2. Cell Cycle/DNA Damage Apoptosis
  3. Topoisomerase Apoptosis
  4. YCJ-02

YCJ-02 是一种选择性的拓扑异构酶 I (Top I) 抑制剂。YCJ-02 能够抑制细胞增殖，并诱导细胞凋亡 (apoptosis) 和 G2/M 期阻滞。YCJ-02 可诱导 DNA 损伤并增加 γ-H2AX 水平。YCJ-02 可通过 ubiquitin/26S 蛋白酶体途径促进 Top I 降解。YCJ-02 可增加促凋亡蛋白 Bad、Bax 和 caspase-3 的表达。YCJ-02 具有广谱抗肿瘤活性。YCJ-02 可用于癌症研究，例如肝内胆管癌 (ICC)。

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YCJ-02

YCJ-02 Chemical Structure

CAS No. : 2260557-09-1

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YCJ-02 相关抗体

Top Publications Citing Use of Products

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC)[1].

IC50 & Target[1]

Topoisomerase I

 

体外研究
(In Vitro)

YCJ-02 在 HepG2、HuCCT1、BXPC-3、SW1990、HCT-116、SW480、A2780、HeLa 和 MCF-7 细胞中显示出抗肿瘤活性，其 IC50 值分别为 0.025、0.079、1.15、0.20、0.16、0.12、0.25、0.79 和 1.08 μM[1]。
YCJ-02 抑制人 HuCCT1、RBE、QBC-939 以及小鼠 A/N、B/R 胆管癌细胞的增殖，其 IC50值分别为 0.079、0.31、0.35、1.51 和 2.68 μM[1]。
YCJ-02 (0.25-1 μM, 72 h) 抑制 QBC-939 和 HuCCT1 细胞的集落形成[1]。
YCJ-02 (0.25-1 μM, 24-48 h) 诱导 QBC-939 和 HuCCT1 细胞发生 G2/M 期阻滞和凋亡[1]。
YCJ-02 (0.05-0.8 μM) 以剂量依赖性方式抑制 Top I 的活性，且对 Top II 的抑制活性极低[1]。
YCJ-02 (0.125-1 μM, 48 h) 可降低 QBC-939 和 HuCCT1 细胞中 Top I 的水平[1]。
YCJ-02 (0.125-1 μM, 48 h) 会诱导 DNA 损伤[1]。
YCJ-02 (0.125-1 μM) 可降低 QBC-939 和 A/N 细胞中 AKT、 p-AKTser473、mTORC1、 p-mTORC1ser2448 以及 Notch1 (NICD) 的水平[1]。

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

YCJ-02 相关抗体:

Apoptosis Analysis[1]

Cell Line: QBC-939 and HuCCT1 cells
Concentration: 0.25, 0.5 and 1μM
Incubation Time: 24 and 48 h
Result: Increased apoptotic rates.
Upregulated levels of p21, p53 and Bcl-2.

Western Blot Analysis[1]

Cell Line: QBC-939 and HuCCT1 cells
Concentration: 0.125, 0.25, 0.5 and 1μM
Incubation Time: 48 h
Result: Reduced Top I levels.

Immunofluorescence[1]

Cell Line: QBC-939 cells
Concentration: 0.125, 0.25, 0.5 and 1μM
Incubation Time: 12 h
Result: Reduced Top I levels.
Increased γ-H2AX levels.
体内研究
(In Vivo)

YCJ-02 (10 mg/kg，腹腔注射，2 周) 在 AKT/NICD 诱导的原发性 ICC 小鼠模型中可抑制肿瘤生长并延长生存期[1]。

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

Animal Model: AKT/NICD-induced primary ICC mice models[1]
Dosage: 10 mg/kg
Administration: Intraperitoneally injection, 2 weeks for 10 times
Result: Reduced tumor volume and prolonged survival.
Had no significant body weight loss.
Decreased tumor area.
Reduced the positive cell rates of CK19 and Ki-67.
Reduced Top I levels and increased the levels of p21, p53, cleaved caspase 3, and γ-H2AX.
Reduced p-AKTser473, mTORC1, p-mTORC1ser2448, and Notch1 (NICD).
分子量

423.41

Formula

C23H19F2N3O3
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

YCJ-02 相关分类

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  • 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:

YCJ-022260557-09-1YCJ02YCJ 02TopoisomeraseApoptosisTop IDNAγ-H2AXICCQBC-939HuCCT1Inhibitorinhibitorinhibit

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目录号：
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