2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. VMY-1-101

VMY-1-101 是一种具有荧光的细胞周期蛋白依赖性激酶 (CDK) 抑制剂，其激发波长为 410 nm，发射波长为 512 nm。VMY-1-101 可竞争性抑制 ATP 与 CDKs 的结合。VMY-1-101 可诱导人乳腺癌细胞发生 G2/M 期细胞周期阻滞。VMY-1-101 可诱导人乳腺癌细胞发生轻度凋亡 (apoptosis)。VMY-1-101 可抑制人乳腺癌细胞 (包括多药耐药阳性细胞) 的增殖，且并非 p-glycoprotein 的底物。VMY-1-101 定位于人乳腺癌细胞的细胞质中。与单独使用荧光团相比，VMY-1-101 与人乳腺癌组织的结合能力更强。VMY-1-101 可用于乳腺癌的研究。

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VMY-1-101

VMY-1-101 Chemical Structure

CAS No. : 1209002-42-5

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VMY-1-101 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer[1].

体外研究
(In Vitro)

VMY-1-101 (0.1 μM；40 分钟) 在受试的纯化人源 CDK/细胞周期蛋白复合物中对 CDK2/cyclin E 复合物的抑制作用最强 (抑制率达 87%)，对其他 CDK 亚型则表现出不同程度的抑制作用[1]。
VMY-1-101 (1-100 μM；48 小时) 可在 48 小时 WST-1 实验中强效抑制人 MDA-MB-231 乳腺癌细胞 (IC50 = 4.86 μM) 和 MCF-7 乳腺癌细胞 (IC50 = 19.05 μM) 的增殖[1]。
VMY-1-101 (5-10 μM；16-40 小时) 可诱导人 MDA-MB-231 和 MCF-7 乳腺癌细胞发生 G2/M 期细胞周期阻滞及中度细胞死亡[1]。
VMY-1-101 (10 μM；48 小时) 可降低人 MDA-MB-231 和 MCF-7 乳腺癌细胞的细胞密度，并诱导其发生异常形态改变[1]。
VMY-1-101 (10-40 μM；48-72 小时) 可通过改变 Bcl-2/Bax 蛋白水平并促进 PARP 切割，在人 MDA-MB-231 乳腺癌细胞中诱导凋亡信号通路[1]。
VMY-1-101 (10 μM；24 小时) 可在人 MCF-7 乳腺癌细胞中诱导显著的早期和晚期凋亡[1]。

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

VMY-1-101 相关抗体:

Cell Cycle Analysis[1]

Cell Line: human MDA-MB-231 breast cancer cells, human MCF-7 breast cancer cells
Concentration: 5 μM; 10 μM
Incubation Time: 16 h, 24 h, 40 h
Result: Induced a clear accumulation of cells in the G2/M phase in both MDA-MB-231 and MCF-7 cells at both 5 μM and 10 μM after 24 h.
Induced similar G2/M phase accumulation patterns at 16 h and 40 h.
Detected a moderate increase in sub-G1 cells (indicating cell death).

Western Blot Analysis[1]

Cell Line: human MDA-MB-231 breast cancer cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Reduced the level of anti-apoptotic Bcl-2 protein after 48 h of treatment.
Increased the level of pro-apoptotic Bax protein after 48 h of treatment, shifting the balance toward apoptosis.

Western Blot Analysis[1]

Cell Line: human MDA-MB-231 breast cancer cells
Concentration: 10 μM; 20 μM; 40 μM
Incubation Time: 72 h
Result: Promoted moderate cleavage of the 116 kDa full-length PARP protein into an 89 kDa fragment, a marker of apoptotic signaling, after 72 h of treatment.

Apoptosis Analysis[1]

Cell Line: human MCF-7 breast cancer cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Provoked a significant induction of early and late apoptotic cells, as indicated by increased annexin V-positive staining, relative to control cells.
分子量

694.25

Formula

C33H40ClN9O4S
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

VMY-1-101 相关分类

  • 摩尔计算器

  • 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:

VMY-1-1011209002-42-5CDKApoptosisCyclin dependent kinaseG2/M cell cycle arrestATPMCF-7 breast cancer cellsmultidrug resistance-positive cellsp-glycoproteincyclin-dependent kinaseMDA-MB-231 breast cancer cellshuman breast cancer cellsCDK2/cyclin E complexCDKsInhibitorinhibitorinhibit

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产品名称：
VMY-1-101
目录号：
HY-182383
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