1. Immunology/Inflammation
  2. Toll-like Receptor (TLR) IFNAR Interleukin Related
  3. ENDO12

ENDO12 是一种 Munc13-4-STX7 蛋白复合物抑制剂,对 STX7 的 Kd 值为 2.7 µM。ENDO12 可阻断 Munc13-4-STX7 的相互作用。ENDO12 可抑制内溶酶体通量、内溶酶体货物降解、中性粒细胞中的细胞外信号调节激酶信号通路、浆细胞样树突状细胞中的 IFN 调节因子信号通路,以及原代树突状细胞对 TLR3TLR7TLR9 的应答。ENDO12 可通过降低髓过氧化物酶、IL-6IFNγ 的水平,减轻 CpG 诱导的全身性炎症。ENDO12 不会干扰宿主对淋巴细胞脉络丛脑膜炎病毒感染的抗病毒应答。\nENDO12 可用于全身性炎症的相关研究。

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ENDO12

ENDO12 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ENDO12 is an inhibitor of the Munc13-4-STX7 protein complex, with a Kd value of 2.7 µM for STX7. ENDO12 blocks the interaction of Munc13-4-STX7. ENDO12 inhibits endolysosomal flux, endolysosomal cargo degradation, the extracellular signal-regulated kinase signaling pathway in neutrophils, the IFN regulatory factor signaling pathway in plasmacytoid dendritic cells, and the responses of primary dendritic cells to TLR3, TLR7, and TLR9. ENDO12 alleviates CpG-induced systemic inflammation by reducing the levels of myeloperoxidase, IL-6 and IFNγ. ENDO12 does not interfere with the host's antiviral response to lymphocytic choriomeningitis virus infection.\nENDO12 can be used in studies related to systemic inflammation[1].

IC50 & Target[1]

IL-6

 

TLR3

 

TLR9

 

TLR7

 

体外研究
(In Vitro)

ENDO12 (31.25 nM-3 μM) 与重组 STX7 结合,其 Kd 值为 2.7 µM,亲和力高于 ENDO3[1]
ENDO12 可强效抑制 HEK-Blue hTLR9 细胞中 CpG 诱导的 TLR9 激活,其 IC50 为 1 × 10-7 M[1]
ENDO12 (10 µM; 1 h) 可降低 RAW 264.7 小鼠巨噬细胞中 STX7 与 Munc13-4、TLR7 与 LAMP1、TLR9 与 LAMP1 的共定位水平,从而抑制内体成熟和 TLR 转运[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence[1]

Cell Line: RAW 264.7 murine macrophages
Concentration: 10 µM
Incubation Time: 1 h
Result: Significantly decreased colocalization of STX7 with Munc13-4.
Significantly decreased colocalization of TLR7 and TLR9 with LAMP1+ organelles, indicating impaired endosomal maturation and TLR trafficking to late endolysosomes.
体内研究
(In Vivo)

ENDO12 (30 mg/kg;腹腔注射;单次;CpG 攻击前 1 小时) 可减轻小鼠体内 CpG 诱导的全身性炎症,降低血浆 IL-6、IFNγ 及 MPO 水平[1]
ENDO12 (15 mg/kg;腹腔注射;单次;淋巴细胞脉络丛脑膜炎病毒感染前 1 小时) 不会削弱小鼠对淋巴细胞脉络丛脑膜炎病毒 (LCMV) 感染的宿主抗病毒应答,仅会使 MIP1β 和 MIP2 水平出现轻微降低[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (male and female, 6-10 weeks old)[1]
Dosage: 30 mg/kg
Administration: i.p.; single dose; 1 hour before CpG challenge
Result: Significantly reduced CpG-induced plasma levels of interleukin 6 (IL-6), interferon gamma (IFNγ), and myeloperoxidase (MPO) compared to vehicle-treated controls.
Animal Model: C57BL/6J mice (male and female, 8 weeks old)[1]
Dosage: 15 mg/kg
Administration: i.p.; single dose; 1 hour before LCMV infection
Result: Did not significantly alter plasma levels of IL-6, IFNα, IFNγ, or MPO induced by LCMV infection.
Caused only a mild reduction in plasma levels of macrophage inflammatory proteins MIP1β and MIP2, while all other measured cytokines and chemokines remained unchanged compared to vehicle-treated controls.
分子量

288.32

Formula

C15H17FN4O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ENDO12
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HY-183079
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