2. PROTAC Epigenetics Cell Cycle/DNA Damage Immunology/Inflammation
  3. PROTACs PARP DNA/RNA Synthesis PD-1/PD-L1
  4. PROTAC PARP1 degrader-5

PROTAC PARP1 degrader-5 是一种 PARP1 PROTAC 降解剂，其 DC50 为 0.12 μM。PROTAC PARP1 degrader-5 可通过催化三元复合物的形成劫持泛素-蛋白酶体系统，从而驱动 PARP1 的持续降解。PROTAC PARP1 degrader-5 可诱导 DNA 损伤，促使肿瘤细胞中少量胞质双链 DNA 积累，并上调肿瘤细胞表面的 PD-L1 表达。PROTAC PARP1 degrader-5 包裹于脂质纳米粒中时，在小鼠黑色素瘤模型中表现出肿瘤生长抑制活性。PROTAC PARP1 degrader-5 可用于癌症相关研究，例如黑色素瘤。
(粉色: PARP-1 配体 (HY-10162)；蓝色: VHL 配体 (HY-112078)；黑色: 连接子 (HY-W012241))。

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PROTAC PARP1 degrader-5

PROTAC PARP1 degrader-5 Chemical Structure

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PROTAC PARP1 degrader-5 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 PARP 亚型特异性产品:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

查看 DNA/RNA Synthesis 亚型特异性产品:

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma[1]. (Pink: PARP-1 ligand (HY-10162); Blue: VHL ligand (HY-112078); Black: linker (HY-W012241)).

IC50 & Target[1]

PARP1

0.12 μM (DC50)

VHL

 

体外研究
(In Vitro)

PROTAC PARP1 degrader-5 (0.01-25 μM; 12-24 h) 可在 B16F10 细胞中强效降解 PARP1 蛋白，其 DC50 为 0.12 μM[1]。
PROTAC PARP1 degrader-5 (1 μM; 24 h) 可降低 B16F10 细胞中的 PARP1 荧光强度[1]。
PROTAC PARP1 degrader-5 (1 μM; 24 h) 可诱导轻微的 DNA 损伤，使 B16F10 细胞中的胞质 dsDNA 水平升高 3.7 倍[1]。
PROTAC PARP1 degrader-5 (1 μM; 12 h) 可上调 B16F10、4T1、H22、KPC 和 CT26 细胞中 PD-L1 的表达，使 B16F10 细胞中的 PD-L1 表达水平升高 1.7 倍[1]。
PROTAC PARP1 degrader-5 (1 μM) 可将成熟 BMDCs 的比例提升至 41.9%[1]。
PROTAC PARP1 degrader-5 (1 μM; 24 h) 可在共培养的 DC2.4 和 THP-1 细胞中诱导 cGAMP 的产生[1]。
PROTAC PARP1 degrader-5 (The lipid nanoparticle-encapsulated PROP) (0.01-25 μM; 24 h) 对 H22 和 CT26 细胞表现出细胞毒性，其 IC50 值分别为 18.6 μM 和 13.1 μM，并减少集落形成[1]。

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

PROTAC PARP1 degrader-5 相关抗体:

Western Blot Analysis[1]

Cell Line: B16F10
Concentration: 0.01, 0.1, 1, 10, 25 μM
Incubation Time: 12 h; 24 h
Result: Induced PARP1 protein degradation with a half-maximal degradation concentration of 0.12 μM.
Reduced PARP1 protein levels to 21.8% of PBS-treated controls after 24 h of treatment.

Immunofluorescence[1]

Cell Line: B16F10
Concentration: 1 μM
Incubation Time: 24 h
Result: Resulted in a marked reduction of PARP1-specific fluorescence signals compared to PBS-treated controls.
体内研究
(In Vivo)

PROTAC PARP1 degrader-5 (The lipid nanoparticle-encapsulated PROP) (12 mg/kg；静脉注射；每日 1 次；连续 5 天) 可延缓 B16F10 黑色素瘤的生长，降低肺转移，诱导肿瘤组织中 PD-L1 的上调，并将雌性 C57BL/6J 小鼠的中位生存期延长至 40 天[1]。
PROTAC PARP1 degrader-5 (The lipid nanoparticle-encapsulated PROP) (12 mg/kg；静脉注射；每日一次；连续 5 天) 在雌性 BALB/cJ 小鼠中无法有效抑制 CT26 结肠癌和 4T1 乳腺癌细胞的生长[1]。

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

Animal Model: C57BL/6J (female, 6 to 8 weeks old, subcutaneous injection B16F10 cells)[1]
Dosage: 10 mg/kg (delivered via LNP@PROₚ formulation)
Administration: i.v.; daily; 5 consecutive days
Result: Delayed tumor growth but did not achieve robust suppression compared to combination formulation.
Extended median survival to up to 40 days, with no mice surviving to 60 days.
Induced a 1.3±0.2-fold up-regulation of PD-L1 in tumor tissue versus PBS controls.
Inhibited lung metastasis
分子量

1005.25

Formula

C55H69FN8O7S
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-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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:

PROTAC PARP1 degrader-5PROTACsPARPDNA/RNA SynthesisPD-1/PD-L1poly ADP ribose polymerase PD-1/Programmed death-ligand 1melanomabone marrow-derived dendritic cellsubiquitin-proteasome systemlipid nanoparticlesBRD4cancer cell linesPARP1murine melanoma modelsprogrammed death-ligand 1base excision repairInhibitorinhibitorinhibit

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