1. Stem Cell/Wnt
  2. β-catenin
  3. CGK012

CKG012 是 Wnt/βcatenin 信号通路抑制剂。CGK012 抑制 HMGB1 的释放和 β-catenin 的转录,对改善盲肠结扎和穿刺引发的脓毒症和多发性骨髓瘤癌症具有活性。

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CGK012 Chemical Structure

CGK012 Chemical Structure

CAS No. : 2044497-76-7

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CKG012 is an inhibitor for Wnt/βcatenin signaling pathway. CGK012 inhibits release of HMGB1 and transcription of β-catenin, exhibits attenuating activities against cecal ligation and puncture (CLP)-induced sepsis and multiple myeloma cancer[1][2].

体外研究
(In Vitro)

CGK012 (0-20 μM) 通过抑制 LPS 诱导的 HMGB1 乙酰化和 SIRT1 表达来抑制 HMGB1 释放,从而降低 HUVEC 中过度的血管通透性,降低 TLR2/4 等病原体相关分子的表达,而不影响 HUVEC 的细胞活力[1]
CGK012 (0-20 μM) 通过减少炎症免疫细胞的粘附和迁移,抑制 IL-6、TNF-α、β 等促炎细胞因子以及转录因子 NF-kB 和 ERK1/2 的产生来改善炎症反应[1]
CGK012 (0-20 μM) 促进 β-catenin 磷酸化和降解并抑制 β-catenin 依赖性基因的表达,抑制多发性骨髓瘤细胞 RPMI-8226 的增殖,IC50 为 5.08 μM[2]

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

Cell Viability Assay[1]

Cell Line: HUVEC
Concentration: 5-100 μM
Incubation Time: 48 h
Result: Revealed no effects on cell viability.

Western Blot Analysis[1]

Cell Line: HUVECs, HEK293-FL reporter, RPMI-8226
Concentration: 0-20 μM
Incubation Time: 12 h
Result: Reduced levels of SIRT1 and acetylation of HMGB1, inhibited vascular permeability in HUVECs. Reduced levels of β-catenin in HEK293-FL reporter and RPMI-8226.

Cell Migration Assay [1]

Cell Line: HUVEC
Concentration: 0-20 μM
Incubation Time: 6 h
Result: Inhibited migration of neutrophils through monolayers of HUVECs.
体内研究
(In Vivo)

CGK012 (0.05-0.53 mg/kg,静脉注射,双剂量) 抑制 HMGB1 释放和免疫细胞迁移,提高由盲肠结扎和穿刺引发脓毒症的 C57BL/6 小鼠血管细胞稳定性和小鼠存活率[1]

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

Animal Model: CLP- induced sepsis in C57BL/6 mice[1]
Dosage: 0.26-0.53 mg/kg
Administration: double doses, 12 or 50 h after surgery.
Result: Reduced expression of HMGB1 and improved the survival rate.
分子量

357.40

Formula

C20H23NO5

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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  • 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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产品名称:
CGK012
目录号:
HY-163409
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