PARP1/BRD4-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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。

PARP1/BRD4-IN-1

PARP1/BRD4-IN-1 Chemical Structure

CAS No. : 2758117-74-5

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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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd 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

2758117-74-5
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.
参考文献

  • [1]. Huang SH, et al. Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. Eur J Med Chem. 2022;230:114116.

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