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

PARP1/BRD4-IN-2 是一种有效且具有选择性的 PARP1 和 BRD4 抑制剂，IC50 分别为 197 nM 和 238 nM。PARP1/BRD4-IN-2 抑制 DNA 损伤修复，阻止 G0/G1 细胞周期转变，诱导细胞凋亡 (apoptosis)。PARP1/BRD4-IN-2 在MDA-MB-468小鼠异种移植瘤模型中具有抗肿瘤活性。PARP1/BRD4-IN-2 可用于三阴性乳腺癌 (TNBC) 的研究。

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PARP1/BRD4-IN-2 Chemical Structure

PARP1/BRD4-IN-2 Chemical Structure

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PARP1/BRD4-IN-2 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-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC)[1].

IC50 & Target[1]

BRD4

238 nM (IC50)

PARP1

197 nM (IC50)

体外研究
(In Vitro)

PARP1/BRD4-IN-2 (compound BP44) can directly bind to BRD4 and PARP1 in MDA-MB-468 cells and improve their thermal stability[1].
PARP1/BRD4-IN-2 has antiproliferative activity against MDA-MB-231 and MDA-MB-468 with IC50s of 6.61±0.58 μM and 3.01±0.83 μM, respectively[1].
PARP1/BRD4-IN-2 (5, 10, and 20 μM) down-regulates Bcl-2 and up-regulates Bax and cleaved caspase3 at 20 μM; inhibits colony formation and promotes cell apoptosis in MDA-MB-468 cells[1].
PARP1/BRD4-IN-2 (5, 10, and 20 μM) down-regulates DNA damage-related proteins CtIP, Mre11, Rad51, and p-RPA32 dose-dependently; causes DNA damage repair defects by down-regulating Rad51 and p-RPA32[1].

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

PARP1/BRD4-IN-2 相关抗体:
体内研究
(In Vivo)

PARP1/BRD4-IN-2 (40 and 80 mg/kg; IG, for 16 days) significantly inhibits tumor growth in xenograft mice and without significant toxicities, and significantly down-regulates the expression of CtIP, c-Myc, PAR, and Rad51 in tumor tissues[1].
Pharmacokinetic Parameters of PARP1/BRD4-IN-2 in Sprague-Dawley rats[1].

IV (1 mg/kg) PO (10 mg/kg)
T1/2 (h) 3.02 ± 0.57 3.33 ± 0.71
Cmax (ng/mL) 258 ± 11 242 ± 6
AUC0-t (ng/mL·h) 629 ± 49 1489 ± 130
AUC0-∞ (ng/mL·h) 642 ± 36 1530 ± 146
VZ (L/kg) 21.1 ± 2.6
CL (mL/min/kg) 33.7 ± 1.5
F (%) 23.8 ± 1.3

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

Animal Model: Female BALB/c nude mice (implanted subcutaneously with MDA-MB-468 tumor cells)[1]
Dosage: 40 and 80 mg/kg
Administration: IG, for 16 days
Result: Significantly inhibited tumor growth and exhibits no significant toxicities; and significantly down-regulated the expression of CtIP, c-Myc, PAR, and Rad51 in tumor tissues.
分子量

440.45

Formula

C25H20N4O4
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-2 相关分类

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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:

PARP1/BRD4-IN-2Epigenetic Reader DomainPARPApoptosispoly ADP ribose polymerase anti-tumorantiproliferativeDNA damageMDA-MB-468triple-negative breast cancerTNBCMDA-MB-231BALB/c nude miceInhibitorinhibitorinhibit

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