2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. PARP Apoptosis Caspase
  4. YCH3971

YCH3971 是一种 PARP1 抑制剂，其 PARP1 IC50 为 7.52 nM，PARP1 EC50 为 67.75 nM。YCH3971 y抑制 BRCA 缺陷型肿瘤细胞增殖。YCH3971 诱导三阴性乳腺癌细胞 DNA 损伤、G2/M 期阻滞、 caspase 介导的细胞凋亡 (Apoptosis)。YCH3971 可用于 BRCA 缺陷型肿瘤的研究。

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YCH3971

YCH3971 Chemical Structure

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YCH3971 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

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YCH3971 is a PARP1 inhibitor with a PARP1 IC50 of 7.52 nM and a PARP1 EC50 of 67.75 nM. YCH3971 inhibits the proliferation of BRCA-deficient tumor cells. YCH3971 induces DNA damage, G2/M phase arrest, and caspase-mediated Apoptosis in triple-negative breast cancer cells. YCH3971 can be used for the research of BRCA-deficient tumors[1].

IC50 & Target

PARP-1

7.52 nM (IC50)

PARP-1

67.75 nM (EC50)

体外研究
(In Vitro)

YCH3971 (0.01-10000 nM, 7 days) 可强效抑制 BRCA1 缺陷型 MDA-MB-436 细胞的增殖，其 IC50 为 2.10 nM[1]。
YCH3971 (0.01-10000 nM, 7 days) 可抑制 BRCA2 缺陷型 V-C8 细胞的增殖，其 IC50 为 69.61 nM；而对 BRCA2 功能正常的 V79 细胞仅表现出极微弱的活性[1]。
YCH3971 (0.01-10000 nM, 7 days) 可抑制 BRCA1 突变型 UWB1.289 卵巢癌细胞的增殖，其 IC50 为 112.86 nM，而对恢复 BRCA1 表达的 UWB1.289 + BRCA1 细胞几乎无活性[1]。
YCH3971 (0.01-1 μM; 48 h) 可在 MDA-MB-436 细胞中诱导剂量依赖性的 DNA 损伤[1]。
YCH3971 (0.01-1 μM; 3 days) 可在 MDA-MB-436 细胞中诱导剂量依赖性 G2/M 期阻滞[1]。
YCH3971 (0.01-1 μM; 4 days) 可在 MDA-MB-436 细胞中诱导剂量依赖性的 caspase 介导的细胞凋亡[1]。

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

YCH3971 相关抗体:

Immunofluorescence[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 48 h
Result: Induced dose-dependent DNA damage.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 3 days
Result: Led to a dose-dependent accumulation of cells in the G2/M phase.
At concentrations ≥0.1 μM, caused a statistically significant increase in G2/M phase cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 4 days
Result: Led to a dose-dependent increase in Annexin V+/PI+ apoptotic cells.
At 1 μM, induced a slightly higher level of apoptosis.
Confirmed dose-dependent cleavage of caspases-3, -7, and -8 via western blotting.
At 1 μM, induced slightly stronger caspase activation.

Western Blot Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 48 h
Result: Activated DNA damage response markers, including phosphorylated CHK1 (p-CHK1), phosphorylated RPA32 (p-RPA32), and γH2AX.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-last T1/2 CL Vss_obs Cmax Tmax Bioavailability
Rat[1] 1 mg/kg i.v. 837 ng·h/mL 12.6 h 19.8 mL/min/kg 1727 L/kg / / /
Rat[1] 3 mg/kg p.o. 30.8 2.59 h / / 16.9 ng/mL 0.83 h 1.22 %
分子量

387.48

Formula

C23H25N5O
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

YCH3971 相关分类

  • 摩尔计算器

  • 稀释计算器

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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)
× = ×
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:

YCH3971YCH 3971YCH-3971PARPApoptosisCaspasepoly ADP ribose polymerase PARP1 inhibitortriple-negative breast cancerV-C8 cellsMDA-MB-436 cellsUWB1.289 ovarian cancer cellsInhibitorinhibitorinhibit

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