2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis Autophagy
  3. Polo-like Kinase (PLK) Akt Apoptosis Necroptosis Autophagy
  4. MCC1019

MCC1019 是一种选择性的 PLK1 PBD 抑制剂，IC50 为 16.4 μmol/L。MCC1019 可使癌细胞中的 AKT 信号通路失活，诱导凋亡 (Apoptosis)、坏死性凋亡 (Necroptosis)、自噬 (Autophagy)。MCC1019 对肺癌、前列腺癌具有抗癌活性。

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MCC1019

MCC1019 Chemical Structure

CAS No. : 29115-34-2

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MCC1019 相关抗体

Top Publications Citing Use of Products

查看 Polo-like Kinase (PLK) 亚型特异性产品:

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PLK1 PLK2 PLK3 PLK4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MCC1019 is a selective PLK1 PBD inhibitor with an IC50 of 16.4 μmol/L. MCC1019 inactivates the AKT signaling pathway in cancer cells, and induces Apoptosis, Necroptosis and Autophagy. MCC1019 exhibits anticancer activity against lung cancer and prostate cancer[1][2].

IC50 & Target[1]

PLK1 PBD

16.4 μM (IC50)

体外研究
(In Vitro)

MCC1019 可强效且选择性地抑制 PLK1 PBD，在无细胞生化分析中的 IC50 为 16.4 μM[1]。
MCC1019 可灭活 AKT 信号通路、抑制细胞复制并诱导肺腺癌 A549 细胞发生有丝分裂灾难[1]。
MCC1019 可结合 PLK1 (Kd = 12.77 μmol/L) 与 PLK1 PBD (Kd = 18.9 μmol/L)[2]。
MCC1019 (10-40 μmol/L; 24 h) 可在肺腺癌细胞 A549 中诱导浓度依赖性 G2/M 期细胞周期阻滞[2]。
MCC1019 (40 μmol/L; 48 h) 可诱导肺腺癌细胞 A549 发生自噬[2]。

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

MCC1019 相关抗体:

Cell Cytotoxicity Assay[2]

Cell Line: Human cancer cell lines (A549, K562, MCF-7, HCT116 p53+/+, HepG2, U87MG, CCRF-CEM, CEM/ADR5000)
Concentration: 0.001-100 μmol/L
Incubation Time: 72 h
Result: Exhibited cytotoxicity across all tested cell lines, with IC50 values of 23.7 ± 3.7 μmol/L (A549), 2.2 ± 0.09 μmol/L (K562), 25.4 ± 4.08 μmol/L (MCF-7), 18.7 ± 2.8 μmol/L (HCT116 p53+/+), 21.3 ± 3.6 μmol/L (HepG2), 22.7 ± 6.06 μmol/L (U87MG), 1.6 ± 0.24 μmol/L (CCRF-CEM), and 1.3 ± 0.4 μmol/L (CEM/ADR5000).
体内研究
(In Vivo)

MCC1019 (腹腔注射，每日，连续 16 天，剂量 20-40 mg/kg) 可诱导肺癌肿瘤生长抑制，同时在同源小鼠肺癌模型中降低肺部转移负荷且表现出极低的全身毒性[2]。
MCC1019 (腹腔注射；每日；连续 14 天，剂量 40 mg/kg) 可在同源小鼠前列腺癌模型中诱导 61.5% 的前列腺肿瘤生长抑制，且未引起显著的体重变化[2]。
MCC1019 (口服；每日一次；连续 7 天，剂量 100-200 mg/kg) 可使健康 C57BL/6 小鼠的存活率达到 100%，且未出现显著的体重下降[2]。

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

Animal Model: C57BL/6 mice (male and female, 8 weeks old, body weight 25 ± 5 g, syngeneic model via subcutaneous injection of LLC-1 lung cancer cells)[2]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; daily; 16 days
Result: Induced 51.1% tumor growth inhibition and reduced average lung metastatic burden area to 0.1% (from 4.1% in vehicle controls).
Induced 68.1% tumor growth inhibition and reduced average lung metastatic burden area to 2.1%.
Did not cause significant changes in body weight or weights of heart, liver, lung, or kidney (only a minor change in spleen weight was observed).
Downregulated BUBR1 expression in LLC-1 tumors.
分子量

283.12

Formula

C12H11BrO3
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

MCC1019 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)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

MCC101929115-34-2MCC 1019MCC-1019Polo-like Kinase (PLK)AktApoptosisNecroptosisAutophagyPKBProtein kinase BAKT signaling pathwayPLK2 PBDmitotic catastropheapoptosisnecroptosiscancer cellsPLK1 PBDmitotic arrestmurine modelsPLK3 PBDInhibitorinhibitorinhibit

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