torin 2

Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM/ATR/DNA-PK inhibition is 28 nM/35 nM/118 nM, respectively.

PI3K/Akt/mTOR-IN-2 is a potent PI3K/AKT/mTOR inhibitor with anticancer effects and selectivity for MDA-MB-231 cells (IC50 2.29 μM). It induces cell cycle arrest and apoptosis in cancer cells.

Anti-virulence factor-IN-2 (compound C7) is an inhibitor targeting the virulence factor KpsM in Escherichia coli. KpsM facilitates the translocation of capsular polysaccharides to the cell surface, enabling KpsM-positive E. coli to evade phagocytosis by the scavenger receptor Marco on liver Kupffer cells, promoting bacterial dissemination. These bacteria can exacerbate ethanol-induced liver disease. Anti-virulence factor-IN-2 demonstrates anti-infective activity by inhibiting KpsM-dependent capsulation in a mouse model of ethanol-induced liver disease. This compound is applicable for alcoholic hepatitis research.

PI3K/mTOR-IN-20 is a selective dual inhibitor of PI3K/mTOR. It demonstrates nanomolar anti-proliferative effects in MRC-5 and Mlg2908 cells with IC50 values of 0.380 and 0.090 μM, respectively. In a Bleomycin-induced pulmonary fibrosis model, PI3K/mTOR-IN-20 reduces Ashcroft scores, decreases hydroxyproline content and collagen deposition, downregulates fibrosis-related protein expression, and aids in the repair of lung tissue structure. This compound exhibits good safety, as indicated by stable weight recovery in mice without significant hepatic or renal toxicity. PI3K/mTOR-IN-20 is useful for research on pulmonary fibroblasts.

Glucocorticoid receptor-IN-2 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. IC50: 0.171 nM) and also has some transcriptional activating effect on MMTV (EC50: 0.94 nM).

Masofaniten (EPI-7386) is an orally active androgen receptor (AR) inhibitor with antitumor activity for the study of prostate and breast cancers.

Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.