mTOR
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB08711 | Zotarolimus | 221877-54-9 | Zotarolimus is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM. |
| FB08060 | XL388 | 1251156-08-7 | XL388 is a potent and selective ATP-competitive mTOR inhibitor with IC50 value of 9.9 nM. |
| FB08588 | WYE-687 | 1062161-90-3 | WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM showing > 100 fold selectivity for mTOR than PI3Kα/γ. |
| FB06554 | WYE-354 | 1062169-56-5 | WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K (T389) and mTORC2/P-AKT (S473) not P-AKT (T308), selective for mTOR than PI3Kα (> 100-fold) and PI3Kγ (> 500-fold). |
| FB08607 | WYE-125132 | 1144068-46-1 | WYE-125132 is a highly potent, ATP-competitive and specific mTOR kinase inhibitor with an IC50 of 0.19 nM, highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR. |
| FB01435 | WAY-600 | 1062159-35-6 | WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM and blocks mTORC1/P-S6K (T389) and mTORC2/P-AKT (S473) but not P-AKT (T308). It is selective for mTOR than PI3Kα (> 100-fold) and PI3Kγ (> 500-fold). |
| FB08976 | Ridaforolimus | 572924-54-0 | Treatment of HT-1080 cells with Deforolimus induces a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50 of 0.2 nM and 5.6 nM, respectively, and leads to a decrease in cell size, an increase in the proportion of cells in the G1 phase of the cell cycle, and inhibition of glucose uptake. |
| FB07035 | Torin 2 | 1223001-51-1 | Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM, showing 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties and inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM, respectively. |
| FB01112 | Torin 1 | 1222998-36-8 | Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM exhibiting 1000-fold selectivity for mTOR than PI3K. |
| FB09688 | Temsirolimus | 162635-04-3 | Temsirolimus directly inhibits mTOR kinase activity with IC50 values of 1.76 ± 0.15 μM. |
| FB17232 | SAFit2 | 1643125-33-0 | SAFit2 is a novel selective antagonist of the FK506-binding protein 51 with Ki value of 6nM. |
| FB07750 | Rapamycin | 53123-88-9 | Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM. |
| FB11545 | RapaLink-1 | 1887095-82-0 | RapaLink-1 is the third-generation mTOR inhibitor exploiting the unique juxtaposition of two drug (first- and second-generation mTOR kinase inhibitors) –binding pockets to create a bivalent interaction that allows inhibition of the mutants which has resistance to the previous TORKi (mTOR kinase inhibitors). |
| FB02377 | QL-IX-55 | 1223002-54-7 | QL-IX-55 is a selective ATP-competitive inhibitor of mTORC1/2 with IC50s of 50/50/10-50 nM for Human mTORC1/Yeast mTORC1/Yeast mTORC2, respectively. |
| FB15274 | PWT33597 mesylate | 1246203-36-0 | PWT33597 is a dual inhibitor of PI3K alpha and mTOR with selectivity for PI3K alpha (IC50 = 26 nM) over PI3K delta (IC50 = 291 nM) but also displaying activity against mTOR in biochemical assays (IC50 = 21 nM). It had good pharmacokinetic properties in multiple preclinical species. |
| FB10131 | PQR620 | 1927857-56-4 | PRQ620 is a highly potent and selective mTORC1/2 inhibitor, shows anti-tumor effects in vitro and in vivo. |
| FB03012 | PP242 | 1092351-67-1 | PP 242 is the first selective and ATP competitive mTOR inhibitor with IC50 of 8 nM. |
| FB09788 | Palomid 529 | 914913-88-5 | Palomid 529 is a novel dual mTORC1/2 inhibitor. |
| FB08950 | OSI-027 | 936890-98-1 | OSI-027 shows the selective and ATP competitive inhibition activities against mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively. |
| FB07684 | Nordihydroguaiaretic Acid | 500-38-9 | Nordihydroguaiaretic Acid is a naturally occuring mTORC1 inhibitor. |
| FB17786 | Niclosamide olamine | 1420-04-8 | Niclosamide olamine is an anthelmintic that disrupts mitochondrial metabolism in parasitic worms and animal models. Niclosamide olamine inhibits STAT3 (IC50 = 0.25 μM) and stimulates autophagy by reversibly inhibiting mammalian target of Rapamycin complex 1 (mTORC1) signaling. |
| FB02355 | mTOR-IN-1 | 1207358-59-5 | mTOR-IN-1 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 1.5 nM. |
| FB18263 | mTOR inhibitor-1 | 468747-17-3 | mTOR inhibitor-1 is an ATP-competitive inhibitor of mTOR. It suppressed A549 cell proliferation and induced autophagy. |
| FB01597 | MHY1485 | 326914-06-1 | MHY1485 is a mTOR activator and inhibits the autophagic process by inhibition of fusion between autophagosomes and lysosomes leading to the accumulation of LC3II protein and enlarged autophagosomes. |
| FB03288 | LY303511 | 154447-38-8 | LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K. |
| FB10135 | LY303511 HCl | 2070014-90-1 | LY303511 HCl is an analogue of LY294002 which can inhibit mTOR-dependent phosphorylation of S6K, but not PI3K-dependent phosphorylation of Akt. It also blocks voltage-gated potassium (Kv) channels with IC50 value of 64.6 μM. |
| FB16204 | L-Leucine | 61-90-5 | Leucine is one of nine essential amino acids in humans which is important for protein synthesis and many metabolic functions. It contributes to regulation of blood-sugar levels growth and repair of muscle and bone tissue growth hormone production and wound healing. |
| FB03821 | KU-0063794 | 938440-64-3 | KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively) with no effect on PI3Ks. |
| FB08617 | INK-128 | 1224844-38-5 | INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM and is > 200-fold less potent to class I PI3K isoforms. |
| FB08057 | GDC-0349 | 1207360-89-1 | GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, showing > 700-fold selectivity over PI3Kα and other 266 kinases. |
| FB11848 | FT-1518 | 1313026-58-2 | FT-1518 is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor, and exhibits antitumor activity. |
| FB04789 | Everolimus | 159351-69-6 | Everolimus is a mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM. |
| FB04789 | Everolimus | 159351-69-6 | Everolimus is a mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM. |
| FB08672 | ETP-46464 | 1345675-02-6 | ETP-46464 is a cell-permeable quinoline-containing heterotricyclic compound that acts as a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα, and ATM (IC50= 0.6, 14, 36, 170, and 545 nM, respectively). |
| FB10130 | CZ415 | 1429639-50-8 | CZ415 is a potent and highly selective ATP-competitive mTOR inhibitor with pKdapp value of 8.2. |
| FB02386 | CC-223 | 1228013-30-6 | CC-223 is a potent mTOR kinase inhibitor (IC50=16 nM), with > 150-fold sensitivity over the related lipid kinase PI3Kα (IC50=4 μM). |
| FB00106 | AZD8055 | 1009298-09-2 | AZD8055 is an ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (～1,000-fold) against PI3K isoforms and ATM/DNA-PK. |
| FB01075 | AZD2014 | 1009298-59-2 | AZD2014 is an mTOR inhibitor with IC50 of 2.8 nM and is highly selective against multiple PI3K isoforms (α/β/γ/δ). |
| FB12263 | AZD 3147 | 1101810-02-9 | AZD 3147 is a potent and selective dual mTORC1 and 2 inhibitor with IC50 of 1.5 nM. |
| FB04050 | AP20187 | 195514-80-8 | AP20187 is a synthetic, cell-permeable ligand that can be used to induce homodimerization of fusion proteins containing the DmrB domain. |
| FB04049 | AP1903 | 195514-63-7 | AP1903 is a homodimer binding to FKBP and elicites potent and dosedependent apoptotic death of engineered cell line HT1080 in culture with an EC50 of 0.1 nM. |
| FB12803 | 3BDO | 890405-51-3 | 3BDO is a new mTOR activator which can also inhibit autophagy. |