2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. PROTACs PARP
  4. iVeliparib-AP6

iVeliparib-AP6 是一种基于 Veliparb (HY-10129) 设计的蛋白水解靶向嵌合体 (PROTAC) 分子，靶向 PARP1/2。iVeliparib-AP6 诱导 PARP1 和 PARP2 降解的 DC50s 分别为 36 nM 和 63 nM，IC50s 分别为 69 nM 和 21 nM。iVeliparib-AP6 包含一个基于 Veliparib 的 PARP 抑制剂弹头，该弹头与 CRBN E3 连接酶结合体相连；并以 Thalidomide (HY-14658) 作为配体招募 CRBN E3 泛素连接酶，发挥 PARP2 降解机制。

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iVeliparib-AP6

iVeliparib-AP6 Chemical Structure

CAS No. : 2472645-27-3

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iVeliparib-AP6 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) molecule designed based on Veliparib (HY-10129), which targets PARP1/2. The DC50s of iVeliparib-AP6 for inducing the degradation of PARP1 and PARP2 are 36 nM and 63 nM, respectively, and its IC50s are 69 nM and 21 nM, respectively. iVeliparib-AP6 contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder; it uses Thalidomide (HY-14658) as a ligand to recruit CRBN E3 ubiquitin ligase and exerts the PARP2 degradation mechanism[1][2].

IC50 & Target

PARP1

69 nM (IC50)

PARP2

21 nM (IC50)

PARP1

36 nM (ED50)

PARP2

63 nM (ED50)

Cereblon

 

体外研究
(In Vitro)

iVeliparib-AP6 (10 min) 在无细胞实验中可抑制 PARP1 和 PARP2 的催化活性，对应的 IC50 值分别为 69 nM 和 21 nM[1]。

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

iVeliparib-AP6 相关抗体:
分子量

807.89

Formula

C40H53N7O11
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

iVeliparib-AP6 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:

iVeliparib-AP62472645-27-3PROTACsPARPpoly ADP ribose polymerasePARP1thalidomideCRBN E3 ligaseproteasomal degradationproteolysis targeting chimeraPARP2CRBN E3 ubiquitin ligaseInhibitorinhibitorinhibit

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产品名称：
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目录号：
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