2. Cell Cycle/DNA Damage NF-κB Apoptosis
  3. G-quadruplex Keap1-Nrf2 Ferroptosis Apoptosis
  4. Anticancer agent 309

Anticancer agent 309 (Compound HZ-1) 是一种抗癌剂、G-quadruplex 结合剂，对 c-Myc G4 和 KRAS G4 的 Kd 值分别为 2.46 μM 和 1.61 μM。Anticancer agent 309 促进细胞核内 G4 的形成。Anticancer agent 309 对平行 G4 的选择性高于非平行 G4。Anticancer agent 309 抑制 NRF2 信号通路，降低 XCT 和 GPX4 的表达。Anticancer agent 309 可诱导细胞发生铁死亡 (Ferroptosis)、凋亡 (Apoptosis) 和免疫原性细胞死亡。Anticancer agent 309 对乳腺癌具有抗肿瘤功效。Anticancer agent 309 可用于乳腺癌的研究。

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Anticancer agent 309

Anticancer agent 309 Chemical Structure

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Anticancer agent 309 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 309 (Compound HZ-1) is an anticancer agent and G-quadruplex binder, with Kd values of 2.46 μM and 1.61 μM for c-Myc G4 and KRAS G4, respectively. Anticancer agent 309 promotes the formation of intranuclear G4. Anticancer agent 309 shows higher selectivity for parallel G4 than for non-parallel G4. Anticancer agent 309 inhibits the NRF2 signaling pathway and reduces the expression of XCT and GPX4. Anticancer agent 309 induces Ferroptosis, Apoptosis and immunogenic cell death in cells. Anticancer agent 309 exerts antitumor efficacy against breast cancer. Anticancer agent 309 is applicable for the research of breast cancer[1].

体外研究
(In Vitro)

Anticancer agent 309 可与纯化的 c-Myc G4 和 KRAS G4 结构强效结合，其 Kd 值分别为 2.46 μM 和 1.61 μM[1]。
Anticancer agent 309 (24 h) 可抑制多种人源和小鼠肿瘤细胞系的增殖 (MDA-MB-231, HCT116, HepG2, A549, MCF-7, 4T1)，其 IC50 值范围为 7.77 ± 0.77 μM 至 16.71 ± 0.71 μM[1]。
Anticancer agent 309 (10 μM; 24 h) 可促进人乳腺癌 MDA-MB-231 细胞核内 G4 的形成[1]。
Anticancer agent 309 (5-20 μM; 24 h) 可在乳腺癌 MDA-MB-231 细胞中触发凋亡[1]。

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

Anticancer agent 309 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human breast cancer MDA-MB-231 cells, human colon cancer HCT116 cells, human liver cancer HepG2 cells, human lung cancer A549 cells, human breast cancer MCF-7 cells, mouse breast cancer 4T1 cells, human normal breast MCF-10a cells
Concentration: Titrated to determine IC50
Incubation Time: 24 h
Result: Exerted dose-dependent cytotoxicity against all tested tumor cell lines, with IC50 values of 7.77 ± 0.77 μM (MDA-MB-231), 8.33 ± 0.46 μM (HCT116), 9.88 ± 1.18 μM (HepG2), 11.67 ± 0.33 μM (A549), 16.71 ± 0.71 μM (MCF-7), and 15.23 ± 0.95 μM (4T1).
Showed an IC50 of 28.12 ± 1.49 μM against normal MCF-10a cells, which was significantly higher than against tumor cells.

Western Blot Analysis[1]

Cell Line: Human breast cancer MDA-MB-231 cells
Concentration: 5-20 μM
Incubation Time: 24 h
Result: Downregulated c-Myc and KRAS protein expression in a dose-dependent manner.
Suppressed the NRF2 signaling pathway, reducing the expression of XCT and GPX4.
Decreased the expression of Caspase 7, Caspase 3, and anti-apoptotic Bcl-2, while increased Cleaved Caspase 3 expression at 20 μM.

Apoptosis Analysis[1]

Cell Line: Human breast cancer MDA-MB-231 cells
Concentration: 5-20 μM
Incubation Time: 24 h
Result: Triggered a dose-dependent increase in both early apoptotic and late apoptotic cell populations.
体内研究
(In Vivo)

Anticancer agent 309 (10 mg/kg；每隔一天；连续 14 天) 对荷 4T1 乳腺癌细胞的 BALB/c 小鼠具有强效抗肿瘤作用，同时提升脾脏和肿瘤中 CD4+ 及 CD8+ T 细胞的数量[1]。

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

Animal Model: BALB/c (female, 4 weeks old, subcutaneously inoculated with 4×105 4T1 mouse breast cancer cells)[1]
Dosage: 10 mg/kg
Administration: every other day; 14 days
Result: Reduced final tumor weight.
Suppressed tumor growth.
Elevated percentage of CD45+CD3+CD4+ helper T cells in spleens and in tumors.
Elevated percentage of CD45+CD3+CD8+ cytotoxic T lymphocytes in spleens and in tumors.
Induced downregulation of GPX4 and upregulation of Cleaved Caspase 3 in tumor tissues.
Did not cause significant mouse weight loss or major organ weight changes relative to controls.
分子量

492.66

Formula

C31H36N6
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

Anticancer agent 309 相关分类

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  • 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:

Anticancer agent 309Anticancer agent309Anticancer agent-309G-quadruplexKeap1-Nrf2FerroptosisApoptosisferroptosisparallel G-quadruplexesimmunogenic cell deathc-Myc G-quadruplexCD4+ helper T lymphocytesNRF2-XCT-GPX4 pathwayapoptosisbreast cancer cellsKRAS G-quadruplexCD8+ cytotoxic T lymphocytesInhibitorinhibitorinhibit

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