1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. PDI
  3. BAP2

BAP2 是一种别构蛋白质二硫键异构酶 (PDI) 抑制剂,其 IC50 为 0.85 μM。BAP2 结合于 PDI b′结构域的 His256,依赖变构结合 b′结构域发挥抑制作用。BAP2 可上调 GRP78。BAP2 抑制胶质母细胞瘤细胞生长。BAP2 可用于胶质母细胞瘤的相关研究。

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BAP2

BAP2 Chemical Structure

CAS No. : 2284589-16-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BAP2 is an allosteric protein disulfide isomerase (PDI) inhibitor with a IC50 of 0.85 μM. BAP2 binds to His256 in the b′ domain of PDI and exerts inhibitory effects through allosteric binding to the b′ domain. BAP2 upregulates GRP78. BAP2 inhibits the growth of glioblastoma cells. BAP2 can be used in studies related to glioblastoma[1].

体外研究
(In Vitro)

BAP2 (1 h) 可强效抑制重组野生型 PDI 还原酶活性,其 IC50 为 0.85 μM[1]
BAP2 与重组野生型 PDI 结合,通过等温滴定量热法测定的 Kd 值为 9.1 μM[1]
BAP2 可中度抑制 U87MG、A172 和 NU04 胶质母细胞瘤细胞的活力,其 IC50 值介于 10.3 μM 至 16.8 μM 之间;与正常 HFF-1 成纤维细胞相比,它对 NU04 细胞的效力高 5.8 倍[1]
BAP2 (20 μM; 2-24 h) 可通过 GRP78 的表达量,在 U87MG 和 A172 胶质母细胞瘤细胞中诱导内质网应激,且不会改变 PDI 的水平[1]
BAP2 (10-30 μM; 24 h) 可在伤口愈合实验中抑制 A172 胶质母细胞瘤细胞的迁移[1]
BAP2 (1 μM; 10-12 days) 与电离辐射协同作用,降低 D54 胶质母细胞瘤细胞的克隆形成存活率[1]

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

Western Blot Analysis[1]

Cell Line: U87MG and A172 human glioblastoma cells
Concentration: 20 μM
Incubation Time: 2 h (EIF2α phosphorylation analysis); 24 h (GRP78 expression analysis)
Result: Upregulated expression of GRP78, a marker of ER stress.
Left PDI expression unchanged.
分子量

249.26

Formula

C16H11NO2

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
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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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HY-W851050A
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