2. PROTAC Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. PROTACs PARP Apoptosis
  4. PROTAC PARP2 degrader-1

PROTAC PARP2 degrader-1 是一种口服有效的 PARP2 PROTAC 降解剂，其 DC50 为 2 μM。PROTAC PARP2 degrader-1 可强效抑制 PARP1 (IC50 = 2.74 nM) 和 PARP2 (IC50 = 0.32 nM) 的酶活性，对 PARP2 的选择性约高 10 倍。PROTAC PARP2 degrader-1 可诱导细胞周期阻滞和细胞凋亡 (apoptosis)，且在小鼠模型中展现出显著抗肿瘤效果。PROTAC PARP2 degrader-1 可用于三阴性乳腺癌的研究。
(粉色: PARP-2 配体 (HY-75706)；蓝色: Cereblon 配体 (HY-131385)；黑色: 连接子 (HY-W089232))。

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PROTAC PARP2 degrader-1

PROTAC PARP2 degrader-1 Chemical Structure

CAS No. : 2925182-32-5

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PROTAC PARP2 degrader-1 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 PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer[1]. (Pink: PARP-2 ligand (HY-75706); Blue: Cereblon ligand (HY-131385); Black: linker (HY-W089232)).

IC50 & Target[1]

PARP-2

2 μM (DC50)

Cereblon

 

体外研究
(In Vitro)

PROTAC PARP2 degrader-1 (Compound C8) (5-10 天) 可强效抑制 MDA-MB-436、Capan-1、MDA-MB-468 和 MDA-MB-231 细胞的增殖，其 IC50 值分别为 0.026 μM、0.061 μM、0.69 μM 和 0.53 μM，且在非 BRCA 突变型 TNBC 细胞中的活性显著高于 Olaparib[1]。
PROTAC PARP2 degrader-1 (C8) (0.5 μM; 24 h) 可在 MDA-MB-231 细胞中选择性降解核内 PARP2，而对胞质 PARP2 水平无影响[1]。
PROTAC PARP2 degrader-1 (0.312-5 μM; 14 days) 可强效且呈剂量依赖性地抑制 MDA-MB-231 细胞的集落形成[1]。
PROTAC PARP2 degrader-1 (0.156-2.5 μM; 24-48 h) 可在 MDA-MB-436 和 MDA-MB-231 细胞中诱导剂量依赖性的 G2/M 期细胞周期阻滞[1]。
PROTAC PARP2 degrader-1 (C8) (0.312-5 μM; 48-72 h) 可在 MDA-MB-436 和 MDA-MB-231 细胞中诱导剂量依赖性凋亡，且与 Olaparib[1]。

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

PROTAC PARP2 degrader-1 相关抗体:

Immunofluorescence[1]

Cell Line: MDA-MB-231 (wild-type) TNBC cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Resulted in nearly complete degradation of nuclear PARP2, while cytoplasmic PARP2 fluorescence remained unchanged.
Showed no effect on PARP2 levels in either compartment when compared to inactive analog C8-M.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 (wild-type) TNBC cells
Concentration: 0.312, 0.625, 1.25, 2.5 and 5 μM
Incubation Time: 14 days
Result: Reduced colony formation in a dose-dependent manner, with significant inhibition observed at concentrations as low as 0.312 μM.
Nearly completely abolished colony formation at 1.25 μM and higher concentrations.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-436 (BRCA1-/-) breast cancer cells, MDA-MB-231 (wild-type) TNBC cells
Concentration: 0.156, 0.312, 0.625, 1.25, 2.52.5 μM
Incubation Time: 24 h (MDA-MB-231); 48 h (MDA-MB-436)
Result: Induced a dose-dependent G2/M cell cycle arrest in both cell lines, with a significantly greater arrest compared to Olaparib at equivalent concentrations.
Increased G2/M phase distribution in MDA-MB-231 cells from ~26% in controls to ~37% at 1.25 μM C8.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436 (BRCA1-/-) breast cancer cells, MDA-MB-231 (wild-type) TNBC cells
Concentration: 0.312, 0.625, 1.25, 2.5 and 5 μM
Incubation Time: 48 h (MDA-MB-231); 72 h (MDA-MB-436)
Result: Induced dose-dependent apoptosis in both cell lines, with a more pronounced effect in MDA-MB-231 cells.
Reached ~90% apoptosis in MDA-MB-231 cells at 5 μM C8, compared to ~48% with Olaparib.
体内研究
(In Vivo)

PROTAC PARP2 degrader-1 (Compound C8) (12.5-100 mg/kg；灌胃、腹腔注射；21 天) 可剂量依赖性地抑制 MDA-MB-231 三阴性乳腺癌异种移植物的生长[1]。

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

Animal Model: BALB/c nude (female, 5-6 weeks old, subcutaneous xenograft model)[1]
Dosage: 100 mg/kg (ig); 12.5 mg/kg (ip); 25 mg/kg (ip)
Administration: ig; ip; daily; 21 days
Result: Achieved tumor growth inhibition (TGI) of 63.5% at 100 mg/kg ig.
Achieved tumor growth inhibition (TGI) of 82.9% at 12.5 mg/kg ip.
Achieved tumor growth inhibition (TGI) of 98.3% at 25 mg/kg ip.
Caused no obvious weight loss, morbidity, or mortality during 21-day treatment.
Showed no obvious histopathological lesions in heart, liver, spleen, kidney, and lung at 25 mg/kg ip.
分子量

801.35

Formula

C43H50ClFN6O6
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

PROTAC PARP2 degrader-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:

PROTAC PARP2 degrader-12925182-32-5PROTACsPARPApoptosispoly ADP ribose polymerase MDA-MB-231PARP2triple-negative breast cancerPARP1MDA-MB-436Capan-1G2/M cell cycle arrestMDA-MB-468DCAF16proteasomeInhibitorinhibitorinhibit

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