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

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.

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MCC1019

MCC1019 Chemical Structure

CAS No. : 29115-34-2

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MCC1019 Related Antibodies

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Description

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)

In Vitro

MCC1019 potently and selectively inhibits PLK1 PBD, with an IC50 of 16.4 μM in cell-free biochemical assays[1].
MCC1019 inactivates the AKT signaling pathway, inhibits cell replication, and induces mitotic catastrophe in lung adenocarcinoma A549 cells[1].
MCC1019 binds to PLK1 (Kd = 12.77 μmol/L) and PLK1 PBD (Kd = 18.9 μmol/L)[2].
MCC1019 (10-40 μmol/L; 24 h) induces concentration-dependent G2/M cell cycle arrest in human lung adenocarcinoma A549 cells[2].
MCC1019 (40 μmol/L; 48 h) induces autophagy in the lung adenocarcinoma cell line A549[2].

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

MCC1019 Related Antibodies

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).
In Vivo

MCC1019 (20-40 mg/kg; i.p.; daily; 16 days) induces 51.1% and 68.1% lung tumor growth inhibition, respectively, while reducing lung metastatic burden and showing minimal systemic toxicity in syngeneic murine lung cancer models[2].
MCC1019 (40 mg/kg; i.p.; daily; 14 days) induces 61.5% prostate tumor growth inhibition with no significant body weight changes in syngeneic murine prostate cancer models[2].
MCC1019 (100-200 mg/kg; p.o.; daily; 7 days) results in 100% survival and no significant body weight loss in healthy C57BL/6 mice[2].

MedChemExpress (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.
Molecular Weight

283.12

Formula

C12H11BrO3
CAS No.
SMILES

O=C(OCC)C=1OC=2C=CC=CC2C1CBr
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MCC1019 Related Classifications

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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:

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

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