1. PI3K/Akt/mTOR Immunology/Inflammation
  2. PIKfyve Interleukin Related MHC
  3. AS2677131

AS2677131 是一种强效且具有口服活性的 PIKfyve 抑制剂。AS2677131 通过 PIKfyve-c-Rel 通路抑制 IL-12p40、IL-6 和 IL-1β。AS2677131 选择性抑制 c-Rel 与 IL-12p40 和 IL-1β 启动子的 DNA 结合活性。AS2677131 抑制 B 细胞上MHC II 类分子的表达。AS2677131 可用于炎症和免疫学研究,如关节炎。

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AS2677131

AS2677131 Chemical Structure

CAS No. : 2171502-44-4

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AS2677131 is a potent and orally active PIKfyve inhibitor. AS2677131 inhibits f IL-12p40, IL-6 and IL-1β through a PIKfyve-c-Rel pathway. AS2677131 selectively inhibits DNA-binding activity of c-Rel to IL-12p40 and IL-1β promoter. AS2677131 inhibits MHC class II expression on B cells. AS2677131 can be used for the researches of inflammation and immunology, such as arthritis[1].

IC50 & Target[1]

IL-12

 

IL-1β

 

IL-6

 

MHC II

 

体外研究
(In Vitro)

AS2677131 抑制 IL-12p40 的产生,IC50 值为 2.4 nM, 并降低 RAW264.7 小鼠巨噬细胞中 IL-1β 和 IL-6 的水平[1]
AS2677131 (0.1-10000 nM) 可抑制小鼠腹腔巨噬细胞中的 IL-12p40 和 IL-6[1]
AS2677131 (0.1-10000 nM) 能抑制小鼠骨髓来源的树突状细胞中的 IL-12p40 和 IL-6[1]
AS2677131 (10 μM) 对 Ramos 细胞中细胞内 Ca2+ 内流无显著影响[1]
AS2677131 (200 nM) 可抑制 RAW264.7 细胞中 PI (3,5) P2 的产生,抑制率超过 90%[1]
AS2677131 (100 nM, 2 h) 会增大 RAW264.7 细胞的体积,并诱导细胞质中产生大量小囊泡[1]
AS2677131 (10-100 nM, 2h) 会降低 RAW264.7 细胞中启动子的活性,并抑制 c-Rel 与 IL-12p40 和 IL-1β 启动子的结合[1]
AS2677131 (100 nM, 2 h) 会降低 RAW264.7 细胞中的 p-Akt 水平[1]

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

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 100 nM
Incubation Time: 2 h
Result: Reduced p-Akt levels.
体内研究
(In Vivo)

AS2677131 (1-30 mg/kg,口服) 可降低经 Poly (I:C) (HY-107202) 和 MDP (HY-127090) 处理的大鼠血浆中 IL-12p40、IL-6 和 TNFα 的水平[1]
AS2677131 (1-10 mg/kg,口服) 可降低大鼠 CD45R+ B 细胞表面 MHC II 类分子的表达[1]
AS2677131 (1-10 mg/kg,口服,每日一次,持续 24 天) 可减轻佐剂诱导的关节炎大鼠的炎症[1]

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

Animal Model: Rats with adjuvant-induced arthritis[1]
Dosage: 1, 3 and 10 mg/kg
Administration: Orally administration, daily for 24 days
Result: Reduced paw swelling (swelling inhibition rates of 34.3% and 78.3% at doses of 3 and 10 mg/kg, respectively).
Reversed body weight loss.
Decreased joint histological scores (including bone destruction, cartilage destruction, synovial thickening, and inflammatory cell infiltration.
Reduced the proportion of CD3-CD45RA+CD62Llow activated B cells in peripheral blood.
分子量

470.57

Formula

C27H30N6O2

CAS 号
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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AS2677131
目录号:
HY-123876
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