2. Cell Cycle/DNA Damage Apoptosis
  3. DNA Alkylator/Crosslinker Bcl-2 Family Caspase Apoptosis Topoisomerase
  4. MN33-63

MN33-63 是一种 Bcl-2 抑制剂、caspase-3 激活剂和 DNA 交联剂，具有广谱抗癌活性。MN33-63 可提高 SN-38 (HY-13704) 的水溶性，并呈剂量依赖性抑制肿瘤生长和增殖，无明显毒性。MN33-63 可解除线粒体凋亡通路的抑制状态，启动凋亡 (apoptosis) 程序，抑制 Topo I 活性，并通过泛素-蛋白酶体和自噬-溶酶体通路促进其降解。MN33-63 可诱导 DNA 交联、G2/M 期细胞周期阻滞、癌细胞迁移抑制，并通过线粒体通路诱导癌细胞凋亡。MN33-63 可用于结直肠癌、宫颈癌、肝细胞癌、肺腺癌、胃癌的研究。

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MN33-63

MN33-63 Chemical Structure

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MN33-63 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

查看 Caspase 亚型特异性产品:

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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

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II DNA gyrase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MN33-63 is a Bcl-2 inhibitor, caspase-3 activator and DNA crosslinker with broad-spectrum anticancer activity. MN33-63 improves the water solubility of SN-38 (HY-13704), inhibits tumor growth and proliferation in a dose-dependent manner, and causes no obvious toxicity. MN33-63 relieves the inhibition of the mitochondrial apoptotic pathway, initiates the apoptosis program, inhibits Topo I activity, and promotes its degradation via the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-63 induces DNA crosslinking, G2/M cell cycle arrest, inhibition of cancer cell migration, and cancer cell apoptosis through the mitochondrial pathway. MN33-63 can be used in the research of colorectal cancer, cervical cancer, hepatocellular carcinoma, lung adenocarcinoma and gastric cancer[1].

IC50 & Target

Caspase 3

 

Bcl-2

 

Topoisomerase I

 

体外研究
(In Vitro)

MN33-63 可强效抑制 HCT-15、HeLa、HepG2、A549、HGC-27 和 CT26 癌细胞的增殖，72 h 时的 IC50 为 0.05 nM-306.10 nM，其中对 HGC-27 细胞的活性最强[1]。
MN33-63 (100 nM; 24-48 h) 可强效抑制 CT26 细胞迁移，使 24 h 时的迁移率为 2.51%，48 h 时的迁移率为 4.42%[1]。
MN33-63 (100 nM; 48 h) 可在 CT26 细胞中诱导强烈的 G2/M 期阻滞，孵育 48 h 后有 59.8% 的细胞处于 G2/M 期[1]。
MN33-63 (100 nM; 48 h) 可诱导 61.10%的 CT26 细胞发生凋亡，孵育 48 h 后，其促凋亡活性强于 chlormethine hydrochloride (HY-B1253) (CH)、SN-38 (HY-13704) 或二者的物理混合物[1]。
MN33-63 (1-10000 nM, 1 μM; 72 h) 可在 72 h 内以剂量依赖方式降低 CT26 细胞中的 Topo I 蛋白水平，在 1 μM 浓度下的抑制作用显著，且效果优于 SN-38、CH 及其物理混合物[1]。
MN33-63 (1 μM; 72 h) 可下调 Bcl-2 表达并降低 CT26 细胞中总 caspase-3 蛋白水平，从而激活内源性凋亡通路[1]。
MN33-63 (1 μM+ 2 μM MG132 (HY-13259); 1 μM+ 50 μM chloroquine; 72 h) 可通过泛素-蛋白酶体和自噬-溶酶体两条通路促进 CT26 细胞中 Topo I 的降解；经 72 h 孵育后，MG132 和 chloroquine 可逆转 Topo I 的减少[1]。

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

MN33-63 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT-15, HeLa, HepG2, A549, HGC-27, CT26
Concentration: 0.038-100000 nM
Incubation Time: 72 h
Result: Exhibited broad-spectrum antiproliferative activity across all six cell lines, with IC50 values of 49.07 nM (HCT-15), 22.94 nM (HeLa), 9.47 nM (HepG2), 306.10 nM (A549), 0.05 nM (HGC-27), and 9.78 nM (CT26).
Showed superior potency to SN-38, CH, and their physical mixture in most cell lines, particularly exceptional activity against HGC-27 cells.

Western Blot Analysis[1]

Cell Line: CT26
Concentration: 1-10000 nM, 1 μM
Incubation Time: 72 h
Result: Reduced Topo I protein levels in a dose-dependent manner, with significant inhibition observed at concentrations as low as 1 μM.
At 1 μM, inhibited Topo I expression more effectively than SN-38, CH, or their physical mixture.

Western Blot Analysis[1]

Cell Line: CT26
Concentration: 1 μM
Incubation Time: 72 h
Result: Significantly downregulated Bcl-2 expression and reduced total caspase-3 protein levels (reflecting activation and cleavage of pro-caspase-3) compared to SN-38, CH, or their physical mixture.

Western Blot Analysis[1]

Cell Line: CT26
Concentration: 1 μM MN33-63 + 2 μM MG132; 1 μM MN33-63 + 50 μM CQ
Incubation Time: 72 h
Result: The reduction in Topo I protein levels induced by MN33-63 was significantly reversed by both MG132 and CQ, indicating MN33-63 promotes Topo I degradation via the ubiquitin-proteasome and autophagy-lysosome pathways.
体内研究
(In Vivo)

MN33-63 (1.79-7.16 mg/kg；腹腔注射；每日一次；连续 10 天) 在荷 CT26 肿瘤的 BALB/c 小鼠中表现出剂量依赖性的强效抗肿瘤活性，高剂量组的肿瘤重量抑制率达 77.10%，且安全性良好，未观察到器官毒性或体重下降[1]。

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

Animal Model: BALB/c mice with Colorectal cancer (female, 4-5 weeks old, 19-21 g, subcutaneous xenograft model)[1]
Dosage: 1.79 mg/kg; 3.58 mg/kg; 7.16 mg/kg
Administration: i.p.; daily; 10 days
Result: Achieved a tumor weight inhibition rate of 77.10% at 7.16 mg/kg, significantly higher than CH monotherapy, SN-38 monotherapy, and CH + SN-38 physical mixture.
Drastically reduced tumor volume growth in all dose groups, with the 7.16 mg/kg group showing the smallest final tumor volumes.
Caused no body weight loss in any dose group.
Maintained serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), blood urea nitrogen (BUN), and creatinine (CREA) levels within normal reference ranges in all dose groups.
Induced dose-dependent increases in tumor tissue necrotic areas, nuclear condensation, and cell apoptosis, with the 7.16 mg/kg group exhibiting the most extensive tumor cell damage.
Showed no abnormal pathological changes (inflammation, necrosis, degeneration) in heart, liver, spleen, lung, and kidney tissues in any dose group.
分子量

684.37

Formula

C27H26Cl2N3Na2O9P
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

MN33-63 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)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

MN33-63DNA Alkylator/CrosslinkerBcl-2 FamilyCaspaseApoptosisTopoisomeraseTopo Imitochondrial apoptosis pathwayBcl-2hepatocellular carcinomacervical cancerlung adenocarcinomacaspase-3ubiquitin-proteasome pathwayautophagy-lysosome pathwaycolorectal cancerInhibitorinhibitorinhibit

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