1. Metabolic Enzyme/Protease Apoptosis Cell Cycle/DNA Damage
  2. HIF/HIF Prolyl-Hydroxylase Apoptosis HSP Caspase
  3. HIF-2α-IN-17

HIF-2α-IN-17 是一种选择性缺氧诱导因子 2α (HIF2α) 抑制剂,可与 HIF2α 的 PAS-B 结构域结合。HIF-2α-IN-17 可破坏 HIF2α 与分子伴侣 Hsp70 的相互作用,并诱导 HIF2α 的蛋白酶体降解。HIF-2α-IN-17 具有抗肿瘤的活性,可诱导癌细胞凋亡 (apoptosis)。HIF-2α-IN-17 可用于透明细胞肾癌等癌症的研究。

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HIF-2α-IN-17

HIF-2α-IN-17 Chemical Structure

CAS No. : 861212-49-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HIF-2α-IN-17 is a selective hypoxia-inducible factor 2α (HIF2α) inhibitor that binds to the PAS-B domain of HIF2α. HIF-2α-IN-17 disrupts the interaction between HIF2α and the molecular chaperone Hsp70, leading to proteasomal degradation of HIF2α. HIF-2α-IN-17 exhibits antitumor activity and induces apoptosis in cancer cells. HIF-2α-IN-17 is applicable for research on cancers such as clear cell renal cell carcinoma[1].

IC50 & Target[1]

HSP70

 

HIF-2α

 

Caspase-3

 

Caspase-7

 

体外研究
(In Vitro)

HIF-2α-IN-17 (Compound-c2) (0-30 μM;24 小时) 可选择性抑制 VHL 缺失的肾透明细胞癌 (ccRCC) 细胞系 (786-O、A498) 的活力,而对 VHL 阳性的 Caki-1 细胞或正常 HEK293 细胞无影响[1]
HIF-2α-IN-17 (5-30 μM;24 小时) 通过激活 caspase-3 和 caspase-7 诱导 786-O 细胞发生细胞凋亡[1]
HIF-2α-IN-17 (0-30 μM;8-24 小时) 可抑制 786-O 细胞中 HIF2α 的转录活性,并降低 HIF2α 靶基因 (VEGF、NDRG2、CCND1、GLUT1) 的表达水平[1]

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

Western Blot Analysis[1]

Cell Line: 786-O
Concentration: 0, 5, 10, 20 and 30 μM
Incubation Time: 24 h
Result: Increased levels of cleaved caspase-3 and cleaved caspase-7 in a concentration-dependent manner.

Real Time qPCR[1]

Cell Line: 786-O
Concentration: 15 and 30 μM
Incubation Time: 24 h
Result: Downregulated mRNA expression of VEGF, NDRG2, CCND1, and GLUT1 in a concentration-dependent manner.
分子量

311.31

Formula

C17H14FN3O2

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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产品名称:
HIF-2α-IN-17
目录号:
HY-W470101
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