2. Cell Cycle/DNA Damage Epigenetics Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. PARP Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis STING
  4. PARP1-IN-44

PARP1-IN-44，一种 Olaparib (HY-10162) 的衍生物，是一种具有口服活性的 PARP1 抑制剂 (IC50 = 0.6 nM)，同时也抑制 PARP2 (IC50 = 1.0 nM) 和 PARP7 (IC50 = 7.5 nM)。PARP1-IN-44 对 BRCA 缺陷型癌细胞具有选择性抗增殖活性，且对正常细胞的毒性极小。PARP1-IN-44 可诱导 G2/M 期阻滞，促进细胞凋亡 (apoptosis)，升高活性氧 (ROS) 水平，并破坏线粒体膜电位。PARP1-IN-44 抑制 PARylation，同时增加 γH2AX 的积累。PARP1-IN-44 激活 cGAS-STING 通路，上调 IFN-β 和 CXCL10 的表达。PARP1-IN-44 增强 CT26 肿瘤小鼠模型中的 CD8+ T 细胞浸润，显示出强大的体内抗肿瘤活性。

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PARP1-IN-44

PARP1-IN-44 Chemical Structure

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PARP1-IN-44 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-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy[1].

IC50 & Target[1]

PARP1

0.6 nM (IC50)

PARP2

1 nM (IC50)

PARP7

7.5 nM (IC50)

PARP3

12.5 nM (IC50)

PARP5A

20.5 nM (IC50)

PARP5B

38.1 nM (IC50)

体外研究
(In Vitro)

PARP1-IN-44 (Compound B3) (3.63-100 μM，5 天) 对多种肿瘤细胞具有抗增殖活性，IC50 分别为 9.70 μM (HCT-15) 、5.80 μM (HCC1937) 、18.06 μM (HepG2) 、16.48 μM (MCF7) 和9.88 μM (Capan-1) 、12.48 μM (CT26) 。同时还表现出优异的安全性，对非癌性 NCM460 和 GES-1 细胞系的 IC50 值均大于 100 μM[1]。
PARP1-IN-44 (2.5-10 μM，48 小时) 可诱导 HCC1937 细胞凋亡并导致细胞周期停滞[1]。
PARP1-IN-44 (2.5-10 μM, 24 小时) 可抑制 PARP1 介导的 H2O2 诱导的 HCC1937 细胞 DNA 损伤修复[1]。
PARP1-IN-44 (2.5-10 μM, 24 小时) 可诱导 HCC1937 细胞中 ROS 积累 (用 DCFH-DA 探针 (HY-D0940) 检测) 和线粒体去极化 (用 JC-1 (HY-15534) 染色评估)[1]。
PARP1-IN-44 (0.25-2 μM, 72 小时) 可恢复 CT26 细胞的先天免疫应答[1]。

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

PARP1-IN-44 相关抗体:

Apoptosis Analysis[1]

Cell Line: HCC1937 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 h
Result: Induced apoptosis in a concentration dependent manner, with apoptosis rates of 37.14 % and 62.64 % at concentrations of 5 μM and 10 μM.

Immunofluorescence[1]

Cell Line: H2O22 (600 μM, 30 min)-induced HCC1937 cells
Concentration: 1 μM
Incubation Time: 72 h
Result: Decreased fluorescence intensity of PAR (green) compared to the H2O2-induced group.
Increased γH2AX (green) fluorescence intensity in a concentration dependent manner.

RT-PCR[1]

Cell Line: CT26 cells
Concentration: 0.25, 0.5, 1 and 2 μM
Incubation Time: 72 h
Result: Increased in the expression of immune-related genes (IFN-β and CXCL10).
体内研究
(In Vivo)

PARP1-IN-44 (30 和 50 mg/kg，口服，每日一次，14 天) 对患有 CT26 肿瘤的 BALB/c 小鼠表现出抗肿瘤功效[1]。

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

Animal Model: Six-week-old female BALB/c mice subcutaneously inoculated with CT26 cells in the axillary region[1].
Dosage: 30 mg/kg and 50 mg/kg
Administration: Oral gavage, once daily for 14 days
Result: Significantly reduced both tumor volume and weight, with the 30 mg/kg dose group exhibiting comparable tumor inhibition efficacy to RBN-2397 (HY-136174) (30 mg/kg, p.o.).
Demonstrated remarkable antitumor effects with approximately 5-fold reduction in average tumor volume and approximately 943 mg decrease in tumor weight at 50 mg/kg dose group compared to the control group.
Had no significant differences in body weight changes.
Displayed pronounced morphological changes (H&E staining): chromatin condensation, nuclear fragmentation, nuclear envelope rupture, increased and enlarged cytoplasmic vacuolation, loose cellular arrangement, and reduced intercellular connections.
Promoted the infiltration of CD8+ T cells in the tumor microenvironment.
分子量

536.55

Formula

C27H22F2N4O4S
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-IN-44 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-IN-44PARPApoptosisReactive Oxygen Species (ROS)DNA/RNA SynthesisSTINGpoly ADP ribose polymerase Stimulator of Interferon GenesTMEM173MITAERISMPYSBCPPARP1PARP7antitumorCT26HCC1937DNA damagemitochondrial membrane potentialInhibitorinhibitorinhibit

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