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哺乳动物雷帕霉素靶蛋白(mammalian target ofrapamycin, mTOR)是一种非典型的丝氨酸/苏氨酸蛋白激酶，mTOR 信号通路由于处于生长调节的中心环节而倍受关注。
TOR 基因是于1991 年在酵母作为雷帕霉素(rapamycin) 靶蛋白被发现，与酵母TOR 结构和功能相应的哺乳动物TOR 称mTOR，TOR 的基因序列从酵母到哺乳动物都十分保守，在氨基酸水平具有95% 的同源性。mTOR 是一不典型的丝氨酸/ 苏氨酸蛋白激酶，分子量大小为 289kDa。mTOR 是PIKK (phosphoinositide kinase-related kinase)家族成员之一。
mTOR 抑制剂
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| 目录 |
产品名称 |
产品描述 |
| S1009 |
BEZ235 (NVP-BEZ235) |
BEZ235是ATP竞争性的PI3K和mTOR抑制剂，作用于p110α, p110γ, p110δ 和 p110β的IC50分别为4, 5, 7和75 nM。 |
| S1120 |
Everolimus (RAD001) |
Everolimus (RAD001) also known as SDZ-RAD, Certican, Zortress and Afinitorm is an mTOR inhibitor available at Selleck with IC50 of 0.63 nM. |
| S1039 |
Rapamycin (Sirolimus) |
Rapamycin also known as Sirolimus & Rapamune is an mTOR inhibitor. Rapamycin Sirolimus inhibits cell motility by suppression of mTOR-mediated pathways. |
| S1038 |
PI-103 |
PI-103有效抑制PI3K，可穿透细胞，是ATP竞争性抑制剂。PI-103作用于DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β,和p110γ时IC50分别为2, 8, 20, 26, 48, 83, 88, 150 nM。 |
| S1044 |
Temsirolimus (Torisel) |
Temsirolimus (Torisel) is a mTOR inhibitor. |
| S1555 |
AZD8055 |
AZD8055是新型ATP竞争性抑制剂，作用于mTOR激酶时IC50为0.8 nM。 |
| S1226 |
Ku-0063794 |
Ku-0063794 is an mTOR inhibitor, IC50 ~10 nM for mTORC1 and mTORC2, respectively. |
| S2743 |
PF-04691502 |
PF-04691502 is a potent and selective dual PI3K/mTOR inhibitor to phosphorylation of AKT T308 and AKT S473 with IC50 of 7.5 and 3.8 nM, respectively. |
| S2699 |
CH5132799 |
CH5132799 is a novel and selective class I PI3K inhibitor with IC50 of 0.014, 0.12, 0.5, 0.036, 5.3 and 1.6 μM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, PI3K C2β and mTOR, respectively. |
| S2696 |
GDC-0980 (RG7422) |
GDC-0980 (RG7422) is a selective, dual PI3 Kinase and mTOR inhibitor with IC50 of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively. |
| S2668 |
WYE-687 |
WYE-687 is a potent ATP-competitive mTOR inhibitor with an IC50 of 7 nM. |
| S2661 |
WYE-125132 |
WYE-125132 is a highly potent, ATP-competitive and specific mTOR kinase inhibitor with an IC50 of 0.19 nM. |
| S2689 |
WAY-600 |
WAY-600 is a potent ATP-competitive mTOR inhibitor with an IC50 of 9 nM. |
| S2658 |
GSK2126458 |
GSK2126458 is a highly potent PI3K and mTOR inhibitor with an app Ki of 19 pM for PI3K. |
| S2628 |
PKI-587 |
PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively. |
| S2624 |
OSI-027 |
OSI027 is a potent mammalian target of rapamycin (mTOR) kinase inhibitor. |
| S2622 |
PP-121 |
PP121 is a multitargeted dual receptor tyrosine kinases inhibitor with IC50 of 0.052, 1.4, 0.15, 1.1, 0.06, 0.01and 0.002 μM for p110α, p110β, p110δ, p110γ, DNA-PK, mTOR and PDGFR, respectively. |
| S2238 |
Palomid 529 (P529) |
Palomid 529 (P529) is a novel PI3K/Akt/mTOR inhibitor with a GI50 of <35 μM in the NCI-60 cell lines panel. |
| S2218 |
PP242 |
PP242 is a novel selective mTOR inhibitor with an IC50 of 8 nM. |
| S2406 |
Chrysophanic acid (Chrysophanol) |
Chrysophanic acid (Chrysophanol) is a EGFR/mTOR pathway inhibitor. |
| S1523 |
XL765 |
XL765是第一个口服的PI3K和mTOR双重抑制剂，作用于p110α, β, γ, δ, 和mTOR时IC50分别为39, 113, 9, 43, 和～150 nM。 |
| S1360 |
GSK1059615 |
GSK1059615 is a pan-PI3K reversible inhibitor,IC50:PI3Kα(0.4 nM), β (0.6 nM),γ (5 nM),δ (2 nM) and mTOR(12 nM). |
| S1266 |
WYE-354 |
WYE-354 is an mTOR inhibitor with an IC50 of 5 nM. |
| S1022 |
Deforolimus (Ridaforolimus) |
Deforolimus (Ridaforolimus) is a small-molecule inhibitor of mTOR. |
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