2. Stem Cell/Wnt
  3. YAP
  4. OPN-9643

OPN-9643 是一种针对 TEADs 中央棕榈酰结合口袋的共价抑制剂，IC50 为 15 nM，可防止自棕榈酰化并降低 TEAD-驱动的荧光素酶活性和经典 TEAD 靶基因，如 CTGF 和 CYR61。OPN-9643 可用于癌症的研究，如黑色素瘤。

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OPN-9643

OPN-9643 Chemical Structure

CAS No. : 2866423-06-3

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OPN-9643 相关抗体

Top Publications Citing Use of Products

查看 YAP 亚型特异性产品:

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OPN-9643 is a covalent inhibitor targeting the central palmitate binding pocket of TEADs with an IC50 of 15 nM, preventing autopalmitoylation and reducing TEAD-driven luciferase activity and canonical TEAD targets, CTGF and CYR61. OPN-9643 can be used for the research of cancer, such as melanoma[1].

IC50 & Target.
[1]

TEAD

15 nM (IC50)

体外研究
(In Vitro)

OPN-9643 (2 µM；24-48 小时) 可降低 SOX10 KO 细胞中 TEAD 靶基因 (CTGF 和 CYR61) 的表达。OPN-9643 可降低荧光素酶活性。OPN-9643 还可降低 SOX10 KO 黑色素瘤细胞中其他已知的 TEAD 靶基因 (如 DKK1、MYC 和 TGF-β2) 的表达[1]。
OPN-9643 (NCI-H226 细胞；5 天) 抑制了 NCI-H226 细胞中的 TEAD 活性和细胞增殖 (IC50 值为 123 nM)[1]。
与 BRAFi (BRAF 抑制剂) + MEKi (MEK 抑制剂) 联合使用时，与 OPN-9643 (2 μM；48-72 小时) 相比，可显著降低 A375 SOX10 KO 细胞的生长[1]。
OPN-9643 (2 μM; 48 h) 可增加联合处理的 SOX10 KO 细胞中 cleaved-PARP 和 cleaved-GSDME 的水平。

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

OPN-9643 相关抗体:

Western Blot Analysis[1]

Cell Line: A375 parental, A375 crSOX10 #2.18, and A375 crSOX10 #4.21 cells  
Concentration: 2 μM
Incubation Time: 24 h, 48 h
Result: Western blotting analysis detected a reduction in CTGF and CYR61 protein expression in SOX10 KO cells. 
Down-regulated the cell cycle progression regulators (FOXM1 and PLK1), growth factor receptors (phospho-cMET Y1234/5, AXL), a serine protease inhibitor (PAI1), and RAD51. 
分子量

347.33

Formula

C19H16F3NO2
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

OPN-9643 相关分类

  • 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.

Keywords:

OPN-96432866423-06-3OPN9643OPN 9643YAPYes-associated proteinactive TAZCYR61MEK inhibitorsMAPK-targeted therapiesTEAD targetsCTGFTEAD-dependent reporter activitySOX10 knockout cellscovalent inhibitorsBRAF inhibitorsacquired resistanceInhibitorinhibitorinhibit

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