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Dp44mT | Metal chelator

Dp44mT (152095-12-0) is a metal chelator with potent antitumor activity.1,2 It displayed an average IC50 of 30 nM over 28 cancer cell lines (IC50 range was 5 nM to 400 nM).2 Dp44mT retained its antiproliferative activity in both etoposide-resistant MCF-7/VP clones (MCF-7 breast cancer cells) and vinblastine-resistant KB-VB1 clones (KB3-1 epidermoid carcinoma cells) with an IC50 = 12 nM for both lines.2 The potency of Dp44mT has been attributed to the high redox activity of the Dp44mT-Fe complex leading to cytotoxic ROS generation. The antitumor activity of Dp44mT may also be mediated by a redox active copper complex that causes cellular glutathione depletion and lysosomal damage.3,4 It also inhibited T-cell activation and prevented CD25 up-regulation via a copper-dependent mechanism.Dp44mT has recently been shown to effectively inhibit c-Met though metalloprotease-mediated cleavage and lysosomal degradation.6

References/Citations
1) Yuan et al. (2004), Novel di-2-pyridyl-derived iron chelators with marked and selective antitumor activity: in vitro and in vivo assessment; Blood, 104 1450
2) Whitnall et al. (2006), A class of iron chelators with a wide spectrum of potent antitumor activity that overcomes resistance to chemotherapeutics., Proc. Natl. Acad. Sci. USA 103 14910
3) Lovejoy et al. (2011), Antitumor activity of metal-chelating compound Dp44mT is mediated by formation of a redox-active copper complex that accumulates in lysosomes; Cancer Res., 71 5871
4) Gutierrez et al. (2014), The anticancer agent di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbzone (Dp44mT) overcomes prosurvival autophagy by two mechanisms: persistent reduction of autophagosome synthesis and impairment of lysosomal integrity; J. Biol. Chem., 289 33568
5) Gundelach et al. (2013), The anticancer drug Dp344mT inhibits T-cell activation and CD25 through a copper-dependent mechanism; FASEB J., 27 782
6)Park et al. (2020), Thiosemicarbazones suppress expression of the c-Met oncogene by mechanisms involving lysosomal degradation and intracellular shedding; J. Biol.Chem., 295 481

 

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Catalog#  10-4951-0005

$25.00
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CAS:
152095-12-0
Catalog Number:
10-4951
Activity:
Metal chelator
Chemical Name:
3-(Dipyridin-2-ylmethylideneamino)-1,1-
Molecular Weight:
285.37
Molecular Formula:
C14H15N5S
Solubility:
Soluble in DMSO (up to at least 25 mg/ml).
Physical Properties:
Orange solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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