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mTOR抑制劑

2012/4/30 23:28:46  作者:labgogo


    哺乳動(dòng)物雷帕霉素靶蛋白(mammalian target ofrapamycin, mTOR)是一種非典型的絲氨酸/蘇氨酸蛋白激酶,mTOR 信號(hào)通路由于處于生長(zhǎng)調(diào)節(jié)的中心環(huán)節(jié)而倍受關(guān)注。

  TOR 基因是于1991 年在酵母作為雷帕霉素(rapamycin) 靶蛋白被發(fā)現(xiàn),與酵母TOR 結(jié)構(gòu)和功能相應(yīng)的哺乳動(dòng)物TOR 稱mTOR,TOR 的基因序列從酵母到哺乳動(dòng)物都十分保守,在氨基酸水平具有95% 的同源性。mTOR 是一不典型的絲氨酸/ 蘇氨酸蛋白激酶,分子量大小為 289kDa。mTOR 是PIKK (phosphoinositide kinase-related kinase)家族成員之一。

mTOR 抑制劑

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目錄 產(chǎn)品名稱 產(chǎn)品描述
S1009 BEZ235 (NVP-BEZ235) BEZ235是ATP競(jìng)爭(zhēng)性的PI3K和mTOR抑制劑,作用于p110α, p110γ, p110δ 和 p110β的IC50分別為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,可穿透細(xì)胞,是ATP競(jìng)爭(zhēng)性抑制劑。PI-103作用于DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β,和p110γ時(shí)IC50分別為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競(jìng)爭(zhēng)性抑制劑,作用于mTOR激酶時(shí)IC50為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是第一個(gè)口服的PI3K和mTOR雙重抑制劑,作用于p110α, β, γ, δ, 和mTOR時(shí)IC50分別為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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