2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. PROTACs PARP
  4. PROTAC PARP1 degrader-4

PROTAC PARP1 degrader-4 (Compound 11e) 是一种强效的、选择性的 PARP1 PROTAC 降解剂 (DC50: 2.16 μM)。PROTAC PARP1 degrader-4 可促进 PARP1 的泛素化和降解。PROTAC PARP1 degrader-4 对三阴性乳腺癌、结肠癌具有抗癌活性。

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PROTAC PARP1 degrader-4

PROTAC PARP1 degrader-4 Chemical Structure

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PROTAC PARP1 degrader-4 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

PROTAC PARP1 degrader-4 (Compound 11e) is a potent and selective PARP1 PROTAC degrader (DC50: 2.16 μM). PROTAC PARP1 degrader-4 promotes the ubiquitination and degradation of PARP1. PROTAC PARP1 degrader-4 exhibits anticancer activity against triple-negative breast cancer and colon cancer[1].

IC50 & Target[1]

PARP1

2.16 μM (DC50)

体外研究
(In Vitro)

PROTAC PARP1 degrader-4 (48 h) 可强效抑制三阴性乳腺癌细胞 MDA-MB-231 的增殖，其 IC50 为 4.18 μM[1]。
PROTAC PARP1 degrader-4 (Compound 11e) (48 h) 可抑制 SW620 结肠癌细胞的增殖，其 IC50 为 11.15 μM[1]。
PROTAC PARP1 degrader-4 (Compound 11e) (48 h) 可抑制 MDA-MB-468 乳腺癌细胞的增殖，其 IC50 为 6.96 μM[1]。
PROTAC PARP1 degrader-4 (Compound 11e) (1.25-20 μM; 24 h) 可在 MDA-MB-231 细胞中诱导 PARP1 发生浓度和时间依赖性降解；其 DC50 为 2.16 μM[1]。

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

PROTAC PARP1 degrader-4 相关抗体:

Western Blot Analysis[1]

Cell Line: Human triple-negative breast cancer MDA-MB-231 cells
Concentration: 1.25, 2.5, 5, 10, 20 μM (concentration-dependent assay); 4 μM (time-dependent assay)
Incubation Time: 24 h (concentration-dependent assay); 3, 6, 12, 24, 48 h (time-dependent assay)
Result: Induced concentration-dependent PARP1 degradation with a DC50 of 2.16 μM.
Detected PARP1 degradation after 6 h of treatment with 4 μM, with over 80% degradation observed at 24 h, and the degradative effect persisted for at least 48 h.
分子量

627.75

Formula

C36H42FN5O4
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

PROTAC PARP1 degrader-4 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:

PROTAC PARP1 degrader-4PROTACsPARPpoly ADP ribose polymerasetriple-negative breast cancer cellsARG878PARP2ubiquitin-proteasome systemMDA-MB-468SW620PARP1BRCA1/2-proficient carcinoma-derived cell linesMDA-MB-231colon cancerInhibitorinhibitorinhibit

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