rapamycin

MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.

TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca2+.

hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC 50 value of 0.11nM.