2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. MDL-27048

MDL-27048 是一种微管蛋白 (tubulin) 抑制剂，可竞争性、可逆地结合微管蛋白异二聚体上的秋水仙碱 (HY-16569) 结合位点。MDL-27048 可抑制微管组装，诱导预组装微管缓慢解聚，破坏微管聚合-解聚动态平衡，并扰乱细胞质微管网络。MDL-27048 对人类癌细胞具有生长抑制作用，可诱导有丝分裂停滞，且在微管解聚浓度下不会破坏肌动蛋白丝。MDL-27048 可用于恶性肿瘤的相关研究。

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MDL-27048

MDL-27048 Chemical Structure

CAS No. : 124711-23-5

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MDL-27048 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

MDL-27048, a tubulin inhibitor, binds competitively, reversibly to the Colchicine (HY-16569)-binding site on tubulin heterodimers. MDL-27048 inhibits microtubule assembly, induces slow depolymerization of preassembled microtubules, disrupts microtubule polymerization-depolymerization dynamics, and disrupts cytoplasmic microtubule networks. MDL-27048 exerts growth inhibitory effects on human cancer cells, induces mitotic arrest, and does not disrupt actin filaments at microtubule-depolymerizing concentrations. MDL-27048 can be used for the research of malignant tumors[1][2].

体外研究
(In Vitro)

MDL-27048 (0.4-20 μM；40 分钟) 可与纯化的猪脑微管蛋白异二聚体的每个亚基可逆结合一个位点，其表观平衡常数为 (2.1-3.5) × 106 M-1，且其结合位点与 podophyllotoxin/colchicine 结合位点重叠[2]。
MDL-27048 (0.5-20 μM；30-96 分钟) 可在体外抑制纯化猪脑微管蛋白组装为微管：在微管蛋白浓度为 1 mg/mL 时，其 IC50 为 1 μM；同时还能诱导预组装微管缓慢解聚，且其抑制作用可被紫杉醇逆转[2]。
MDL-27048 (0.2-10 μM；10-240 分钟) 可诱导 PtK2 细胞胞质微管发生浓度和时间依赖性的可逆解聚，在 2-5 μM 作用 3 小时时达到最大解聚程度，且在去除药物后 15-30 min 内完成完全复聚[2]。
MDL-27048 (0.05-1 μM；3-27 小时) 可诱导 SV40-3T3 细胞发生有丝分裂阻滞，在 0.2 μM 时阻滞作用显著，且在 1 μM 作用 9 小时后有丝分裂指数升高至 12.7%，导致 DNA 含量加倍的细胞积累[2]。

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

MDL-27048 相关抗体:

Immunofluorescence[2]

Cell Line: PtK2 cells
Concentration: 0.2 μM; 0.5 μM; 0.8 μM; 2 μM; 5 μM
Incubation Time: 3 h
Result: Induced concentration-dependent depolymerization of cytoplasmic microtubules: 0.2 μM caused undulating peripheral microtubules; 0.5-1 μM caused partial depolymerization; 2-5 μM caused maximal depolymerization, leaving only a few drug-resistant microtubules per cell, with no effect on actin filaments.

Immunofluorescence[2]

Cell Line: PtK2 cells
Concentration: 10 μM
Incubation Time: 10 min; 20 min; 80 min; 180 min
Result: Caused full depolymerization within 3 h.

Cell Cycle Analysis[2]

Cell Line: SV40-3T3 cells
Concentration: 1 μM
Incubation Time: 3 h; 6 h; 9 h; 27 h
Result: Increased the mitotic index from 1% (control) to 2.7% at 3 h, 10.2% at 6 h, and 12.7% at 9 h at 1 μM.
Caused a marked shift to higher DNA content in 1 μM-treated cells at 6-9 h, indicating accumulation of cells that completed S phase but failed to progress through mitosis.
分子量

325.40

Formula

C20H23NO3
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

MDL-27048 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:

MDL-27048124711-23-5MDL27048MDL 27048Microtubule/TubulinmicrotubulesPtK2 cellcolchicine-binding siteactin filamentsmalignant tumorsporcine tubulinhuman hepatoma cell lineshuman cancer cellsmitotic arresttubulin heterodimersInhibitorinhibitorinhibit

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目录号：
HY-182478
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