Dp44mT

Product Name

Dp44mT

CAS No.

152095-12-0

Molecular Weight

285.37

Target

Iron Chelator

Formula

C14H15N5S

Appearance

Solid

Purity

≥98.0%

SMILES

S=C(N/N=C(C1=NC=CC=C1)\C2=NC=CC=C2)N(C)C

Description

Dp44mT is an iron chelator with selective anticancer activity.

In Vitro Activity

Dp44mT is cytotoxic to breast cancer cells, at least in part, due to selective inhibition of top2α. Dp44mT alone induced selective cell killing in the breast cancer cell line MDA-MB-231 when compared with healthy mammary epithelial cells (MCF-12A). It induces G1 cell cycle arrest and reduces cancer cell clonogenic growth at nanomolar concentrations. Dp44mT, but not the iron chelator desferal, induces DNA double-strand breaks quantified as S139 phosphorylated histone foci (γ-H2AX) and Comet tails induced in MDA-MB-231 cells. Doxorubicin-induced cytotoxicity and DNA damage are both enhanced significantly in the presence of low concentrations of Dp44mT. The chelator caused selective poisoning of DNA topoisomerase IIα (top2α) as measured by an in vitro DNA cleavage assay and cellular topoisomerase-DNA complex formation. Dp44mT targets lysosome integrity through copper binding. Copper binding is essential for the potent antitumor activity of Dp44mT, as coincubation with nontoxic copper chelators markedly attenuated its cytotoxicity.

Storage

Powder, -20 °C, 3 years; 4 °C, 2 years In solvent: -80 °C, 6 months, -20 °C, 1 month.

Shipping

Room temperature in continental US; may vary elsewhere.