2. Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Apoptosis DNA/RNA Synthesis PARP
  4. Polθ/PARP-IN-1

Polθ/PARP-IN-1 (compound 25d) 是一种有效的双 DNA 聚合酶 θ (DNA polymerase theta (Polθ)) 和 PARP 抑制剂，IC50 值分别为 45.6、5.4 nM。Polθ/PARP-IN-1 显示出抗增殖活性。Polθ/PARP-IN-1 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G2/M 期，导致 DNA 损伤。Polθ/PARP-IN-1 显示出抗肿瘤活性。

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Polθ/PARP-IN-1 Chemical Structure

Polθ/PARP-IN-1 Chemical Structure

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Polθ/PARP-IN-1 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

Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity[1].

体外研究
(In Vitro)

Polθ/PARP-IN-1 (compound 25d) (0-80 µM; 3 days) 对 HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A 显示出抗增殖活性，IC50 值分别为 20.9、2.7、8.9、2.9、18.9、>80 µM[1]。
Polθ/PARP-IN-1 (compound 25d) (2 µM; 3 days) 诱导细胞凋亡和细胞周期停滞在 G2/M 期，导致 DNA 损伤[1]。

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

Polθ/PARP-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells
Concentration: 0-80 µM
Incubation Time: 5 days
Result: Showed antiproliferative activity with IC50s of 20.9, 2.7, 8.9, 2.9, 18.9, >80 µM for HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells, respectively.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 2 µM
Incubation Time: 3 days
Result: Induced apoptosis with a higher apoptosis rate (26.7%) and arrested cell cycle progression at the G2/M phase.
体内研究
(In Vivo)

Polθ/PARP-IN-1 (20, 40 mg/kg; i.p.; daily for 21 consecutive days) 可抑制 MDA-MB-436 异种移植模型中的肿瘤生长[1]。

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

Animal Model: 18-20 g, Six-week-old female BALB/C nude mice (MDA-MB-436 xenograft model)[1]
Dosage: 20, 40 mg/kg
Administration: I.p.; daily for 21 consecutive days
Result: Significantly inhibited the growth of MDA-MB-436 xenografts in a dose-dependent manner, exerted an optimal inhibitory potency with a tumor growth inhibition (TGI) rate of 54.4%, 74.7% at 20, 40 mg/kg, respectively.
分子量

754.23

Formula

C38H33ClFN7O5S
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

Polθ/PARP-IN-1 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 *
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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)
× = ×
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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:

Polθ/PARP-IN-1ApoptosisDNA/RNA SynthesisPARPpoly ADP ribose polymeraseMDA-MB-436 cellsanti-cancerG2/M phaseapoptosisantiproliferativeInhibitorinhibitorinhibit

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