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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CC(C1=CC=C(NC(/C=C/C2=CC=C(CC)O2)=O)C=C1)=O
InChI
1S/C17H17NO3/c1-3-15-8-9-16(21-15)10-11-17(20)18-14-6-4-13(5-7-14)12(2)19/h4-11H,3H2,1-2H3,(H,18,20)/b11-10+
InChI 密鑰
SPTWXRJNCFIDRQ-ZHACJKMWSA-N
應用
Heclin已在人胚胎肾细胞(HEK293)中用作HECT型E3泛素连接酶抑制剂。它也用于检测其对HEK293细胞和成纤维样COS-7细胞系中蒲公英诱导氯离子通道蛋白(ClC-Ka)抑制的影响。
生化／生理作用
Heclin 是 HECT E3 泛素连接酶的选择性可逆抑制剂。Heclin 抑制 Nedd4、Smurf2 和 WWP1 的 IC50值分别为 6.3 μM、6.8 μM 和 6.9 μM，抑制体内 Smurf2 HECT 结构域的自体泛素化，IC50 值为 9 μM，Heclin 对 RING 结构域连接酶 Mdm2 的自体泛素化没有影响。
Heclin不能有效抑制E1或E2蛋白。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Thomas Mund et al.
Proceedings of the National Academy of Sciences of the United States of America, 111(47), 16736-16741 (2014-11-12)
The human genome encodes several hundred E3 ubiquitin ligases containing RING domains, and around 28 containing HECT domains. These enzymes catalyze the transfer of ubiquitin from E2 enzyme thioesters to a huge range of substrates and play crucial roles in
O2-dependent protein internalization underlies astrocytic sensing of acute hypoxia by restricting multimodal TRPA1 channel responses
Uchiyama M, et al.
Current Biology, 30(17), 3378-3396 (2020)
Jadier Redondo et al.
Neurobiology of learning and memory, 167, 107135-107135 (2019-12-11)
Ubiquitination is involved in synaptic plasticity and memory, but the involvement of HECT E3 ligases in these processes has not yet been established. Here, we bilaterally infused heclin, a specific inhibitor of some of these ligases, into the dorsal hippocampus
A Nedd4 E3 Ubiquitin Ligase Pathway Inhibits Robo1 Repulsion and Promotes Commissural Axon Guidance across the Midline.
Gorla, et al.
The Journal of Neuroscience, 42, 7547-7561 (2023)
Ke Wang et al.
Oncogene (2023-02-12)
The IGF1 signal pathway is highly activated in some subtype of gastric cancer(GC) that exhibits poor survival and chemotherapy resistance. Although the results of clinical trials of anti-IGF1R monoclonal antibodies and IGF-1R inhibitors have been mostly disappointing in unselected cancer
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