1. PROTAC
  2. Ligands for E3 Ligase Ligands for Target Protein for PROTAC
  3. AR antagonist 1

AR antagonist 1 (compound 29) 是一种有效的 AR 拮抗剂,与 E3 连接酶配体结合,与 VHL 蛋白结合亲和力较弱,用于合成PROTAC ARD-266 (HY-133020)。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 AR antagonist 1 hydrochloride 通常具有更好的水溶性和稳定性。

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AR antagonist 1 Chemical Structure

AR antagonist 1 Chemical Structure

CAS No. : 1818885-54-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

IC50 & Target

IC50: androgen receptor[1]

体外研究
(In Vitro)

AR antagonist 1 (compound 29) is the ligand for target ligase of ARD-266. ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader.
AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex, it can be successfully employed for the design of highly potent and efficient PROTAC degraders.
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein.
PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

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

分子量

278.78

Formula

C15H19ClN2O

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
  • 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 *
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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.

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产品名称:
AR antagonist 1
目录号:
HY-130845
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