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阿拉丁PI3K/Akt/mTOR信號(hào)通路（二）
PI3K/AKT/mTOR
PI3K/AKT/mTOR是調(diào)節(jié)細(xì)胞周期的重要細(xì)胞內(nèi)信號(hào)通路,。PI3K/AKT/mTOR信號(hào)通路與細(xì)胞的生長(zhǎng)、存活,、增殖,、凋亡、血管生成,、自吞噬過(guò)程中發(fā)揮著重要的生物學(xué)功能,。該通路是由磷脂酰肌醇3- 激酶（PI3Ks）、絲氨酸/蘇氨酸蛋白激酶（Akt）和哺乳動(dòng)物雷帕霉素靶蛋白（mTOR）組成,。
PI3K/Akt/mTOR通路過(guò)程
PI3K激活后產(chǎn)生PIP3, PIP3促使PDK1(phosphoinositide dependent kinase-1)磷酸化含有PH結(jié)構(gòu)域的信號(hào)AKT蛋白（Ser308）,，從而活化AKT。AKT有很多下游效應(yīng)，可通過(guò)磷酸化多種酶,、激酶和轉(zhuǎn)錄因子等下游因子,，進(jìn)而調(diào)節(jié)細(xì)胞的功能。mTOR,，是PI3K/Akt 下游的一種重要的絲氨酸-蘇氨酸蛋白激酶,，調(diào)節(jié)腫瘤細(xì)胞的自噬的經(jīng)典通路。
PI3K/Akt/mTOR信號(hào)通路圖
產(chǎn)品列表
按靶點(diǎn)分類：
*GSK-3
糖原合成酶激酶-3 (GSK-3)是一種絲氨酸/蘇氨酸激酶,，可調(diào)控糖原合成酶(GS ) 的活性,、也作用于眾多信號(hào)蛋白結(jié)構(gòu)蛋白和轉(zhuǎn)錄因子，調(diào)節(jié)細(xì)胞的分化,、增殖,、存活和凋亡。
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | IC50 | Ki |
|---|---|---|---|---|---|---|---|---|
| S129716 | SB216763 | ≥98% | 280744-09-4 | 5mg,10mg,50mg | GSK-3α | 34.3 nM | ||
| C129718 | CHIR-98014 | ≥99% | 252935-94-7 | 5mg,25mg | 無(wú)細(xì)胞 | GSK-3α | 0.65 nM | |
| GSK-3β | 0.58 nM | |||||||
| T126075 | TWS119 | ≥95% | 601514-19-6 | 10mg,25mg,50mg | 無(wú)細(xì)胞 | GSK-3β | 30 nM | |
| T127039 | Tideglusib | ≥98% | 865854-05-3 | 5mg,25mg,100mg | 無(wú)細(xì)胞 | GSK-3β | 60 nM | |
| S129720 | SB415286 | ≥99% | 264218-23-7 | 10mg,50mg | GSK3α | 78 nM | 31 nM | |
| B129724 | BIO | ≥98% | 667463-62-9 | 10mg,50mg | 無(wú)細(xì)胞 | GSK-3α | 5 nM | |
| GSK-3β | 5 nM | |||||||
| C125082 | CHIR-99021 | ≥98% | 252917-06-9 | 5mg,25mg | GSK-3α | 10 nM | ||
| GSK-3β | 6.7 nM | |||||||
| A126819 | AZD2858 | ≥99% | 486424-20-8 | 10mg,50mg | GSK-3 | 68 nM | ||
| A126905 | AZD1080 | ≥98% | 612487-72-6 | 5mg,25mg | GSK3α | 6.9 nM | ||
| GSK3β | 31 nM | |||||||
| A126821 | AR-A014418 | ≥98% | 487021-52-3 | 5mg,10mg,50mg | GSK3β | 104 nM | 38 nM | |
| T126722 | TDZD-8 | ≥98% | 327036-89-5 | 5mg,25mg,100mg | GSK-3β | 2 Μm | ||
| L126079 | LY2090314 | ≥98% | 603288-22-8 | 5mg,25mg,100mg | GSK-3α | 1.5 nM | ||
| GSK-3β | 0.9 nM | |||||||
| I111268 | 靛玉紅 | 95% | 479-41-4 | 50mg | 細(xì)胞周期依賴性激酶 | 5 μM | ||
| GSK-3β | 0.6 μM | |||||||
| I140424 | 靛玉紅 | 分析標(biāo)準(zhǔn)品,≥98% | 479-41-4 | 10mg | 細(xì)胞周期依賴性激酶 | 5 μM | ||
| GSK-3β | 0.6 μM | |||||||
| I111267 | 靛玉紅 | 分析標(biāo)準(zhǔn)品,≥95% | 479-41-4 | 10mg,20mg | 細(xì)胞周期依賴性激酶 | 5 μM | ||
| GSK-3β | 0.6 μM | |||||||
| D167318 | 2-D08 | 98% (HPLC) | 144707-18-6 | 5mg,25mg | Axl | 0.49 nM | ||
| IRAK4 | 3.9 nM | |||||||
| ROS1 | 5.3 nM | |||||||
| MLK4 | 9.8 nM | |||||||
| GSK3β | 11 nM | |||||||
| RET | 11 nM | |||||||
| KDR | 17 nM | |||||||
| PI3Kα | 35 nM | |||||||
| B152410 | Bikinin | ≥98.0% | 188011-69-0 | 5mg,25mg,100mg | GSK-3 | |||
*ATM/ATR
ATM/ATR是絲氨酸-蘇氨酸激酶PI3家族的成員,，是DNA損傷反應(yīng)的傳感器和效應(yīng)器,。ATM和ATR磷酸化常見(jiàn)的以及特定的底物來(lái)激活檢查點(diǎn)信號(hào)，并調(diào)節(jié)G1,、S和G2細(xì)胞周期檢查點(diǎn),。
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | IC50 | Ki | ED50 |
|---|---|---|---|---|---|---|---|---|---|
| B126286 | BEZ235 | ≥99% | 915019-65-7 | 25mg,100mg | 無(wú)細(xì)胞 | p110α | 4 nM | ||
| p110γ | 5 nM | ||||||||
| p110δ | 7 nM | ||||||||
| p110β | 75 nM | ||||||||
| mTOR(p70S6K) | 6 nM | ||||||||
| 3T3TopBP1-ER | ATR | 21 nM | |||||||
| K126884 | KU-55933 (ATM Kinase Inhibitor) | ≥98% | 587871-26-9 | 5mg,25mg,100mg | 無(wú)細(xì)胞 | ATM | 12.9 nM | 2.2 nM | |
| K127121 | KU-60019 | ≥98% | 925701-49-1 | 5mg,25mg,100mg | 無(wú)細(xì)胞 | ATM | 6.3 nM | ||
| V125220 | VE-821 | ≥98% | 1232410-49-9 | 5mg,25mg,100mg | 無(wú)細(xì)胞 | ATR | 26 nM | 13 nM | |
| W100984 | Wortmannin | 98% | 19545-26-7 | 5mg,10mg,25mg | 無(wú)細(xì)胞 | PI3K | 3 nM | ||
| DNA-PK | 16 nM | ||||||||
| ATM | 150 nM | ||||||||
| T129646 | Torin 2 | ≥98% | 1223001-51-1 | 5mg,10mg,50mg | p53−/− MEFs細(xì)胞系 | mTOR | 0.25 nM | ||
| PC3細(xì)胞系 | ATM | 28 nM | |||||||
| ATR | 35 nM | ||||||||
| DNA-PK | 118 nM | ||||||||
| C128014 | CP-466722 | ≥98% | 1080622-86-1 | 5mg,25mg | |||||
| E125288 | ETP-46464 | ≥99% | 1345675-02-6 | 10mg,50mg | ATR | 25 nM | |||
| C129735 | CGK 733 | ≥99% | 905973-89-9 | 5mg,10mg,50mg | ATM/ATR | 200 nM | |||
| A125603 | AZ20 | ≥98% | 1233339-22-4 | 5mg,10mg,50mg | 無(wú)細(xì)胞 | ATR | 5 nM | ||
| S117968 | 五味子乙素 | 分析標(biāo)準(zhǔn)品,>98% | 61281-37-6 | 20mg,25mg,100mg | ATR和P-gp | ||||
| C129284 | Chloroquine Phosphate | ≥99% | 50-63-5 | 5g,10g,25g,100g,500g | ATM | ||||
*PDK-1
PDK-1是此通路的主要激酶，可激活A(yù)KT/PKB和許多其他AGC激酶（包括PKC,，S6K,，SGK）。
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | IC50 | Ki |
|---|---|---|---|---|---|---|---|---|
| O126958 | OSU-03012 (AR-12) | ≥98% | 742112-33-0 | 5mg,25mg,100mg | 無(wú)細(xì)胞 | PDK-1 | 5 μM | |
| B126947 | BX-795 | ≥97% | 702675-74-9 | 10mg,50mg,100mg | 無(wú)細(xì)胞 | PDK1 | 6 nM | |
| B126138 | BX-912 | ≥97% | 702674-56-4 | 5mg,25mg,100mg | 無(wú)細(xì)胞 | PDK1 | 12 nM | |
| P127286 | PHT-427 | ≥98% | 1191951-57-1 | 10mg,50mg | Akt | 2.7 μM | ||
| PDPK1 | 5.2 μM | |||||||
| G126481 | GSK2334470 | ≥98% | 1227911-45-6 | 10mg,50mg | 無(wú)細(xì)胞 | PDK1 | 10 nM |
*S6 Kinase
RSK（核糖體s6激酶）家族成員,。RSK有兩個(gè)亞家族,，p90rsk（也稱為MAPK激活蛋白激酶-1，MAPKAP-K1）和p70rsk（也稱為S6-H1激酶或簡(jiǎn)稱S6激酶）,。
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | IC50 | Ki |
|---|---|---|---|---|---|---|---|---|
| A126209 | AT7867 | ≥98% | 857531-00-1 | 5mg,10mg,50mg | 無(wú)細(xì)胞 | Akt1 | 32 nM | |
| Akt2 | 17 nM | |||||||
| Akt3 | 47 nM | |||||||
| p70S6K | 85 nM | |||||||
| PKA | 20 nM | |||||||
| E129765 | PF-4708671 | ≥99% | 1255517-76-0 | 5mg,10mg,25mg | 無(wú)細(xì)胞 | S6 kinase(S6K1亞型) | 160 nM | 20 nM |
| H129712 | H 89 2HCl | ≥99% | 130964-39-5 | 10mg,50mg | 無(wú)細(xì)胞 | PKA | 48 nM |
*AMPK
AMPK（AMP活化蛋白激酶）是一種在細(xì)胞能量穩(wěn)態(tài)中起作用的酶,，調(diào)節(jié)幾種細(xì)胞內(nèi)系統(tǒng)的代謝，包括葡萄糖的細(xì)胞吸收,，脂肪酸的β-氧化和葡萄糖轉(zhuǎn)運(yùn)蛋白4（GLUT4）和線粒體的生物發(fā)生,。
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | Ki | EC50 |
|---|---|---|---|---|---|---|---|---|
| D129758 | Dorsomorphin 2HCl | ≥98% | 1219168-18-9 | 5mg,10mg,50mg | 無(wú)細(xì)胞 | AMPK | 109 nM | |
| D139352 | Dorsomorphin | ≥98% | 866405-64-3 | 5mg,25mg,100mg | 無(wú)細(xì)胞 | AMPK | 109 nM | |
| A127825 | A-769662 | ≥98% | 844499-71-4 | 5mg,10mg,50mg | 無(wú)細(xì)胞 | AMPK | 0.8 μM | |
| A129749 | Acadesine | ≥98% | 2627-69-2 | 50mg,250mg,1g | AMPK | |||
| P102146 | 苯乙雙胍鹽酸鹽 | 97% | 834-28-6 | 1g,5g | AMPK | |||
| A111884 | 腺苷-5'-磷酸 | from yeast,≥97% | 18422-05-4 | 5g,25g,100g | AMPK |
*DNA-PK
DNA依賴性蛋白激酶（DNA-PK）是絲/蘇氨酸蛋白激酶，屬于PI3K的相關(guān)激酶(PIKK)家族成員,。參與非同源末端連接(NHEJ)通路,，也和ATR/ATM協(xié)同磷酸化DNA損傷檢查點(diǎn)的蛋白。
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | IC50 |
|---|---|---|---|---|---|---|---|
| P125961 | PI-103 | ≥98% | 371935-74-9 | 10mg,50mg,100mg | 無(wú)細(xì)胞 | p110α | 2 nM |
| p110β | 3 nM | ||||||
| p110δ | 3 nM | ||||||
| p110γ | 15 nM | ||||||
| mTOR | 30 nM | ||||||
| DNA-PK | 23 nM | ||||||
| K126842 | NU7441 (KU-57788) | ≥98% | 503468-95-9 | 5mg,25mg,100mg | 無(wú)細(xì)胞 | DNA-PK | 14 nM |
| PI3K | 5 μM | ||||||
| P125966 | PIK-75 | ≥98% | 372196-77-5 | 10mg,50mg,100mg | p110α | 5.8 nM | |
| 無(wú)細(xì)胞 | DNA-PK | 2 nM | |||||
| N129741 | NU7026 | ≥98% | 154447-35-5 | 10mg,50mg | 無(wú)細(xì)胞 | DNA-PK | 0.23 μM |
| P126419 | PP121 | ≥98% | 1092788-83-4 | 10mg,50mg | PDGFR | 2 nM | |
| Hck | 8 nM | ||||||
| mTOR | 10 nM | ||||||
| VEGFR2 | 12 nM | ||||||
| Src | 14 nM | ||||||
| Abl | 18 nM | ||||||
| DNA-PK | 60 nM | ||||||
| K129743 | KU-0060648 | ≥99% | 881375-00-4 | 2mg,25mg | DNA-PK | 8.6 nM | |
| PI3Kα | 4 nM | ||||||
| PI3Kβ | 0.5 nM | ||||||
| PI3Kδ | 0.1 nM | ||||||
| PI3Kγ | 0.59 μM |
*PI4K
磷脂酰肌醇4激酶（PI4Ks）參與合成磷脂酰肌醇4磷酸酯（PI4P）,，屬于磷脂酰肌醇家族,。
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 靶點(diǎn) | IC50 |
|---|---|---|---|---|---|---|
| P126888 | PIK-93 | ≥96% | 593960-11-3 | 5mg,25mg,100mg | PI4KIIIβ | 19 nM |
| PI3Kα | 39 nM |