SMILES string
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 key
SPTWXRJNCFIDRQ-ZHACJKMWSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
Quality Level
相关类别
Application
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。
Biochem/physiol Actions
HECT E3 泛素连接酶抑制剂
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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
Zeming Zhang et al.
Journal of immunology (Baltimore, Md. : 1950), 204(7), 1904-1918 (2020-02-23)
IFN regulatory factor 3 (IRF3) is critical for the transcription of type I IFNs in defensing virus and promoting inflammatory responses. Although several kinds of posttranslational modifications have been identified to modulate the activity of IRF3, whether atypical ubiquitination participates
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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