||Sirolimus is a macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses bot
||Everolimus is an inhibitor of cell proliferation and immunosuppressive agent that is used alone or in combination with calcineurin inhibitors to prevent cellular rejection after organ transplantation, and in combination with other anticancer agents as treatment of advanced renal cell and other cance
||INK 128 is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.
||AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells) with excellent selectivity ( about 1,000-fold) against ATM/DNA-PK and PI3K isoforms.
||GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
||MHY1485 is a mTOR activator. It inhibits the autophagic process by inhibition of fusion between autophagosomes and lysosomes, leading to the accumulation of LC3II protein and enlarged autophagosomes.
||Apitolisib (GDC-0980, RG7422)
||Apitolisib, an effective, class I PI3K inhibitor for PI3Kα（IC50=5 nM）, PI3Kβ（IC50=27 nM）, PI3Kδ（IC50=7 nM）, PI3Kγ （IC50=14 nM）, is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.
||AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
||AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
||Gedatolisib is a highly effective dual inhibitor targeting the PI3Kα/γ (IC50: 0.4/5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K/mTOR signaling pathway.
||Pictilisib has been used in trials studying the treatment of Solid Cancers, Breast Cancer, Advanced Solid Tumours, Metastatic Breast Cancer, and Non-Hodgkin's Lymphoma, Solid Cancers, among others.
||PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
||ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
||Tacrolimus is a macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.
||Temsirolimus is a specific mTOR inhibitor, used in the treatment of advanced renal cell cancer.
||Dactolisib is an orally bioavailable imidazoquinoline targeting the phosphatidylinositol 3 kinase (PI3K) and the mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
||GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
||PP 242 is a specific and ATP competitive mTOR inhibitor (IC50=8 nM).
||PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
||LY303511, an inactive analogue of LY294002, is a mTOR inhibitor and no inhibition for PI3-K.
||KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
||PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
||CH5132799 has been used in trials studying the treatment of Solid Tumors.
||KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
||Palomid 529 has been used in trials studying the treatment of Age-Related Macular Degeneration.
||MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
||CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. CC-223 is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivi
||Timosaponin AIII induces autophagy in HeLa cells followed by apoptotic cell death (IC50: 10μM). The Timosaponin AIII cellular response is mediated via inhibition of mTORC1 and induction of ER stress (IC50: 2.5µM, BT474 cells; 6µM, MDAMB231). The Timosaponin AIII pro-apoptotic response is selectiv
||CZ415 is a potent and highly selective mTOR inhibitor.
||CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
||PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R.
||GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor.
||GDC-0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC-0084 specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and
||SF2523 is a highly selective and potent inhibitor.
||Desmethyl-VS-5584 is a dimethyl analog of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
||XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
||Zotarolimus, an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).
||Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
||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.
||VS-5584 is a pan-PI3K/mTOR kinase inhibitor.
||NU7441 (KU-57788) is a highly effective and specific DNA-PK inhibitor with IC50 of 14 nM. And NU7441 can inhibit PI3K with IC50 of 5 μM.
||OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.
||Ridaforolimus is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumo
||WYE-125132 (WYE-132) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.
||GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
||WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
||WYE-354(IC50=5 nM) is an effective, selective and ATP-competitive mTOR inhibitor. It blocks mTORC2/P-AKT(S473) and mTORC1/P-S6K(T389), not P-AKT(T308). The selectivity for mTOR is higher than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
||WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
||LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. LY3023414 has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.
||LY303511 (NV-128)is a potent mTOR inhibitor