mTOR | 陶素生化

mTOR

T1537	Rapamycin	Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells).
T1784	Everolimus	Everolimus is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.
T1838	INK 128	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.
T1859	AZD8055	AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
T1861	Omipalisib	GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
T1908	MHY1485	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 enlar
T1916	Apitolisib	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
T1958	AZ20	AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
T1961	Vistusertib	AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
T1970	Gedatolisib	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.
T2083	PI3065	PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
T2084	ETP46464	ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
T2144	Tacrolimus	Tacrolimus can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.
T2145	Temsirolimus	Temsirolimus is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.
T2235	Dactolisib	Dactolisib is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).
T2357	GSK1059615	GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
T2414	Torkinib	Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
T2415	PP121	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-P
T2434	LY 303511	LY303511, an inactive analogue of LY294002, is a mTOR inhibitor and no inhibition for PI3-K.
T2475	KU0063794	KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
T2616	PIK93	PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
T2619	CH5132799	CH5132799 has been used in trials studying the treatment of Solid Tumors.
T2685	KU55933	KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
T2706	Palomid 529	Palomid 529 has been used in trials studying the treatment of Age-Related Macular Degeneration.
T3153	Serabelisib	MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
T3351	CC223	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
T3395	Timosaponin AIII	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 ind
T3514	CZ415	CZ415 is a potent and highly selective mTOR inhibitor.
T3541	CC115	CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
T3692	GNE 477	GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor.
T3705	GDC0084	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, th
T3986	SF2523	SF2523 is a highly selective and potent inhibitor.
T4199	Desmethyl-VS-5584	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.
T6030	XL388	XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
T6033	Zotarolimus	Zotarolimus, an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).
T6045	Torin 1	Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
T6100	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 To
T6103	VS5584	VS-5584 is a pan-PI3K/mTOR kinase inhibitor.
T6319	OSI027	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
T6334	Ridaforolimus	Ridaforolimus is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits t
T6510	GDC0349	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.
T6731	WYE354	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
T6732	WYE687	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
T6883	LY3023414	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, CO
T4423	LY303511 hydrochloride	LY303511 (NV-128)is a potent mTOR inhibitor
T4488	GSK25	GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (
T4639	MSDC 0602	MSDC-0602 is an insulin sensitizer potentially for the treatment of diabetes.
T1920	Capivasertib	Capivasertib (AZD5363) is a new-type orally available inhibitor of the serine/threonine protein kinase AKT (IC50s: 3/7/7 nM for Akt1/2/3).
T5338	mTOR inhibitor-1	C-4 is a potential ATP-competitive inhibitor of mTOR. C-4 could inhibit cell growth and proliferation.
T5472	PQR620	PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1/2.
T7166	GNE-493	GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3
T2265	PI3K-IN-2	PI3K-IN-2 is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta
T6143	PI103	PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).
T2998	Dihydromyricetin	Dihydromyricetin is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of 48 μM. Dihydromyri
TN1245	3-Deoxysappanchalcone	3-Deoxysappanchalcone is an effective HO-1 inducer at the translational level.
TN1140	Onjisaponin B	Onjisaponin B induces autophagy via the AMPK-mTOR signaling pathway, increases the NGF level and accelerates both the removal of mutant huntingtin and A53T α±-synuclein, it may h
TN2118	Pulsatilla saponin D	Pulsatilla saponin D exhibits anticancer activities in various cancer types, it Inhibits autophagic flux and synergistically enhances the anticancer activity of chemotherapeutic ag
TN2250	Syringaresinol	(-)-Syringaresinol may be a potential chemotherapeutic agent for the treatment of cancer; it against H/R-induced cardiomyocyte injury and death, the degradation of HIF-1α± throug
TN2328	Zeylenone	Zeylenone has good antitumor efficacy, it inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways. Zeylenone shows inhibito
T12123	mTOR inhibitor-3	mTOR inhibitor-3 is an inhibitor of remarkably selective mTOR (Ki : 1.5 nM)
T12124	mTOR inhibitor-2	mTOR inhibitor-2 is an inhibitor of selective and oral mTOR (IC50 of 7 nM).
T12270	NV-5138	NV-5138 is a selective and orally active activator of brain mTORC1, with antidepressant effects.
T14033	3BDO	3BDO is an activator of mTOR. It can also inhibit autophagy..
T14552	Dactolisib Tosylate	Dactolisib Tosylate (BEZ235 Tosylate) is an inhibitor of dual PI3K and mTOR kinase(IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively). Dactolisib Tosylate also inh
T11328	FT-1518	FT-1518 ,exhibits antitumor activity, is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor.
T11742L	K-7174 dihydrochloride	K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
T16263	N6-Cyclopentyladenosine	N6-Cyclopentyladenosine (CPA) is a selective agonist of Adenosine A1 receptor (Ki: 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively).
T8569	DMH-25	DMH25 is a novel covalent and potent inhibitor of mTOR and shows in vivo antitumor activity against triple-negative breast cancer cells.
T2S1040	Jolkinolide B	Jolkinolide B has potent anti-inflammatory, and antitumor activities, it is able to enhance apoptosis of human leukemic HL-60 and THP-1 cells, at least in part, through downregulat
T3851	Vicenin -2	Vicenin -2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen
T3S0209	Vincristine	Vincristine-induced nociceptive painful sensation, may be due to its potential of antioxidative, neuroprotective and calcium channel inhibitory action.Vincristine can treat MM, ERK
TN3218	7-(4-Hydroxyphenyl)-1-phenyl-4-hepten-3-one	7-(4-Hydroxyphenyl)-1-phenyl-4-hepten-3-one as a beneficial compound to ameliorate the deleterious effects of Aβ on dendrite integrity and cell survival, and may provide new insig
TN3310	9,9'-Di-O-(E)-feruloylsecoisolariciresinol	1,4-O-Diferuloylsecoisolariciresinol(9,9'-Di-O-(E)-feruloylsecoisolariciresinol),and pierreione B, two novel inhibitors of mTOR signaling, have strong anticancer activity. (+)-9,9'
TN4213	Hirsutenone	Hirsutenone has potent antioxidant activity, it shows significant free radical scavenging activity and exhibits inhibition effect on the mitochondrial lipid peroxidation.Hirsutenon
TN4356	Jolkinolide A	Jolkinolide A has anti-tumor activity. It inhibited VEGF expression in A549 cells through the inhibition of the Akt-STAT3-mTOR signaling pathway, and directly inhibited the prolife
TN4382	Kazinol A	Kazinol A shows strong inhibition of arachidonic acid (AA)-induced platelet aggregation. It also exhibits potent inhibition with IC50 values ranging 0.6-164 M against XOD. Kazinol
TN4788	Pierreione B	Pierreione B is an inhibitor of mTOR signaling with strong anticancer activity. Pierreione A and Pierreione B demonstrate solid tumor selectivity with minimal cytotoxicity.
TN5050	Sprengerinin C	Sprengerinin C exerts anti-tumorigenic effects in hepatocellular carcinoma via inhibition of proliferation and angiogenesis and induction of apoptosis, it can strongly suppress tum
TMA0507	Tomatidine	Tomatidine shows antibiotic, and anti-inflammatory activities, it significantly suppresses the activity of ACAT and leads to reduction of atherogenesis. Tomatidine inhibits the inv
T8649	TMBIM6 antagonist-1	TMBIM6 antagonist-1 is an antagonist of TMBIM6.