| Bioactivity | 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]. |
| Invitro | 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. 0 --> CGK012 相关抗体: Cell Viability Assay[1] Cell Line: |
| 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: |
| CAS | 2044497-76-7 |
| Formula | C20H23NO5 |
| Molar Mass | 357.40 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Park YJ, et al., Antiseptic Functions of CGK012 against HMGB1-Mediated Septic Responses. Int J Mol Sci. 2024 Mar 4;25(5):2976. [2]. Choi PJ,et al., Anti-proliferative activity of CGK012 against multiple myeloma cells via Wnt/β-catenin signaling attenuation. Leuk Res. 2017 Sep;60:103-108. |