2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. PARP-1-IN-1

PARP-1-IN-1 是一种高选择性且具有口服活性的 PARP-1 抑制剂 (IC50=0.96 nM)。PARP-1-IN-1 在 MDA-MB-436 异种移植模型中具有良好的耐受性和显著的单剂量活性。

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PARP-1-IN-1 Chemical Structure

PARP-1-IN-1 Chemical Structure

CAS No. : 2763840-83-9

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PARP-1-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

PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
106.3 μM
Compound: Y49
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 34656898]
MCF7 IC50
123.5 μM
Compound: Y49
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 34656898]
MX1 IC50
9.46 μM
Compound: Y49
Antiproliferative activity against human BRCA mutant MX1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human BRCA mutant MX1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 34656898]
体外研究
(In Vitro)

PARP-1-IN-1 (compound Y49) (48 hours) has effective inhibition on different cancer cells (IC50s of 9.64, 123.5 106.3 μM for MX-1, MCF7 and A548 cells, respectively)[1].
PARP-1-IN-1 (2.5-10 μM, 48 hours) successfully inhibits the activity of PARP-1 and reduces the production of PAR in A549 cells, which is dose-dependent to some extent[1].

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

PARP-1-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 2.5 μM, 5 μM and 10 μM
Incubation Time: 48h
Result: Inhibited the activity of PARP-1 successfully and reduced the production of PAR in cancer cells. PARP-1-IN-1 was dose-dependent to some extent.
体内研究
(In Vivo)

PARP-1-IN-1 (compound Y49) (50 mg/kg/day; p.o.; daily for 18 days) inhibits the growth of MDA-MB-436 tumor in BALB/c nude mice[1].

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

Animal Model: Female athymic BALB/c nude mice (inoculated MDA-MB-436 cells)[1]
Dosage: 50 mg/kg
Administration: p.o., daily for 18 days
Result: Inhibited the growth of MDA-MB-436 tumor significantly, and no significant change in the body weight of PARP-1-IN-1 treated mice.
分子量

392.47

Formula

C23H25FN4O
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

PARP-1-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 *
= × ×

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:

PARP-1-IN-12763840-83-9PARPpoly ADP ribose polymerasePARP-1 inhibitorCancerRucaparib analoguesSelectivityInhibitorinhibitorinhibit

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