Cbz-B3A

Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).

Signaling Pathways >> PI3K/Akt/mTOR >> mTOR

Research Areas >> Others

mTORC1 signaling[1].

Cbz-B3A slows cellular growth of some human leukemia cell lines, but is not cytotoxic. Cbz-B3A has a larger effect on the phosphorylation of 4EBP1 than p70S6k compared to repamycin. Cbz-B3A inhibits mTOR through Ubiquilins. Cbz-B3A decreases the incorporation of [35S]methionine/cysteine into protein in a dose-dependent manner, with maximal inhibition of 68% observed at 10 μM, and an EC50 of ~3 μM.

[1]. Coffey RT, et al. Ubiquilin-mediated Small Molecule Inhibition of Mammalian Target of Rapamycin Complex 1 (mTORC1) Signaling. J Biol Chem. 2016 Mar 4;291(10):5221-33.

Rapamycin (Sirolimus) | Torin 1 | MHY1485 | Sapanisertib (MLN0128) | AZD8055 | Dactolisib (BEZ235) | Vistusertib (AZD2014) | Torkinib (PP242) | LY3023414 | Torin 2 | GSK2126458(GSK458) | PF-04691502 | Salidroside | PQR-309 | OSI-027