418805-02-4 Usage
Description
PYR 41, also known as Pyr41 (418805-02-4), is an irreversible and cell-permeable ubiquitin activating enzyme E1 (UBE1) inhibitor. It selectively targets and inhibits the E1 enzyme with little or no activity against E2 or E3 enzymes, making it a potent tool for studying the role of ubiquitination in various cellular processes.
Uses
Used in Pharmaceutical Industry:
PYR 41 is used as a research tool for studying the role of ubiquitination in cellular processes and its potential as a therapeutic target in various diseases. Its ability to selectively inhibit the E1 enzyme makes it a valuable compound for understanding the mechanisms of protein ubiquitination and the development of targeted therapies.
Used in Cancer Research:
PYR 41 is used as an inhibitor of ubiquitin activating enzyme E1 in cancer research. By inhibiting the E1 enzyme, PYR 41 can potentially disrupt the ubiquitin-proteasome system, which plays a crucial role in the regulation of cell cycle, apoptosis, and other cellular processes that are often dysregulated in cancer cells. This inhibition may lead to the development of novel cancer therapies targeting the ubiquitin-proteasome system.
Used in Cell Biology Research:
PYR 41 is used as a cell-permeable inhibitor in cell biology research to investigate the role of the ubiquitin-proteasome system in various cellular processes, such as protein degradation, signal transduction, and cell cycle regulation. Its cell-permeable property allows researchers to study the effects of E1 inhibition in living cells, providing valuable insights into the molecular mechanisms underlying these processes.
Biochem/physiol Actions
PYR-41 is a cell permeable inhibitor of Ubiquitin activating enzyme (E1) with little or no activity against E3, E2, or caspase enzymatic activity.
in vitro
in addition to blocking ubiquitylation, pyr-41 was found to increase total sumoylation in cells. pyr-41 could attenuate cytokine-mediated nuclear factor-kbactivation. this correlated with inhibition of nonproteasomal ubiquitylation of traf6, which is important to ikbkinase activation. pyr-41 also prevented the downstream ubiquitylation and proteasomal degradation of ikba. moreover, pyr-41 has demonstrated effective uae e1 inhibition as well as some off-target inhibition of the other ubiquitin regulatory enzymes and signal-transducing proteins, suggesting it is a nonspecific inhibitor [1].
References
1) Yang et al. (2007), Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics; Cancer Res., 67 9472
2) Mi et al. (2009), Cancer Preventive isothiocyanates induce selective degradation of cellular alpha- and beta-tubulins by proteasomes; J. Biol. Chem., 284 17039
3) Maehama et al. (2014), Nucleolar Stress Induces Ubiquitination-independent Proteasomal Degradation of PICT1 Protein PYR41; J. Biol. Chem., 289 20802 [Focus Citation]
Check Digit Verification of cas no
The CAS Registry Mumber 418805-02-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,1,8,8,0 and 5 respectively; the second part has 2 digits, 0 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 418805-02:
(8*4)+(7*1)+(6*8)+(5*8)+(4*0)+(3*5)+(2*0)+(1*2)=144
144 % 10 = 4
So 418805-02-4 is a valid CAS Registry Number.
