2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis Caspase
  4. Microtubule destabilizing agent-3

Microtubule destabilizing agent-3 是 B32B3 (HY-12240) 的类似物，是一种微管去稳定剂。Microtubule destabilizing agent-3 通过去稳定微管并促进有丝分裂阻滞发挥其抗骨髓瘤表型，最终导致细胞死亡。Microtubule destabilizing agent-3 可诱导 G2/M 期阻滞和 caspase 依赖性细胞凋亡 (apoptosis)。Microtubule destabilizing agent-3 可用于多发性骨髓瘤的研究。

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Microtubule destabilizing agent-3

Microtubule destabilizing agent-3 Chemical Structure

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Microtubule destabilizing agent-3 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Microtubule destabilizing agent-3, a B32B3 (HY-12240) analog, is a microtubule destabilizing agent. Microtubule destabilizing agent-3 exerts its antimyeloma phenotypes by destabilizing microtubules and promoting mitotic arrest, leading to cell death. Microtubule destabilizing agent-3 induces G2/M phase arrest and caspase-dependent apoptosis. Microtubule destabilizing agent-3 can be used for the research of multiple myeloma[1].

体外研究
(In Vitro)

Microtubule destabilizing agent-3 (VPR8) (500 nM；24-48 小时) 在 JJN3 细胞系中表现出显著的细胞死亡 (IC50 值约为 190 nM) 和 G2M 期阻滞，并诱导细胞凋亡[1]。
Microtubule destabilizing agent-3 (500 nM；1-24 小时) 上调 G2/M 期和自噬相关信号，并下调 MYC 信号[1]。
Microtubule destabilizing agent-3 (0.25-20 μM；24 小时) 不会降低多发性骨髓瘤细胞中 H2AT120P、EZH2 或 H3K27me3 的水平。Microtubule destabilizing agent-3 在 CETSA 实验中表现出对 DCAF1 的热稳定性增强作用[1]。

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

Microtubule destabilizing agent-3 相关抗体:

Cell Cycle Analysis[1]

Cell Line: JJN3 cells
Concentration: 500 nM
Incubation Time: 24 h, 48 h
Result: Reduced cell viability in multiple myeloma cell lines, with an IC50 of approximately 190 nM.
Induced G2M cell cycle arrest. G2M phase was significantly prolonged, and cells spent more time in G2M before dying.

Apoptosis Analysis[1]

Cell Line: JJN3 cells
Concentration: 500 nM
Incubation Time: 24 h, 48 h
Result: Triggered cell surface phosphatidylserine exposure and accumulation of cells in a sub-G1 peak, features of apoptotic cell death.
体内研究
(In Vivo)

Microtubule destabilizing agent-3 (VPR8) (15 mg/kg，腹腔注射，连续给药 5 天，休息 2 天) 在多发性骨髓瘤和淋巴瘤异种小鼠移植模型中显著延迟了肿瘤进展并提高了生存率[1]。

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

Animal Model: NOD.Cg-Prkdcscid IL2rgtmIWjl/Szj (NSG) mice bearing JJN3Luc2 myeloma cells[1]
Dosage: 15 mg/kg
Administration: i.p., five daily doses followed by 2 days of rest
Result: Tumor progression was significantly delayed in NSG mice bearing luciferase-tagged JJN3 xenografts and overall survival was significantly prolonged (median 27 days for vehicle vs. 33 days). No overt hematopoietic toxicity was observed, as evidenced by preserved peripheral blood leukocyte and platelet counts and hemoglobin concentration.
Animal Model: Ptprca mice bearing EμMyc lymphoma cells[1]
Dosage: 15 mg/kg
Administration: i.p., five daily doses followed by 2 days of rest
Result: Tumor progression was significantly suppressed in Ptprca mice transplanted with EμMyc lymphoma cells, as indicated by reduced spleen weight, peripheral blood, and nodal tumor burden. Continued treatment (10 days) significantly improved overall survival (median 17 days for vehicle vs. 22 days).
分子量

363.48

Formula

C20H21N5S
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

Microtubule destabilizing agent-3 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:

Microtubule destabilizing agent-3Microtubule destabilizing agent3Microtubule destabilizing agent 3Microtubule/TubulinApoptosisCaspasemicrotubule destabilizing agentcaspase-dependent apoptosisG2/M phase arrestmultiple myelomaInhibitorinhibitorinhibit

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