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

PROTAC PARP1 degrader-4 (Compound 180055) 是一种选择性的 PARP1 PROTAC 降解剂 (在 T47D 和 MDA-MB-231 细胞系中的 DC50 分别为 180 nM 和 240 nM)。PROTAC PARP1 degrader-4 可促进 PARP1 的泛素化和降解，并抑制 PARP1 酶的活性，但不会产生明显的 DNA 诱捕效应。PROTAC PARP1 degrader-4 能抑制携带 BRCA 基因突变肿瘤，同时对正常细胞的生长影响较小 (粉红色：PARP1 ligand (HY-10617A); 蓝色：E3 ligase VHL ligand (HY-125845); 黑色：linker (HY-W014787))。

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PROTAC PARP1 degrader-4 Chemical Structure

PROTAC PARP1 degrader-4 Chemical Structure

1.  客户无需承担相应的运输费用。

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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 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PROTAC PARP1 degrader-4 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PROTAC PARP1 degrader-4 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787))[1].

IC50 & Target[1]

PARP1

 

体外研究
(In Vitro)

PROTAC PARP1 degrader-4 (1-10 μM，24-48 h) 可保护 T47D 和 MOLT4 细胞免于基因毒性诱导的细胞死亡[1]。
PROTAC PARP1 degrader-4 (10 μM，3-6 天) 在 BRCA1 突变的 MOLT4 细胞中诱导细胞毒性作用[1]。

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

PROTAC PARP1 degrader-4 相关抗体:

Cell Viability Assay[1]

Cell Line: Cardiomyocyte cell lines lacking BRCA1 mutations and MOLT4 cells
Concentration: 1, 5, 10 μM
Incubation Time: 144 h
Result: Showed minimal cytotoxicity in cardiomyocyte cell lines lacking BRCA1 mutations.
Induced substantial cytotoxic effects in MOLT4 cells with BRCA1 mutation.
体内研究
(In Vivo)

PROTAC PARP1 degrader-4 (40 mg/kg，腹腔注射，16 天) 对 BRCA1 突变的 MOLT4 异种移植小鼠具有抗肿瘤作用[1]。

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

Animal Model: 5-week-old NSG mice (injected 8 × 106 MOLT4 cells or 4 × 106 A2780)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), 16 days
Result: Exhibited a noticeable reduction in tumor size compared to the control group.
Effectively degraded PARP1 in tumors derived from MOLT4-xenografted mice.
Showed no significant alterations in neutrophil count, lymphocyte count or glutamic-pyruvic transaminase levels.
分子量

920.14

Formula

C51H62FN7O6S
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 polymeraseMOLT4Anti-tumorT47DMDA-MB-231XenograftsOvarian and Breast cancer.Inhibitorinhibitorinhibit

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