1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. Plicamycin

Plicamycin (Synonyms: Mithramycin A)

Cat. No.: HY-A0122 Purity: >99.0%
Handling Instructions

Plicamycin is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.

For research use only. We do not sell to patients.

Plicamycin Chemical Structure

Plicamycin Chemical Structure

CAS No. : 18378-89-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 573 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Plicamycin is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.

IC50 & Target

Sp1 transcription factor[1]

In Vitro

Sp1 is a zinc-finger transcription factor that regulates multiple cellular functions and promotes tumor progression by controlling expression of genes involved in cell cycle, apoptosis and DNA damage. Sp1 binds to GC-rich motifs of promoters and interacts with components of the general transcriptional machinery and co-activator complexes of multiple signaling pathways. Plicamycin (Mith) decreases Sp1 protein by inducing proteasome-dependent degradation, thereby suppressing cervical cancer growth through a DR5/caspase-8/Bid signaling pathway. To assess the antiproliferative effects of Plicamycin on cervical cancer cells, two cervical cancer cell lines with different genetic backgrounds are grown with or without treatment with Plicamycin at different concentrations. Plicamycin inhibits HEp-2 and KB cell growth in a concentration-dependent manner after 48 h. Apoptotic cell death is qualitatively estimated by DAPI staining for nuclear condensation and fragmentation. Plicamycin leads to significant DNA fragmentation compared to untreated controls[1].

In Vivo

The antitumorigenic activity of Plicamycin (0.2 mg/kg/day) is determined in a xenograft model and observed reduction in tumor volume and weight. No significant mouse body weight loss is observed in Plicamycin-treatment groups, indicating that Plicamycin-associated toxicity is minimal. Plicamycin also increases TUNEL-positive cells in tumor xenografts. No notable intergroup differences are observed among organs, indicating no marked signs of systemic toxicity at the Plicamycin dose used in this study[1].

Molecular Weight

1085.15

Formula

C₅₂H₇₆O₂₄

CAS No.

18378-89-7

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (92.15 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9215 mL 4.6077 mL 9.2153 mL
5 mM 0.1843 mL 0.9215 mL 1.8431 mL
10 mM 0.0922 mL 0.4608 mL 0.9215 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

HEp-2 cells and KB cells are cultured in DMEM 100 U/mL each of Penicillin and Streptomycin and 10% FBS for HEp-2 cells and 5% FBS for KB in a humidified atmosphere containing 5% CO2 at 37°C. Equal numbers of cells are seeded and allowed to attach. At 50-60% confluence, cells are treated with DMSO or indicated concentrations of Plicamycin (50, 100, and 200 nM for HEp-2 cells; 20, 40, and 80 nM for KB cells). Cell viability is determined using CellTiter 96 Aqueous One Solution Cell Proliferation Assay Kits. In brief, cells are seeded in 96-well plates and incubated with Plicamycin. After treatment, 30 µL MTS solution is added to each well and cells are incubated for 2 h at 37°C. MTS solution is analyzed using a microplate reader at 490 nm and 690 nm[1].

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

Animal Administration
[1]

Mice[1]
Female nude mice are used. KB cells are suspended in sterile PBS and injected subcutaneously into the right flank of mice. Mice are randomized into two groups containing five mice each and treated with 0.2 mg/kg/day of Plicamycin (i.p.) three times per week for 29 days. Control mice receive an equal volume of vehicle. After 29 days, bodies, organs and tumors are weighed and tumor volumes determined. Tumors are measured[1].

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

References

Purity: >99.0%

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