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首页 >  新闻动态 >  阿拉丁小分子抑制剂、激动剂、拮抗剂--PI3K/Akt/mTOR信号通路(一)

阿拉丁小分子抑制剂、激动剂、拮抗剂--PI3K/Akt/mTOR信号通路(一)

发布时间:2019-12-09

阿拉丁小分子抑制剂、激动剂、拮抗剂--PI3K/Akt/mTOR信号通路(一)

PI3K/AKT/mTOR

PI3K/AKT/mTOR是调节细胞周期的重要细胞内信号通路。PI3K/AKT/mTOR信号通路与细胞的生长、存活、增殖、凋亡、血管生成、自吞噬过程中发挥着重要的生物学功能。该通路是由磷脂酰肌醇3- 激酶(PI3Ks)、丝氨酸/苏氨酸蛋白激酶(Akt)和哺乳动物雷帕霉素靶蛋白(mTOR)组成。

PI3K/Akt/mTOR通路过程

PI3K激活后产生PIP3, PIP3促使PDK1(phosphoinositide dependent kinase-1)磷酸化含有PH结构域的信号AKT蛋白(Ser308),从而活化AKT。AKT有很多下游效应,可通过磷酸化多种酶、激酶和转录因子等下游因子,进而调节细胞的功能。mTOR,是PI3K/Akt 下游的一种重要的丝氨酸-苏氨酸蛋白激酶,调节肿瘤细胞的自噬的经典通路。

PI3K/Akt/mTOR信号通路图

产品列表

按靶点分类:     

*PI3K

PI3K,是一种胞内磷脂酰肌醇激酶,也具有丝氨酸/苏氨酸(Ser/Thr)激酶的活性。能够通过PI3K诱发PIP3生成的激活因子,则能够激活 Akt 信号途径,包括受体酪氨酸激酶、整合素、B 细胞和 T 细胞受体、细胞因子受体、G 蛋白偶联受体等等。     

项目号产品名称规格CAS包装细胞靶点IC50KiKd
B126286BEZ235≥99%915019-65-725mg,100mg无细胞p110α4 nM

p110γ5 nM 

p110δ7 nM

p110β75 nM

mTOR(p70S6K)6 nM

3T3TopBP1-ER 细胞ATR21 nM

G126357GDC-0941≥98%957054-30-710mg,50mg,250mg无细胞PI3Kα3 nM

PI3Kδ3 nM

L124970LY294002≥98%154447-36-610mg,25mg,50mg无细胞PI3Kα0.5 μM

PI3Kδ0.57 μM

PI3Kβ0.97 μM

C127044CAL-101≥99%870281-82-610mg,50mg,100mg,250mg,500mg无细胞p110δ2.5 nM

N127553BKM120≥99%944396-07-05mg,10mg,50mg无细胞p110α52 nM

p110β166 nM

p110δ116 nM

p110γ262 nM

P125961PI-103≥98%371935-74-910mg,50mg,100mg无细胞p110α2 nM

p110β3 nM

p110δ3 nM

p110γ15 nM

K126842NU7441 (KU-57788)≥98%503468-95-95mg,25mg,100mg无细胞DNA-PK14 nM

PI3K5 μM

T127773TGX-221≥99%663619-89-45mg,25mg,100mg无细胞p110β5 nM

I126757IC-87114≥98%371242-69-2 5mg,25mg,100mg无细胞PI3Kδ0.5 μM

W100984Wortmannin98%19545-26-75mg,10mg,25mg无细胞PI3K3 nM

DNA-PK16 nM

ATM150 nM

X129499XL147≥98%956958-53-510mg,50mg无细胞PI3Kα39 nM

PI3Kδ36 nM

PI3Kγ23 nM

Z126804ZSTK474≥98%475110-96-410mg,25mg,50mg,100mg无细胞PI3K37 nM

B127311BYL719≥99%1217486-61-75mg,10mg,20mg,50mg无细胞PI3Kα5 nM

A127765AS-605240≥98%648450-29-75mg,25mg,100mg
PI3Kγ8 nM

P125966PIK-75≥98%372196-77-510mg,50mg,100mg无细胞p110α5.8 nM

DNA-PK2 nM

M1294963-甲基腺嘌呤0.985142-23-450mg,250mg,1g,5g,25g HeLa细胞Vps3425 μM

PI3Kγ60 μM

A128051A66≥99%1166227-08-25mg,10mg,50mg无细胞p110α32 nM

S129513SAR245409 (XL765)≥98%1349796-36-65mg,10mg,50mg
p110γ9 nM

G127233GSK2126458 (GSK458)≥98%1086062-66-92mg,5mg,10mg,50mg无细胞p110α
0.019 nM
p110β
0.13 nM
p110γ
0.024 nM
p110δ
0.06 nM
mTORC1
0.18 nM
mTORC2
0.3 nM
P126920PIK-90≥99%677338-12-45mg,10mg,50mg
PI3Kα11 nM

PI3Kγ18 nM

PI3Kδ58 nM

A129523AZD6482≥98%1173900-33-85mg,10mg,50mg无细胞PI3Kβ10 nM

P126369PF-04691502≥99%1013101-36-45mg,10mg,50mg无细胞PI3Kα1.8 nM

PI3Kβ2.1 nM

PI3Kδ1.6 nM

PI3Kγ1.9 nM

G126387GDC-0980 (RG7422)≥98%1032754-93-05mg,25mg,100mg无细胞PI3Kα5 nM

PI3Kβ27 nM

PI3Kδ7 nM

PI3Kγ14 nM

mTOR17 nM

G127955GSK1059615≥98%958852-01-25mg,25mg,100mg
PI3Kα0.4 nM

PI3Kβ0.6 nM

PI3Kδ2 nM

PI3Kγ5 nM

mTOR12 nM

I126464Duvelisib (IPI-145, INK1197)≥98%1201438-56-35mg,10mg,25mg,50mg,100mg无细胞PI3Kδ1 nM

PI3Kγ50 nM

P129530Gedatolisib (PF-05212384, PKI-587)≥98%1197160-78-35mg,10mg,50mg无细胞PI3Kα0.4 nM

PI3Kγ5.4 nM

mTOR1.6 nM

T127783TG100-115≥98%677297-51-75mg,25mg,100mg
PI3Kγ83 nM

PI3Kδ235 nM

A129503AS-252424≥98%900515-16-42mg,5mg,25mg,100mg无细胞PI3Kγ30 nM

N125612BGT226 (NVP-BGT226)≥98%1245537-68-15mg,25mg,100mg
PI3Kα4 nM

PI3Kβ63 nM

PI3Kγ38 nM

C126527CUDC-907≥99%1339928-25-45mg,10mg,50mg
PI3Kα19 nM

HDAC11.7 nM

HDAC25 nM

HDAC31.8 nM

HDAC102.8 nM

P129553PIK-294≥98%900185-02-65mg,10mg,50mg
p110δ10 nM

A129517AS-604850≥98%648449-76-75mg,25mg,100mg
PI3Kγ250 nM

G125299GSK2636771≥98%1372540-25-45mg,10mg,50mg
PI3Kβ5.2 nM

B129540BAY 80-6946 (Copanlisib)≥99%1032568-63-05mg,10mg,50mg,250mg
PI3Kα0.5 nM

PI3Kβ3.7 nM

PI3Kγ6.4 nM

PI3Kδ0.7 nM

C127596CH5132799≥97%1007207-67-15mg,25mg,100mg
PI3Kα14 nM

C129600CAY10505≥99%1218777-13-910mg,25mg,50mg,250mg
PI3Kγ30 nM

P129615PIK-293≥97%900185-01-55mg,25mg,50mg
PI3Kδ0.24 μM

P127674PKI-402≥98%1173204-81-3 5mg,10mg,50mg
PI3Kα2 nM

PI3Kβ7 nM

PI3Kγ16 nM

PI3Kδ14 nM

mTOR3 nM

T129620TG100713≥97%925705-73-310mg,50mg
PI3Kγ50 nM


PI3Kδ24 nM


PI3Kα165 nM


PI3Kβ215 nM

V125616VS-5584 (SB2343)≥98%1246560-33-710mg,50mg
mTOR3.4 nM

PI3Kα2.6-21 nM

PI3Kβ2.6-21 nM

PI3Kδ2.6-21 nM

C128050CZC24832≥98%1159824-67-510mg,50mg
PI3Kγ27 nM

Q111274槲皮素95%117-39-510g,50g,250g
PI3K2.4-5.4 μM

D1673182-D0898% (HPLC)144707-18-65mg,25mg
Axl0.49 nM


IRAK43.9 nM


ROS15.3 nM


MLK49.8 nM


GSK3β11 nM


RET11 nM


KDR17 nM


PI3Kα35 nM

S174388SAR-40597%1523406-39-4100mg
Vps34

1.5 nM
X127130Pilaralisib (XL147)≥98%934526-89-35mg,25mg,100mg无细胞PI3Kα39 nM

PI3Kδ36 nM

PI3Kγ23 nM

D134674Deguelin≥95%522-17-85mg,25mg
PI3K/Akt


A174656AZD-818697%1627494-13-65mg,25mg,50mg,100mg
PI3Kβ4 nM


PI3Kδ12 nM

 *Akt

又称PKB或Rac,是一种丝氨酸/苏氨酸特异性蛋白激酶B,在细胞存活和凋亡中起重要作用,如葡萄糖代谢、凋亡、细胞增殖、转录和细胞迁移。Akt的Thr308可以被PDK1磷酸化,而被部分激活。或者473位点上的丝氨酸被mTORC2磷酸化,激发Akt的完全酶活性。

项目号产品名称规格CAS包装细胞靶点IC50KiED50
M129684MK-2206 2HCl≥98%1032350-13-210mg,50mg,100mg无细胞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无细胞Akt12 nM

G127588GDC-0068≥98%1001264-89-65mg,10mg,50mg无细胞Akt15 nM

Akt218 nM

Akt38 nM

A128036AZD5363≥98%1143532-39-15mg,25mg,100mg无细胞Akt13 nM

Akt28 nM

Akt38 nM

P126369PF-04691502≥99%1013101-36-45mg,10mg,50mg无细胞PI3Kα1.8 nM

PI3Kβ2.1 nM

PI3Kδ1.6 nM

PI3Kγ1.9 nM

mTOR16 nM

A126209AT7867≥98%857531-00-15mg,10mg,50mg无细胞Akt132 nM

Akt217 nM

Akt347 nM

p70S6K85 nM

PKA20 nM

T126748Triciribine≥99%35943-35-25mg,10mg,50mgPC3细胞Akt130 nM

CEM-SS,H9,H9IIIB,U1细胞HIV-120 nM

C127073CCT128930≥99%885499-61-65mg,10mg,50mg无细胞Akt26 nM

A126845A-674563≥98%552325-73-25mg,25mg,100mg无细胞Akt
11 nM
P127286PHT-427≥98%1191951-57-1 10mg,50mg
Akt
2.7 μM
PDPK1
5.2 μM
N130417米替福新>98%58066-85-6100mg,1g,5g,25g癌细胞系A431和HeLaPI3K

17.2 μM
Akt

8.1 μM
T129707TIC10 Analogue≥98%41276-02-25mg,25mg,100mg
Akt、ERK


D134674Deguelin≥95%522-17-85mg,25mg
PI3K/Akt


*mTOR

mTOR是细胞生长和增殖的重要调节因子。mTOR与其它蛋白质结合,形成两种不同蛋白质复合物,mTORC1和mTORC2,参与调节不同的细胞过程。

项目号产品名称规格CAS包装细胞靶点IC50KiED50
B126286BEZ235≥99%915019-65-725mg,100mg无细胞PI3Kα4 nM

PI3Kβ5 nM

PI3Kδ7 nM

PI3Kγ75 nM

mTOR(p70S6K)6 nM

3T3TopBP1-ER 细胞ATR21 nM

S293790Rapamycin≥95%(HPLC)53123-88-950mg,250mg,1g HEK293细胞mTOR~0.1 nM

S115842Rapamycin≥98%(HPLC)53123-88-910mg,25mg,50mg,250mg,1g HEK293细胞mTOR~0.1 nM

E125341Everolimus≥98%159351-69-610mg,25mg,100mg无细胞mTOR1.6-2.4 nM

A126366AZD8055≥99%1009298-09-210mg,50mgMDA-MB-468 细胞mTOR0.8 nM

T126606Temsirolimus (CCI-779, NSC 683864)≥98%162635-04-35mg,25mg,100mg无细胞mTOR1.76 μM

P125961PI-103≥98%371935-74-910mg,50mg,100mg无细胞PI3Kα2 nM

PI3Kβ3 nM

PI3Kδ3 nM

PI3Kγ15 nM

mTOR30 nM

DNA-PK23 nM

K127530KU-0063794≥98%938440-64-35mg,25mg,100mg无细胞mTOR~10 nM

P129635PP242≥98%1092351-67-15mg,10mg,50mg无细胞mTOR8 nM

T101160他克莫司≥98%(HPLC)104987-11-350mg,1g




T101159他克莫司分析标准品,≥98%104987-11-310mg




D126066Ridaforolimus (Deforolimus, MK-8669)≥95%572924-54-05mg,10mg,50mgHT-1080细胞mTOR0.2 nM

I128086INK 128 (MLN0128)≥98%1224844-38-55mg,25mg,100mg无细胞mTOR1 nM

S129513SAR245409 (XL765)≥98%1349796-36-65mg,10mg,50mg
p110γ9 nM


mTOR、PI3K、DNA-PK


T129642Torin 1≥97%1222998-36-810mg,25mg,50mg无细胞mTORC12 nM

mTORC210 nM

G127233GSK2126458 (GSK458)≥98%1086062-66-92mg,5mg,10mg,50mg无细胞PI3Kα
0.019 nM
PI3Kβ
0.13 nM
PI3Kδ
0.024 nM
PI3Kγ
0.06 nM
mTORC1
0.18 nM
mTORC2
0.3 nM
O127920OSI-027≥98%936890-98-15mg,10mg,50mg无细胞mTORC122 nM

mTORC265 nM

P126369PF-04691502≥99%1013101-36-45mg,10mg,50mg无细胞PI3Kα
1.8 nM
PI3Kβ
2.1 nM
PI3Kδ
1.6 nM
PI3Kγ
1.9 nM
mTOR
16 nM
G126387GDC-0980 (RG7422)≥98%1032754-93-05mg,25mg,100mg无细胞PI3Kα5 nM

PI3Kβ27 nM

PI3Kδ7 nM

PI3Kγ14 nM

mTOR
17 nM
G127955GSK1059615≥98%958852-01-25mg,25mg,100mg
PI3Kα0.4 nM

PI3Kβ0.6 nM

PI3Kδ2 nM

PI3Kγ5 nM

mTOR12 nM

P129530Gedatolisib (PF-05212384, PKI-587)≥98%1197160-78-35mg,10mg,50mg无细胞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无细胞mTOR2.8 nM

T129646Torin 2≥98%1223001-51-15mg,10mg,50mgp53?/? MEFs细胞系mTOR0.25 nM

PC3细胞系ATM

28 nM
ATR

35 nM
DNA-PK

118 nM
W128041WYE-125132 (WYE-132)≥98%1144068-46-15mg,25mg,100mgmTORmTOR0.19 nM

N125612BGT226 (NVP-BGT226)≥98%1245537-68-15mg,25mg,100mg
PI3Kα4 nM

PI3Kβ63 nM

PI3Kγ38 nM

P126419PP121≥98%1092788-83-410mg,50mg
PDGFR2 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,50mg
ATR25 nM

G128080GDC-0349≥99%1207360-89-15mg,25mg
mTOR
3.8 nM
X124864XL388≥99%1251156-08-710mg,25mg
mTOR9.9 nM


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