EN6 是一种小分子自噬激活剂,共价靶向溶酶体 v-ATPase 的 ATP6V1A 亚基中的半胱氨酸 277,通过 Rag 鸟苷三磷酸酶激活机械靶 mTORC1。EN6 介导的 ATP6V1A 修饰使 v-ATPase 与 Rags 解耦,导致 mTORC1 信号抑制、溶酶体酸化增加和自噬激活。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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产品名称 | ATPase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
(-)-Blebbistatin | 99%+ | ||||||||||||||||||
PF 03716556 |
++++
H+/K+-ATPase, pIC50: ~6.5 |
98% | |||||||||||||||||
Esomeprazole sodium | ✔ | 98% | |||||||||||||||||
BTB06584 | ✔ | 98% | |||||||||||||||||
Ciclopirox | ✔ | 97% | |||||||||||||||||
CB-5083 |
++++
p97 AAA ATPase, IC50: 11 nM |
99%+ | |||||||||||||||||
Ciclopirox olamine | ✔ | 99% | |||||||||||||||||
Brefeldin A |
+++
ATPase (HCT 116), IC50: 0.2 μM |
99%+ | |||||||||||||||||
Oligomycin A | ✔ | 99% | |||||||||||||||||
Sodium orthovanadate |
+++
(Na,K)-ATPase, IC50: 40 nM |
99% | |||||||||||||||||
Golgicide A | ✔ | 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。 |
描述 | The vacuolar H+-ATPase (v-ATPase) is a universal component of eukaryotic organisms, which is present in both intracellular compartments and the plasma membrane. Its proton-pumping action creates the low intravacuolar pH, benefiting many processes such as, membrane trafficking, protein degradation, renal acidification, bone resorption, and tumor metastasis [1]. EN6 is a small-molecule activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase, which activates mechanistic target of rapamycin complex 1 (mTORC1) via the Rag guanosine triphosphatases. EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner [2]. |
作用机制 | EN6 covalently binds to cysteine 277 in the ATP6V1A subunit of v-ATPase . |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.71mL 0.54mL 0.27mL |
13.57mL 2.71mL 1.36mL |
27.15mL 5.43mL 2.71mL |
CAS号 | 1808714-73-9 |
分子式 | C19H14F2N4O2 |
分子量 | 368.337 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 4 mg/mL(10.86 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 无水乙醇: 1 mg/mL(2.71 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 |
动物实验配方 |