2. Cell Cycle/DNA Damage Epigenetics
  3. PARP Epigenetic Reader Domain
  4. PCIP-1

PCIP-1 是一种 PARP2 抑制剂。PCIP-1 可招募 BET 蛋白至 PARP2 以抑制 DNA 修复，通过事件驱动药理学发挥作用且不抑制 PARP 催化的 PARylation。PCIP-1 可抑制 DNA 修复，从而在同源重组缺陷的癌细胞中产生合成致死效应，并提高 PARP1 敲除细胞的敏感性。PCIP-1 可用于同源重组缺陷型癌症、T 细胞急性淋巴细胞白血病以及 BRCA 突变型癌症的研究。

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PCIP-1

PCIP-1 Chemical Structure

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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Customer Review

PCIP-1 相关抗体

Top Publications Citing Use of Products

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

PCIP-1 is a PARP2 inhibitor. PCIP-1 recruits BET proteins to PARP2 to inhibit DNA repair, acts via event-driven pharmacology, and does not inhibit PARP-catalyzed PARylation. PCIP-1 inhibits DNA repair, thereby inducing synthetic lethality in homologous recombination-deficient cancer cells and increasing the sensitivity of PARP1-knockout cells. PCIP-1 can be used in the research of homologous recombination-deficient cancers, T-cell acute lymphoblastic leukemia, and BRCA-mutant cancers[1].

IC50 & Target[1]

PARP2

 

BET

 

体外研究
(In Vitro)

PCIP-1 可在体外诱导 BRD4 溴结构域 1 与 PARP1 催化结构域形成三元复合物，该过程通过 HTRF 信号检测[1]。
PCIP-1 (Up to 50 µM; 2 h pre-incubation with PCIP-1, followed by 45 min incubation with dBET6) 在 Jurkat-BRD4-HiBit 细胞中对 BRD4 表现出微弱、非饱和的结合作用，其 EC50 为 26 µM，且它的抗增殖活性并非由基于占据机制的 BRD4 抑制作用介导[1]。
PCIP-1 (1 nM-100 μM; 72 h) 可强效抑制 Jurkat T 细胞活力，其 IC50 为 662 nM；在 DNA 损伤剂 MMS 存在时，其活性可提升 14 倍以上 (IC50 = 45 nM)[1]。
PCIP-1 (1 µM; 4 h) 可诱导 22Rv1 细胞中 BET 蛋白 (BRD4) 与 PARP1/2 发生近距离相互作用，这一点可通过这些蛋白对的免疫共沉淀水平升高得到证实[1]。
PCIP-1 (100 nM-10 µM; 24 h) 可抑制 MMS 诱导的 DNA 损伤修复，并诱导 Jurkat 细胞发生凋亡，且不会抑制整体 PARP 催化的 PARylation[1]。
PCIP-1 (100 nM-1 µM; 24 h) 可诱导 Jurkat 细胞发生 S 期细胞周期阻滞，这与 DNA 损伤修复受到抑制的结果一致[1]。
PCIP-1 (1 µM; up to 14 days) 可降低 PARP2 功能正常的 Jurkat-Cas9 细胞的竞争适配性，从而使 PARP2 缺陷型细胞被选择性富集，证明 PCIP-1 的活性依赖于 PARP2[1]。
PCIP-1 (0.1 nM-10 μM; 6 days) 在 DLD1 结肠癌细胞中与 BRCA2 缺陷表现出合成致死效应，其中 BRCA2K/O 细胞的敏感性比亲本细胞高 100 倍以上[1]。

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

PCIP-1 相关抗体:

Cell Viability Assay[1]

Cell Line: Jurkat T-cell acute lymphoblastic leukemia (T-ALL) cells
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM
Incubation Time: 72 h
Result: Inhibited Jurkat cell viability with an IC50 of 662 nM.
Improved the IC50 to 45 nM in the presence of 25 µM methyl methanesulfonate (MMS).

Western Blot Analysis[1]

Cell Line: Jurkat T-cell acute lymphoblastic leukemia (T-ALL) cells
Concentration: 100 nM-10 µM (24 h incubation); 1 µM (time-course incubation)
Incubation Time: 24 h (dose-response); 12, 16, 24 h (time-course)
Result: Induced accumulation of the DNA damage marker γH2AX, especially with MMS.
Caused dose-responsive and time-dependent increases in cleaved PARP1/2 and cleaved Caspase 3.
Showed minimal effects on global PARylation levels.

Cell Cycle Analysis[1]

Cell Line: Jurkat T-cell acute lymphoblastic leukemia (T-ALL) cells
Concentration: 100 nM, 1 µM
Incubation Time: 24 h
Result: Induced a strong S-phase arrest.
分子量

833.41

Formula

C45H46ClFN8O3S
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

PCIP-1 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:

PCIP-1PCIP1PCIP 1PARPEpigenetic Reader Domainpoly ADP ribose polymeraseBET proteinsBRCA mutated cancershomologous recombination deficienciest-cell acute lymphoblastic leukemiaJurkat cellsPARP1 catalytic domainDNA repairPARP2DLD1 colon cancer cellsBRD4 bromodomain 1Inhibitorinhibitorinhibit

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