2. M4K3233

M4K3233 是一种选择性的 ALK2 PROTAC 降解剂，其 pDC50 为 7.3，pIC50 为 6.6。M4K3233 可募集 CRBN 与 ALK2 形成三元复合物，通过蛋白酶体和溶酶体途径介导 ALK2 降解。M4K3233 可诱导 RIPK2 中度下调以及 SIK3 显著下调。M4K3233 可用于胶质母细胞瘤的相关研究。
(粉色: ALK2 配体 (HY-149591)；蓝色: Cereblon 配体 (HY-14658)；黑色: 连接子)。

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M4K3233

M4K3233 Chemical Structure

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M4K3233 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

M4K3233 is a selective ALK2 PROTAC degrader with a pDC50 of 7.3 and a pIC50 of 6.6. M4K3233 recruits CRBN to form a ternary complex with ALK2, mediating ALK2 degradation via the proteasomal and lysosomal pathways. M4K3233 induces moderate downregulation of RIPK2 and significant downregulation of SIK3 in mammalian cells. M4K3233 is applicable to research related to glioblastoma[1]. (Pink: ALK2 ligand (HY-149591); Blue: Cereblon ligand (HY-14658); Black: linker).

体外研究
(In Vitro)

M4K3233 (1 μM; 24 h) 是 ALK2 过表达 HEK-293 细胞和 U87-MG 胶质母细胞瘤细胞中的选择性 ALK2 降解剂，可显著降低 ALK2 水平以及包括 PDE6D、FIZ1、SIK3 和 RIPK2 在内的一小部分脱靶蛋白水平，同时对大多数其他激酶无影响[1]。
M4K3233 (4 h) 在 HEK-293 细胞中促进 ALK2 与 CRBN 之间形成三元复合物，其表观 pEC50 为 7.42[1]。
M4K3233 (0.0002-30 μM; 8 days) 可抑制患者来源的 PDHGG 细胞系增殖，其 GI50 值为 0.3 μM 至 5 μM，但该效应不依赖于 CRBN 介导的 ALK2 降解[1]。
M4K3233 (0.0002-30 μM; 4 days) 可降低 U87-MG 胶质母细胞瘤细胞的存活率，但该细胞毒性作用不依赖于 CRBN 介导的 ALK2 降解[1]。

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

M4K3233 相关抗体:

Western Blot Analysis[1]

Cell Line: ALK2-HiBiT transfected HEK-293 cells
Concentration: 1 μM (M4K3233, 24 h incubation); 20 μM pomalidomide (20 min pretreatment); 20 μM M4K2009 (20 min pretreatment); 1 μM MG132 (20 min pretreatment); 1 μM bafilomycin A1 (20 min pretreatment)
Incubation Time: 24 h (M4K3233 treatment); 20 min (pretreatments)
Result: Blocked ALK2 degradation when cells were pretreated with either pomalidomide or M4K2009, confirming reliance on both ALK2 and CRBN binding.
Partially recovered ALK2 levels when cells were pretreated with either MG132 or bafilomycin A1, while combined pretreatment with both inhibitors completely blocked ALK2 degradation.
分子量

772.89

Formula

C44H48N6O7
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

M4K3233 相关分类

  • 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.

Keywords:

M4K3233human liver microsomesmouse liver microsomesALK2SIK3CRBNPDE6DFIZ1HEK-293 cellsALK5RIPK2Inhibitorinhibitorinhibit

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