2. Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. Epigenetic Reader Domain PARP Apoptosis DNA/RNA Synthesis
  4. PARP1/BRD4-IN-1

PARP1/BRD4-IN-1 是一种有效、且具有高选择性的 PARP1/BRD4 抑制剂，PARP1 与 BRD4 的 IC50分别为 49 nM 与 202 nM。PARP1/BRD4-IN-1 通过抑制 PARP1 和 BRD4 的表达与活性，协同抑制胰腺癌细胞的恶性生长。

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PARP1/BRD4-IN-1 Chemical Structure

PARP1/BRD4-IN-1 Chemical Structure

CAS No. : 2758117-74-5

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PARP1/BRD4-IN-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

PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells[1].

IC50 & Target

BRD4

202 nM (IC50)

PARP1

49 nM (IC50)

体外研究
(In Vitro)

PARP1/BRD4-IN-1 (compound III-7) (0-2 μM; 3-7 days) has potent inhibition of the growth of cancer cell lines[1].
PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) can significantly inhibit the expression of PARP1 and BRD4 at 2 μM in SW1990 cells[1].
PARP1/BRD4-IN-1 (1, 2 μM; 4 days) arrests the cell cycle at G0/G1 and G2/M phase in SW1990 cells[1].
PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) has the potent efficacy on the apoptosis of SW1990 cells at 2 μM[1].
PARP1/BRD4-IN-1 (1, 2 μM; 4 days) regulates the expression of HEXIM1, c-Myc, FOXO1, MDC1 and TOPBP1 to enhance the inhibition of DNA repair in SW1990 cells[1].

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

PARP1/BRD4-IN-1 相关抗体:

Cell Proliferation Assay

Cell Line: CFPAC-1, SW1990, MDA-MB-231, MDA-MB-468, HCT-116, THP-1[1]
Concentration: 0-2 μM
Incubation Time: 3, 4 or 7 days
Result: Showed potent inhibition of the growth of cancer cell lines.

Western Blot Analysis

Cell Line: SW1990[1]
Concentration: 0, 1, 2 μM
Incubation Time: 4 days
Result: Significantly inhibited the expression of PARP1 and BRD4 at 2 μM.

Cell Cycle Analysis

Cell Line: SW1990[1]
Concentration: 1, 2 μM
Incubation Time: 4 days
Result: Arrested the cell cycle at G0/G1 and G2/M phase.

Apoptosis Analysis

Cell Line: SW1990[1]
Concentration: 0, 1, 2 μM
Incubation Time: 4 days
Result: Showed potent efficacy on the apoptosis of SW1990 cells at 2 μM.
体内研究
(In Vivo)

PARP1/BRD4-IN-1 (30mg/kg; intraperitoneal injection for 28 days) can significantly inhibit the tumor size and weight, and does not cause significant damage of the kidney, lung, spleen, liver and heart in mice[1].

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

Animal Model: Athymic nude mice (6-7 weeks, 18-20 g, SW1990-injected)[1]
Dosage: 30mg/kg
Administration: Intraperitoneal injection for 28 days
Result: Significantly inhibited the tumor size and weight and did not cause significant damage of the kidney, lung, spleen, liver and heart.
分子量

506.56

Formula

C29H26N6O3
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

PARP1/BRD4-IN-1 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:

PARP1/BRD4-IN-12758117-74-5Epigenetic Reader DomainPARPApoptosisDNA/RNA Synthesispoly ADP ribose polymerase PARP1BRD4SelectiveCell cycleDNA damageHR repairPancreaticCancerSW1990Inhibitorinhibitorinhibit

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