torin1

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

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

PI3K/mTOR-IN-17 is a dual inhibitor that targets both PI3K and mTOR, with IC50 values of 1.21 μM and 0.21 μM, respectively. It induces apoptosis mediated by caspases and arrests cell growth in the G1 phase. The compound elevates the levels of caspases-3, 7, 8, and 9, enhances p53 expression, and increases the Bax/Bcl-2 ratio. By inhibiting the PI3K/mTOR signaling pathway, PI3K/mTOR-IN-17 is applicable in cancer research, including studies on non-small cell lung cancer (NSCLC).

DEPTOR-IN-1 is an inhibitor of DEPTOR with a Kd of 9.3 μM.

Estrogen receptor-IN-1 (compound 16) is an effective estrogen receptor (ER) inhibitor with IC50 values of 13 μM for ERα and 5 μM for ERβ, respectively [1].

Glucocorticoid receptor-IN-1 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. glucocorticoid receptor-IN-1 has good transcriptional repression, acting on hMMP1 ( IC50: 2.11 nM) and also has a transcriptional activating effect on MMTV (EC50: 5.59 nM).

hIgG-hFc receptor-IN-1 is a human immunoglobulin G - human neonatal Fc receptor (hIgG-hFcRn) protein-protein interaction inhibitor (IC50: 2 μM).

HSP90/mTOR-IN-1 is an effective and orally administrable inhibitor targeting both Hsp90 and mTOR, displaying IC50 values of 69 nM and 29 nM, respectively. This compound inhibits the proliferation of SW780 cells by overly activating the PI3K/AKT/mTOR pathway and induces apoptosis and autophagy through its selective inhibition of Hsp90 and mTOR. Additionally, HSP90/mTOR-IN-1 exhibits significant anti-tumor activity in vivo and is applicable in bladder cancer research.

Epigenetic factor-IN-1 (40569Z) is an inhibitor that exhibits potent binding affinity for SIRT7 and is utilized in the study of liver cancer [1].

Akt/mTOR-IN-1 (Compound 8r) is an inhibitor of the AKT/mTOR signaling pathway, exhibiting an IC50 of 0.8 µM and possessing anticancer activity. This compound decreases the expression of Caspase 3 while enhancing the expression of the autophagic protein Cyclin B1, thereby inducing autophagy and apoptosis. Akt/mTOR-IN-1 is applicable for research in the field of non-small cell lung cancer (NSCLC).

Transcription factor-IN-1 (Compound 4e) acts as an inhibitor of transcription factors. It exhibits anticonvulsant activity by antagonizing pentylenetetrazole (PTZ) with an ED50 of 34.5 mg/kg. Additionally, Transcription factor-IN-1 demonstrates antidepressant activity in a rat model.