Proscillaridin A

SKU: orb2943137

Description

Proscillaridin A is a natural cardiac glycoside that potently inhibits both topoisomerase I and II with IC50 values of 30 nM and 100 nM, respectively. It is utilized in cancer research to study DNA damage mechanisms and has demonstrated cytotoxic effects in various in vitro cell line assays.

Research Area

Molecular Biology

Images & Validation

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Key Properties

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CAS Number	466-06-8
MW	530.65
Purity	98.38%
Formula	C₃₀H₄₂O₈
SMILES	O[C@@]12[C@]3([C@@]([C@]4(C)C(CC3)=C[C@@H](O[C@H]5[C@H](O)[C@H](O)[C@@H](O)[C@H](C)O5)CC4)(CC[C@]1(C)[C@H](CC2)C=6C=CC(=O)OC6)[H])[H]
Target	Topoisomerase
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.54 mM);DMSO:100 mg/mL (188.45 mM)

Bioactivity

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Target IC50

Topo I:30 nM |Topo II:100 nM

In Vitro

proscillaridin A, on the proliferation of breast cancer MCF-7 cells. In terms of inhibition of cell proliferation of MCF-7 cells, the compounds rank in the order proscillaridin A>digoxin>ouabain. While both digoxin and ouabain inhibited topoisomerase II catalytic activity at nanomolar concentrations (100 nM), neither agent inhibited topoisomerase I catalytic activity even at concentrations as high as 100 microM. On the other hand, proscillaridin A was a potent poison of topoisomerase I and II activity at nanomolar drug concentrations (30 nM, 100 nM, respectively), suggesting that this agent may produce its cytotoxic activity by targeting both enzymes simultaneously. These studies suggest that the stabilization of DNA-topoisomerase II complexes is closely linked to the mechanism of digoxin, ouabain and proscillaridin A cytotoxicity. The potential DNA-binding properties of the cardiac glycosides have been assessed by measuring the displacement of ethidium bromide from calf thymus DNA.

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Inhibitor, MCF-7, inhibit, breast, cell, cancer, Proscillaridin A, topoisomerase II, Topoisomerase, topoisomerase I

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Compound Identifiers

PubChem CID

5284613 ↗

Key Properties

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No computed properties available.

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