2. Stem Cell/Wnt
  3. YAP
  4. OPN-9652

OPN-9652 是一种强效、口服有效的共价 TEAD 抑制剂 (对 MSTO-211H TEAD 的 IC50 为 0.005 µM)，靶向 TEAD 的中心棕榈酸酯结合口袋。OPN-9652 可降低 TEAD 依赖性报告基因活性和 TEAD 靶基因 (CTGF 和 CYR61) 的表达。OPN-9652 可使耐药的 SOX10 KO 细胞重新对 BRAFi + MAPKi 敏感。在 BRAF 突变 A375 异种移植小鼠模型中，OPN-9652 可延缓从微小残留病灶 (MRD) 阶段开始使用 BRAFi + MEKi 后肿瘤耐药性的出现。OPN-9652 可用于黑色素瘤研究。

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OPN-9652

OPN-9652 Chemical Structure

CAS No. : 2866423-35-8

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OPN-9652 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-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research[1].

IC50 & Target[1]

TEAD

0.005 μM (IC50)

分子量

365.32

Formula

C19H15F4NO2
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-9652 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

OPN-96522866423-35-8OPN9652OPN 9652YAPYes-associated proteinCTGFCYR61SOX10 KO cellsBRAFiMAPKiminimal residual diseaseBRAF mutant A375 xenograft mouse modelmelanomaInhibitorinhibitorinhibit

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