阿拉丁小分子抑制劑、激動劑、拮抗劑--PI3K/Akt/mTOR信號通路(一)

來源: 上海阿拉丁生化科技股份有限公司   2019-12-9   訪問量:926評論(0)

ertical-align: top; padding: 0px; box-sizing: border-box;">PI3Kγ83 nMPI3Kδ235 nMA129503AS-252424≥98%900515-16-42mg,5mg,25mg,100mg無細胞PI3Kγ30 nMN125612BGT226 (NVP-BGT226)≥98%1245537-68-15mg,25mg,100mgPI3Kα4 nMPI3Kβ63 nMPI3Kγ38 nMC126527CUDC-907≥99%1339928-25-45mg,10mg,50mgPI3Kα19 nMHDAC11.7 nMHDAC25 nMHDAC31.8 nMHDAC102.8 nMP129553PIK-294≥98%900185-02-65mg,10mg,50mg p110δ10 nMA129517AS-604850≥98%648449-76-75mg,25mg,100mg PI3Kγ250 nMG125299GSK2636771≥98%1372540-25-45mg,10mg,50mg PI3Kβ5.2 nMB129540BAY 80-6946 (Copanlisib)≥99%1032568-63-05mg,10mg,50mg,250mgPI3Kα0.5 nMPI3Kβ3.7 nMPI3Kγ6.4 nMPI3Kδ0.7 nMC127596CH5132799≥97%1007207-67-15mg,25mg,100mg PI3Kα14 nMC129600CAY10505≥99%1218777-13-910mg,25mg,50mg,250mg PI3Kγ30 nMP129615PIK-293≥97%900185-01-55mg,25mg,50mg PI3Kδ0.24 μMP127674PKI-402≥98%1173204-81-3 5mg,10mg,50mgPI3Kα2 nMPI3Kβ7 nMPI3Kγ16 nMPI3Kδ14 nMmTOR3 nMT129620TG100713≥97%925705-73-310mg,50mgPI3Kγ50 nMPI3Kδ24 nMPI3Kα165 nMPI3Kβ215 nMV125616VS-5584 (SB2343)≥98%1246560-33-710mg,50mgmTOR3.4 nMPI3Kα2.6-21 nMPI3Kβ2.6-21 nMPI3Kδ2.6-21 nMC128050CZC24832≥98%1159824-67-510mg,50mgPI3Kγ27 nMQ111274槲皮素95%117-39-510g,50g,250g PI3K2.4-5.4 μMD1673182-D0898% (HPLC)144707-18-65mg,25mgAxl0.49 nMIRAK43.9 nMROS15.3 nMMLK49.8 nMGSK3β11 nMRET11 nMKDR17 nMPI3Kα35 nMS174388SAR-40597%1523406-39-4100mgVps341.5 nMX127130Pilaralisib (XL147)≥98%934526-89-35mg,25mg,100mg無細胞PI3Kα39 nMPI3Kδ36 nMPI3Kγ23 nMD134674Deguelin≥95%522-17-85mg,25mgPI3K/AktA174656AZD-818697%1627494-13-65mg,25mg,50mg,100mgPI3Kβ4 nMPI3Kδ12 nM

*Akt

又稱PKB或Rac,是一種絲氨酸/蘇氨酸特異性蛋白激酶B,在細胞存活和凋亡中起重要作用,如葡萄糖代謝、凋亡、細胞增殖、轉錄和細胞遷移。Akt的Thr308可以被PDK1磷酸化,而被部分激活。或者473位點上的絲氨酸被mTORC2磷酸化,激發Akt的完全酶活性。

項目號產品名稱規格CAS包裝細胞靶點IC50KiED50
M129684MK-2206 2HCl≥98%1032350-13-210mg,50mg,100mg無細胞Akt18 nM
Akt212 nM
Akt365 nM
P124979Perifosine (KRX-0401)99%157716-52-45mg,10mg,50mg Akt4.7 μM
G127527GSK690693≥98%937174-76-0 10mg,50mg無細胞Akt12 nM
G127588GDC-0068≥98%1001264-89-65mg,10mg,50mg無細胞Akt15 nM
Akt218 nM
Akt38 nM
A128036AZD5363≥98%1143532-39-15mg,25mg,100mg無細胞Akt13 nM
Akt28 nM
Akt38 nM
P126369PF-04691502≥99%1013101-36-45mg,10mg,50mg無細胞PI3Kα1.8 nM
PI3Kβ2.1 nM
PI3Kδ1.6 nM
PI3Kγ1.9 nM
mTOR16 nM
A126209AT7867≥98%857531-00-15mg,10mg,50mg無細胞Akt132 nM
Akt217 nM
Akt347 nM
p70S6K85 nM
PKA20 nM
T126748Triciribine≥99%35943-35-25mg,10mg,50mgPC3細胞Akt130 nM
CEM-SS,H9,H9IIIB,U1細胞HIV-120 nM
C127073CCT128930≥99%885499-61-65mg,10mg,50mg無細胞Akt26 nM
A126845A-674563≥98%552325-73-25mg,25mg,100mg無細胞Akt11 nM
P127286PHT-427≥98%1191951-57-1 10mg,50mgAkt2.7 μM
PDPK15.2 μM
N130417米替福新>98%58066-85-6100mg,1g,5g,25g癌細胞系A431和HeLaPI3K17.2 μM
Akt8.1 μM
T129707TIC10 Analogue≥98%41276-02-25mg,25mg,100mg Akt、ERK
D134674Deguelin≥95%522-17-85mg,25mgPI3K/Akt

*mTOR

mTOR是細胞生長和增殖的重要調節因子。mTOR與其它蛋白質結合,形成兩種不同蛋白質復合物,mTORC1和mTORC2,參與調節不同的細胞過程。

項目號產品名稱規格CAS包裝細胞靶點IC50KiED50
B126286BEZ235≥99%915019-65-725mg,100mg無細胞PI3Kα4 nM
PI3Kβ5 nM
PI3Kδ7 nM
PI3Kγ75 nM
mTOR(p70S6K)6 nM
3T3TopBP1-ER 細胞ATR21 nM
S293790Rapamycin≥95%(HPLC)53123-88-950mg,250mg,1g HEK293細胞mTOR~0.1 nM
S115842Rapamycin≥98%(HPLC)53123-88-910mg,25mg,50mg,250mg,1g HEK293細胞mTOR~0.1 nM
E125341Everolimus≥98%159351-69-610mg,25mg,100mg無細胞mTOR1.6-2.4 nM
A126366AZD8055≥99%1009298-09-210mg,50mgMDA-MB-468 細胞mTOR0.8 nM
T126606Temsirolimus (CCI-779, NSC 683864)≥98%162635-04-35mg,25mg,100mg無細胞mTOR1.76 μM
P125961PI-103≥98%371935-74-910mg,50mg,100mg無細胞PI3Kα2 nM
PI3Kβ3 nM
PI3Kδ3 nM
PI3Kγ15 nM
mTOR30 nM
DNA-PK23 nM
K127530KU-0063794≥98%938440-64-35mg,25mg,100mg無細胞mTOR~10 nM
P129635PP242≥98%1092351-67-15mg,10mg,50mg無細胞mTOR8 nM
T101160他克莫司≥98%(HPLC)104987-11-350mg,1g
T101159他克莫司分析標準品,≥98%104987-11-310mg
D126066Ridaforolimus (Deforolimus, MK-8669)≥95%572924-54-05mg,10mg,50mgHT-1080細胞mTOR0.2 nM
I128086INK 128 (MLN0128)≥98%1224844-38-55mg,25mg,100mg無細胞mTOR1 nM
S129513SAR245409 (XL765)≥98%1349796-36-65mg,10mg,50mgp110γ9 nM
mTOR、PI3K、DNA-PK
T129642Torin 1≥97%1222998-36-810mg,25mg,50mg無細胞mTORC12 nM
mTORC210 nM
G127233GSK2126458 (GSK458)≥98%1086062-66-92mg,5mg,10mg,50mg無細胞PI3Kα0.019 nM
PI3Kβ0.13 nM
PI3Kδ0.024 nM
PI3Kγ0.06 nM
mTORC10.18 nM
mTORC20.3 nM
O127920OSI-027≥98%936890-98-15mg,10mg,50mg無細胞mTORC122 nM
mTORC265 nM
P126369PF-04691502≥99%1013101-36-45mg,10mg,50mg無細胞PI3Kα1.8 nM
PI3Kβ2.1 nM
PI3Kδ1.6 nM
PI3Kγ1.9 nM
mTOR16 nM
G126387GDC-0980 (RG7422)≥98%1032754-93-05mg,25mg,100mg無細胞PI3Kα5 nM
PI3Kβ27 nM
PI3Kδ7 nM
PI3Kγ14 nM
mTOR17 nM
G127955GSK1059615≥98%958852-01-25mg,25mg,100mgPI3Kα0.4 nM
PI3Kβ0.6 nM
PI3Kδ2 nM
PI3Kγ5 nM
mTOR12 nM
P129530Gedatolisib (PF-05212384, PKI-587)≥98%1197160-78-35mg,10mg,50mg無細胞PI3Kα0.4 nM
PI3Kγ5.4 nM
mTOR1.6 nM
W128007WYE-354≥98%1062169-56-55mg,25mg,100mg mTOR5 nM
A127600AZD2014≥98%1009298-59-25mg,25mg,100mg無細胞mTOR2.8 nM
T129646Torin 2≥98%1223001-51-15mg,10mg,50mgp53−/− MEFs細胞系mTOR0.25 nM
PC3細胞系ATM28 nM
ATR35 nM
DNA-PK118 nM
W128041WYE-125132 (WYE-132)≥98%1144068-46-15mg,25mg,100mgmTORmTOR0.19 nM
N125612BGT226 (NVP-BGT226)≥98%1245537-68-15mg,25mg,100mgPI3Kα4 nM
PI3Kβ63 nM
PI3K, γ38 nM
P126419PP121≥98%1092788-83-410mg,50mgPDGFR2 nM
Hck8 nM
mTOR10 nM
VEGFR212 nM
Src14 nM
Abl18 nM
DNA-PK60 nM
W126399WYE-687≥98%1062161-90-35mg,25mg,50mg mTOR7 nM
W129657WAY-600≥98%1062159-35-65mg,25mg,50mg mTOR9 nM
E125288ETP-46464≥99%1345675-02-610mg,50mgATR25 nM
G128080GDC-0349≥99%1207360-89-15mg,25mgmTOR3.8 nM
X124864XL388≥99%1251156-08-710mg,25mgmTOR9.9 nM

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阿拉丁小分子抑制劑、激動劑、拮抗劑--PI3K/Akt/mTOR信號通路(一)

PI3K/AKT/mTOR

PI3K/AKT/mTOR是調節細胞周期的重要細胞內信號通路。PI3K/AKT/mTOR信號通路與細胞的生長、存活、增殖、凋亡、血管生成、自吞噬過程中發揮著重要的生物學功能。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)和哺乳動物雷帕霉素靶蛋白(mTOR)組成。

PI3K/Akt/mTOR通路過程

PI3K激活后產生PIP3, PIP3促使PDK1(phosphoinositide dependent kinase-1)磷酸化含有PH結構域的信號AKT蛋白(Ser308),從而活化AKT。AKT有很多下游效應,可通過磷酸化多種酶、激酶和轉錄因子等下游因子,進而調節細胞的功能。mTOR,是PI3K/Akt 下游的一種重要的絲氨酸-蘇氨酸蛋白激酶,調節腫瘤細胞的自噬的經典通路。

PI3K/Akt/mTOR信號通路圖

產品列表

按靶點分類:

*PI3K

PI3K,是一種胞內磷脂酰肌醇激酶,也具有絲氨酸/蘇氨酸(Ser/Thr)激酶的活性。能夠通過PI3K誘發PIP3生成的激活因子,則能夠激活 Akt 信號途徑,包括受體酪氨酸激酶、整合素、B 細胞和 T 細胞受體、細胞因子受體、G 蛋白偶聯受體等等。

項目號產品名稱規格CAS包裝細胞靶點IC50KiKd
B126286BEZ235≥99%915019-65-725mg,100mg無細胞p110α4 nM
p110γ5 nM
p110δ7 nM
p110β75 nM
mTOR(p70S6K)6 nM
3T3TopBP1-ER 細胞ATR21 nM
G126357GDC-0941≥98%957054-30-710mg,50mg,250mg無細胞PI3Kα3 nM
PI3Kδ3 nM
L124970LY294002≥98%154447-36-610mg,25mg,50mg無細胞PI3Kα0.5 μM
PI3Kδ0.57 μM
PI3Kβ0.97 μM
C127044CAL-101≥99%870281-82-610mg,50mg,100mg,250mg,500mg無細胞p110δ2.5 nM
N127553BKM120≥99%944396-07-05mg,10mg,50mg無細胞p110α52 nM
p110β166 nM
p110δ116 nM
p110γ262 nM
P125961PI-103≥98%371935-74-910mg,50mg,100mg無細胞p110α2 nM
p110β3 nM
p110δ3 nM
p110γ15 nM
K126842NU7441 (KU-57788)≥98%503468-95-95mg,25mg,100mg無細胞DNA-PK14 nM
PI3K5 μM
T127773TGX-221≥99%663619-89-45mg,25mg,100mg無細胞p110β5 nM
I126757IC-87114≥98%371242-69-2 5mg,25mg,100mg無細胞PI3Kδ0.5 μM
W100984Wortmannin98%19545-26-75mg,10mg,25mg無細胞PI3K3 nM
DNA-PK16 nM
ATM150 nM
X129499XL147≥98%956958-53-510mg,50mg無細胞PI3Kα39 nM
PI3Kδ36 nM
PI3Kγ23 nM
Z126804ZSTK474≥98%475110-96-410mg,25mg,50mg,100mg無細胞PI3K37 nM
B127311BYL719≥99%1217486-61-75mg,10mg,20mg,50mg無細胞PI3Kα5 nM
A127765AS-605240≥98%648450-29-75mg,25mg,100mg PI3Kγ8 nM
P125966PIK-75≥98%372196-77-510mg,50mg,100mg無細胞p110α5.8 nM
DNA-PK2 nM
M1294963-甲基腺嘌呤0.985142-23-450mg,250mg,1g,5g,25g HeLa細胞Vps3425 μM
PI3Kγ60 μM
A128051A66≥99%1166227-08-25mg,10mg,50mg無細胞p110α32 nM
S129513SAR245409 (XL765)≥98%1349796-36-65mg,10mg,50mg p110γ9 nM
G127233GSK2126458 (GSK458)≥98%1086062-66-92mg,5mg,10mg,50mg無細胞p110α0.019 nM
p110β0.13 nM
p110γ0.024 nM
p110δ0.06 nM
mTORC10.18 nM
mTORC20.3 nM
P126920PIK-90≥99%677338-12-45mg,10mg,50mgPI3Kα11 nM
PI3Kγ18 nM
PI3Kδ58 nM
A129523AZD6482≥98%1173900-33-85mg,10mg,50mg無細胞PI3Kβ10 nM
P126369PF-04691502≥99%1013101-36-45mg,10mg,50mg無細胞PI3Kα1.8 nM
PI3Kβ2.1 nM
PI3Kδ1.6 nM
PI3Kγ1.9 nM
G126387GDC-0980 (RG7422)≥98%1032754-93-05mg,25mg,100mg無細胞PI3Kα5 nM
PI3Kβ27 nM
PI3Kδ7 nM
PI3Kγ14 nM
mTOR17 nM
G127955GSK1059615≥98%958852-01-25mg,25mg,100mgPI3Kα0.4 nM
PI3Kβ0.6 nM
PI3Kδ2 nM
PI3Kγ5 nM
mTOR12 nM
I126464Duvelisib (IPI-145, INK1197)≥98%1201438-56-35mg,10mg,25mg,50mg,100mg無細胞PI3Kδ1 nM
PI3Kγ50 nM
P129530Gedatolisib (PF-05212384, PKI-587)≥98%1197160-78-35mg,10mg,50mg無細胞PI3Kα0.4 nM
PI3Kγ5.4 nM
mTOR1.6 nM
T127783TG100-115≥98%677297-51-75mg,25mg,100mg 上海阿拉丁生化科技股份有限公司   商家主頁

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