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PYR-41

Chemical Structure : PYR-41

CAS No.: 418805-02-4

PYR-41 (PYR41;PYR 41)

Catalog No.: PC-43474Not For Human Use, Lab Use Only.

PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of <10 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of <10 uM.
PYR-41 does not affect the transfer of ubiquitin to E2 from E1, directly inhibits E1, but not E2.
In addition to blocking ubiquitylation, PYR-41 increases total sumoylation in cells, attenuates cytokine-mediated nuclear factor-kappaB activation and inhibits nonproteasomal (Lys-63) ubiquitylation of TRAF6, also prevents the downstream ubiquitylation and proteasomal degradation of IκBα。
PYR-41 inhibits degradation of p53 and activates the p53 transcriptional activity, demonstrates anti-tumor activity in animal studies.

Physicochemical Properties

M.Wt 371.30
Formula C17H13N3O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 46 mg/mL

Chemical Name/SMILES

Benzoic acid, 4-[4-[(5-nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]-, ethyl ester

References

1. Yang Y, et al. Cancer Res. 2007 Oct 1;67(19):9472-81.

2. Kapuria V, et al. Biochem Pharmacol. 2011 Aug 15;82(4):341-9.

3. Chen C, et al. Immunology. 2014 Jun;142(2):307-19.

4. Matsuo S, et al. Shock. 2018 Apr;49(4):442-450.

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