WYE-132是一种高效的、ATP 竞争性特异性 mTOR 激酶抑制剂,IC50 为 0.19 nM,对 mTOR 比对 PI3K 或 PI3K 相关激酶 hSMG1 和 ATR 更具选择性。


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| 产品名称 | mTOR ↓ ↑ | mTORC1 ↓ ↑ | mTORC2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| AZD-8055 |
++++
mTOR (truncated), IC50: 0.13 nM mTOR (full length), IC50: 0.8 nM |
99%+ | |||||||||||||||||
| Gedatolisib |
++++
mTOR, IC50: 1.6 nM |
99% | |||||||||||||||||
| GSK1059615 |
++
mTOR, IC50: 12 nM |
98% | |||||||||||||||||
| Vistusertib |
+++
mTOR, IC50: 2.8 nM |
99%+ | |||||||||||||||||
| Torin 1 |
+++
mTOR, IC50: 4.32 nM |
+++
mTORC1, IC50: 2 nM |
++
mTORC2, IC50: 10 nM |
DNA-PK | 99%+ | ||||||||||||||
| Dactolisib |
+++
mTOR (p70S6K), IC50: 6 nM |
98+% | |||||||||||||||||
| PI-103 |
+
mTOR, IC50: 30 nM |
99%+ | |||||||||||||||||
| WAY-600 |
++
mTOR, IC50: 9 nM |
99% | |||||||||||||||||
| Voxtalisib |
+
mTOR, IC50: 157 nM |
99%+ | |||||||||||||||||
| PF-04691502 |
++
mTOR, Ki: 16 nM |
98+% | |||||||||||||||||
| Onatasertib |
++
mTOR, IC50: 16 nM |
DNA-PK | 99%+ | ||||||||||||||||
| Chrysophanol | ✔ | EGFR | 98% | ||||||||||||||||
| Samotolisib | ✔ | DNA-PK | 99%+ | ||||||||||||||||
| Torkinib |
+++
mTOR, IC50: 8 nM |
PDGFR,DNA-PK | 99%+ | ||||||||||||||||
| Everolimus | 99%+ | ||||||||||||||||||
| WYE-354 |
+++
mTOR, IC50: 5 nM |
98% | |||||||||||||||||
| Tacrolimus | ✔ | 98% | |||||||||||||||||
| PP121 |
++
mTOR, IC50: 13 nM |
VEGFR,PDGFR | 99%+ | ||||||||||||||||
| Torin 2 |
++++
mTOR, IC50: 0.25 nM |
DNA-PK | 99%+ | ||||||||||||||||
| Rapamycin |
++++
mTOR, IC50: ~0.1 nM |
98% | |||||||||||||||||
| GDC-0349 |
+++
mTOR, Ki: 3.8 nM |
98% | |||||||||||||||||
| XL388 |
++
mTOR, IC50: 9.9 nM |
+++
mTORC1, IC50: 8 nM |
+
mTORC2, IC50: 166 nM |
99%+ | |||||||||||||||
| WYE-687 |
+++
mTOR, IC50: 7 nM |
98% | |||||||||||||||||
| Apitolisib |
+
mTOR, Ki app: 17 nM |
98%+ | |||||||||||||||||
| WYE-132 |
++++
mTOR, IC50: 0.19 nM |
99%+ | |||||||||||||||||
| Sapanisertib |
++++
mTOR, Ki: 1.4 nM |
99%+ | |||||||||||||||||
| BGT226 maleate | ✔ | 99%+ | |||||||||||||||||
| ETP-46464 |
++++
mTOR, IC50: 0.6 nM |
DNA-PK | 98% | ||||||||||||||||
| PI3K-IN-1 |
+
mTOR, IC50: 157 nM |
98+% | |||||||||||||||||
| Zotarolimus |
+++
FKBP-12, IC50: 2.8 nM |
98% | |||||||||||||||||
| OSI-027 |
+++
mTOR, IC50: 4 nM |
+
mTORC1, IC50: 22 nM |
+
mTORC2, IC50: 65 nM |
99%+ | |||||||||||||||
| Ridaforolimus |
++++
mTOR, IC50: 0.2 nM |
99%+ | |||||||||||||||||
| Temsirolimus |
+
mTOR, IC50: 1.76 μM |
95% | |||||||||||||||||
| CZ415 |
++
mTOR, pIC50: 8.07 |
99%+ | |||||||||||||||||
| SF2523 |
+
mTOR, IC50: 280 nM |
DNA-PK | 99%+ | ||||||||||||||||
| KU-0063794 |
++
mTORC1, IC50: ~10 nM |
++
mTORC2, IC50: ~10 nM |
99%+ | ||||||||||||||||
| Omipalisib |
++++
mTORC1, Ki: 0.18 nM |
++++
mTORC2, Ki: 0.3 nM |
99%+ | ||||||||||||||||
| Palomid 529 | ✔ | 99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | WYE-125132 is a highly potent, ATP-competitive and specific mTOR kinase inhibitor with an IC50 of 0.19 nM, highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR. |
| Concentration | Treated Time | Description | References | |
| Human foreskin fibroblast cells (HFF) | 5 µM | 20 hours | WYE-132 significantly inhibited parasite growth and caused abnormal localization of TgGST2 | Parasit Vectors. 2022 Dec 12;15(1):461. |
| African green monkey kidney cells (Vero) | 5 µM | 20 hours | WYE-132 significantly inhibited parasite growth and caused abnormal localization of TgGST2 | Parasit Vectors. 2022 Dec 12;15(1):461. |
| HEK293 | 0.5 µM | 3 hours | Measure the level of tRNA precursors, WYE-132 significantly reduced pre-tRNA levels | J Biol Chem. 2010 May 14;285(20):15380-15392. |
| MG63 | 0.5 µM | 3 hours | Measure the level of tRNA precursors, WYE-132 significantly reduced pre-tRNA levels | J Biol Chem. 2010 May 14;285(20):15380-15392. |
| Administration | Dosage | Frequency | Description | References | ||
| Arabidopsis thaliana | A. thaliana WT and TOR/tor-1 heterozygotes | Solid medium | 0.01-1 μM | Single administration, lasting 6 days | WYE-132 inhibited Arabidopsis root growth, and TOR/tor-1 heterozygotes were twice as sensitive to WYE-132 as WT. | J Exp Bot. 2013 Nov;64(14):4361-74 |
| Drosophila melanogaster | Y w male Drosophila | Dietary supplementation | 10 pM to 1 µM | Lifelong supplementation | Testing the effect of WYE-132 on lifespan; a slight increase (5-6%) at the lowest dose (10 pM), but no significant effect at other doses | Int J Mol Sci. 2024 Oct 26;25(21):11504 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.92mL 0.38mL 0.19mL |
9.62mL 1.92mL 0.96mL |
19.25mL 3.85mL 1.92mL |
|
| CAS号 | 1144068-46-1 |
| 分子式 | C27H33N7O4 |
| 分子量 | 519.6 |
| SMILES Code | O=C(NC)NC1=CC=C(C2=NC(N3CC(O4)CCC4C3)=C5C(N(C(CC6)CCC76OCCO7)N=C5)=N2)C=C1 |
| MDL No. | MFCD22420813 |
| 别名 | WYE-125132 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 25 mg/mL(48.11 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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