PI3K/Akt/mTOR信号通路相关高活性小分子抑制剂
时间: 2020-04-23
作者: 百灵威
分享:
PI3K/Akt/mTOR是哺乳动物细胞内非常重要的信号通路之一，它通过影响下游多种效应分子的活化状态，在细胞内抑制凋亡、促进增殖。研究表明：PI3K/Akt/mTOR信号通路与肝癌、结肠癌、肺癌、乳腺癌等多种肿瘤的发生、发展密切相关[1-2]。
其中AMG319是一种有效的选择性 PI3Kδ抑制剂，用于治疗头颈癌[3]；AZD8186是一种有效的选择性PI3Kβ和PI3Kδ抑制剂，用于治疗晚期去势抵抗前列腺癌(CRPC)、鳞状非小细胞肺癌(sqNSCLC)、三阴性乳腺癌与PTEN基因缺失患者的晚期实体瘤[4]。
百灵威提供PI3K/Akt/mTOR信号通路中的小分子抑制剂，可作用于PI3K、mTOR、PDK-1、Akt等多个靶点，助力信号通路研究及新药筛选。
- 靶点信息清晰明确，便于选择；
- 严格的质检，确保产品高纯度、高品质；
- 生物活性经多客户验证；
- 性价比高：每个产品可节约5%-20%成本。
![图1 The PI3K/AKT/mTOR pathway, molecular targets for anticancer therapy and most common locations for gain-of-function aberrations (green) or loss-of function aberrations (red). <sup>[2]</sup>](https://shop.jkchemical.com/res/0-2237.png)
图1 The PI3K/AKT/mTOR pathway, molecular targets for anticancer therapy and most common locations for gain-of-function aberrations (green) or loss-of function aberrations (red). [2]
产品列表（按靶点分类）
911191
371935-74-9
PI-103, 99%
Description:
a potent PI3K and mTOR inhibitor
a potent PI3K and mTOR inhibitor
1004472
1217486-61-7
Alpelisib, 98%
Description:
a potent and selective PI3Kα inhibitor
a potent and selective PI3Kα inhibitor
1024276
1086062-66-9
Omipalisib, 98%
Description:
a highly selective and potent inhibitor of PI3K
a highly selective and potent inhibitor of PI3K
1232641
957054-30-7
Pictilisib, 98%
Description:
a potent inhibitor of PI3Kα/δ
a potent inhibitor of PI3Kα/δ
1232676
663619-89-4
TGX-221, 98%
Description:
a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit
a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit
1239104
870281-82-6
CAL-101, 99%
Description:
a selective p110δ inhibitor
a selective p110δ inhibitor
1239139
944396-07-0
Buparlisib, 98%
Description:
a selective PI3K inhibitor
a selective PI3K inhibitor
1562554
1197160-78-3
Gedatolisib, 98%
Description:
a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, mTORC1 and mTORC2
a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, mTORC1 and mTORC2
1578548
1282512-48-4
GDC-0032, 98%
Description:
a potent β-sparing small molecule inhibitor of PI3K
a potent β-sparing small molecule inhibitor of PI3K
1759176
1166227-08-2
A66, 98%
Description:
a potent and specific p110α inhibitor
a potent and specific p110α inhibitor
1835029
1349796-36-6
Voxtalisib analogue, 98%
Description:
a potent inhibitor of PI3K
a potent inhibitor of PI3K
1952693
1627494-13-6
AZD8186, 98%
Description:
a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC50=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM)
a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC50=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM)
2465312
1693758-51-8
IPI-549, 98%
Description:
a potent and selective PI3Kγ Inhibitor
a potent and selective PI3Kγ Inhibitor
282611
19545-26-7
Wortmannin, 98%
Description:
a multi-target inhibitor of PI3K and MLCK
a multi-target inhibitor of PI3K and MLCK
284107
154447-36-6
2-Morpholino-8-phenylchromone, 98%
Description:
a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively
a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively
369172
5142-23-4
3-Methyladenine, 90%
Description:
a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K
a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K
626764
475110-96-4
ZSTK474, 98%
Description:
an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively
an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively
916582
371935-74-9
PI-103, 98%
Description:
a potent PI3K/Akt and mTOR inhibitor
a potent PI3K/Akt and mTOR inhibitor
985598
1222998-36-8
Torin 1, 99%
Description:
a potent inhibitor of mTOR with an IC50 of 3 nM
a potent inhibitor of mTOR with an IC50 of 3 nM
9000070
1092788-83-4
PP121, 98%
Description:
a multi-targeted kinase inhibitor
a multi-targeted kinase inhibitor
901580
1223001-51-1
Torin 2, 98%
Description:
an mTOR inhibitor
an mTOR inhibitor
914307
326914-06-1
MHY1485, 99%
Description:
a cell-permeable mTOR activator
a cell-permeable mTOR activator
1126271
1009298-09-2
AZD-8055, 98%
Description:
a novel ATP-competitive inhibitor of mTOR kinase with an IC50 of 0.8 nM
a novel ATP-competitive inhibitor of mTOR kinase with an IC50 of 0.8 nM
1239103
1092351-67-1
Torkinib, 98%
Description:
a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM,PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM
a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM,PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM
1239137
1222998-36-8
Torin 1, 98%
Description:
a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM
a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM
1497296
1009298-59-2
Vistusertib, 98%
Description:
a novel mTOR inhibitor
a novel mTOR inhibitor
1561319
1224844-38-5
Sapanisertib, 98%
Description:
a potent and selective mTOR inhibitor
a potent and selective mTOR inhibitor
1761872
914913-88-5
Palomid 529, 98%
Description:
a novel potent inhibitor of both the mTORC1 and mTORC2
a novel potent inhibitor of both the mTORC1 and mTORC2
623756
159351-69-6
Everolimus, 95%
Description:
a potent mTOR inhibitor that binds to FKBP-12 to generate an immunosuppressive complex
a potent mTOR inhibitor that binds to FKBP-12 to generate an immunosuppressive complex
628156
162635-04-3
Temsirolimus, 99%
Description:
an inhibitor of mTOR with an IC50 of 1.76 μM
an inhibitor of mTOR with an IC50 of 1.76 μM
814294
221877-54-9
Zotarolimus, 98%
Description:
a tetrazole-containing Rapamycin analog
a tetrazole-containing Rapamycin analog
2276028
871361-88-5
SC66, 98%
Description:
a novel Akt inhibitor
a novel Akt inhibitor
1587022
1191951-57-1
PHT-427, 98%
Description:
an inhibitor of the pleckstrin homology (PH) domain of Akt
an inhibitor of the pleckstrin homology (PH) domain of Akt
621993
612847-09-3
AKT inhibitor VIII, 98%
Description:
a cell-permeable quinoxaline compound that has been shown to potently
a cell-permeable quinoxaline compound that has been shown to potently
532437
522-17-8
Deguelin, 98%
Description:
a naturally occurring rotenoid, is a potent PI3K/AKT inhibitor
a naturally occurring rotenoid, is a potent PI3K/AKT inhibitor
1747973
305834-79-1
SC79, 98%
Description:
a selective and cell-permeable Akt activator
a selective and cell-permeable Akt activator
1109328
157716-52-4
Perifosine, 98%
Description:
an oral Akt inhibitor
an oral Akt inhibitor
114705
35354-74-6
Honokiol, 98%
Description:
inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2
inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2
1189640
1032350-13-2
MK 2206 dihydrochloride, 98%
Description:
an allosteric Akt inhibitor
an allosteric Akt inhibitor
1561522
1143532-39-1
AZD5363, 99%
Description:
a potent pan-AKT kinase inhibitor
a potent pan-AKT kinase inhibitor
320518
35943-35-2
Triciribine, 98%
Description:
a DNA synthesis inhibitor
a DNA synthesis inhibitor
618339
667463-62-9
GSK 3 Inhibitor IX, 99%
Description:
a potent, selective, reversible and ATP-competitive inhibitor
a potent, selective, reversible and ATP-competitive inhibitor
1018987
252917-06-9
CHIR-99021, 98%
Description:
a GSK-3α/β inhibitor with an IC50 of 10 and 6.7 nM, showing 500-fold selectivity over its closest homologs CDC2 and ERK2, as well as other protein kinases
a GSK-3α/β inhibitor with an IC50 of 10 and 6.7 nM, showing 500-fold selectivity over its closest homologs CDC2 and ERK2, as well as other protein kinases
613609
280744-09-4
SB 216763, 98%
Description:
is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β
is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β
1232532
702675-74-9
BX795, 98%
Description:
a potent and selective dual inhibitor of TBK1/PDK1
a potent and selective dual inhibitor of TBK1/PDK1
1232463
501437-28-1
BI-D1870, 98%
Description:
ATP-competitive inhibitor of RSK isoforms
ATP-competitive inhibitor of RSK isoforms
2286643
1627709-94-7
LJI308, 98%
Description:
a new and potent pan-RSK inhibitor
a new and potent pan-RSK inhibitor
1433446
1255517-76-0
PF-4708671, 99%
Description:
a potent cell-permeable S6K1 inhibitor
a potent cell-permeable S6K1 inhibitor
460618
127243-85-0
H-89 dihydrochloride, 98%
Description:
a potent and selective inhibitor of PKA
a potent and selective inhibitor of PKA
786108
866405-64-3
Dorsomorphin, 98%
Description:
a potent and selective AMPK inhibitor
a potent and selective AMPK inhibitor
2286494
1613724-42-7
HTH-01-015, 98%
Description:
a selective NUAK1/ARK5 inhibitor (IC50 is 100 nM)
a selective NUAK1/ARK5 inhibitor (IC50 is 100 nM)
1835021
1214265-58-3
WZ4003, 97%
Description:
the first potent and highly specific NUAK kinase inhibitor
the first potent and highly specific NUAK kinase inhibitor
1386067
844499-71-4
A 769662, 98%
Description:
a potent, reversible AMPK activator with EC50 of 0.8 μM
a potent, reversible AMPK activator with EC50 of 0.8 μM
155684
2627-69-2
5-Aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, 98%
Description:
a cell-permeable AMP-activated protein kinase (AMPK) activator
a cell-permeable AMP-activated protein kinase (AMPK) activator
334798
834-28-6
Phenformin hydrochloride, 98%
Description:
an anti-diabetic drug from the biguanide class, can activate AMPK activity
an anti-diabetic drug from the biguanide class, can activate AMPK activity
相关文章
- Porta C, Paglino C, Mosca A. Targeting PI3K/Akt/mTOR signaling in cancer. Frontiers in oncology, 2014, 4: 64.
- Jiri Polivka Jr. , Filip Janku . Molecular targets for cancer therapy in the PI3K/AKT/mTOR pathway. Pharmacology & Therapeutics, 2014, 142: 164–175.
- Cushing TD, et al. Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. J Med Chem. 2015 Jan 8;58(1):480-511.
- Hancox U, et al. Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with RP-56976. Mol Cancer Ther. 2015 Jan;14(1):48-58.
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