PYR-41

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Chemical Information

Product name：PYR-41	Purity：98% min
CAS NO：418805-02-4	Solubility：DMSO : ≥ 46 mg/mL (123.89 mM)
Molecular Formula：C₁₇H₁₃N₃O₇	Package：Package according to customer requirements
Molecular Weight：371.301	Storage：Store at -20℃

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Remarks

PYR-41 is the first cell permeable inhibitor of ubiquitin-activating enzyme E1,irreversibly inhibits ubiquitin-activating enzyme activity.It is a pyrazone compound that showed little or no activity on E2,E3. Unexpectedly, despite of ubiquitylation inhibition, PYR-41 also enhances total sumoylation in cells. PYR41 also blocks the downstream ubiquitination and ubiquitination-dependent protein degradation or other ubiquitination-mediated cellular activities. Besides, PYR-41 inhibits degradation of p53, a tumour suppressor and also activates the transcription activity of it. PYR-41 and related pyrazones selectively kill transformed p53 expressing cells, suggesting that E1 inhibitors may be potential therapeutics in cancer.

References

[1]. Yang Y, et al. Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics. Cancer Res. 2007 Oct 1;67(19):9472-81.

[2]. Kapuria V, et al. Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity. Biochem Pharmacol. 2011 Aug 15;82(4):341-9.