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PYR-41

Catalog No. T6629 CAS 418805-02-4

Synonyms: PYR41, PYR 41

PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.

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PYR-41, CAS 418805-02-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 52.00
10 mg	In stock	$ 79.00
25 mg	In stock	$ 165.00
50 mg	In stock	$ 327.00
100 mg	In stock	$ 497.00
200 mg	In stock	$ 687.00
500 mg	In stock	$ 1,080.00
1 mL * 10 mM (in DMSO)	In stock	$ 58.00

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Purity: 99.24%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
Targets&IC50	E1:< 10 μM
In vitro	PYR-41 (50 μM) inhibits activity of ubiquitin-activating enzyme E1 by over 90%. PYR-41 could be a target for nucleophilic attack and potentially reacts with the active site cysteine of E1. PYR-41 efficiently blocks cyclin E degradation. PYR-41 decreases the level of E1fUb thioesters in cells with a IC50 of between 10 and 25 μM, and prevents proteasome inhibitor–induced accumulation of ubiquitylated proteins. PYR-41 increases total sumoylation in cells and in cell harboring temperature-sensitive E1. PYR-41 is able to inhibit both proteasome-dependent and proteasome-independent activities of ubiquitylation. PYR-41 (50 μM) attenuates 1 ng/mL IL-1α-mediated nuclear factor-κB activation by >60% through preventing the downstream ubiquitylation and proteasomal degradation of IκBα. PYR-41 inhibits degradation of p53 and activates the transcriptional activity of p53, which enable its differentially killing transformed p53-expressing cells. [1] PYR-41 blocks ubiquitination reactions but paradoxically leads to the accumulation of high MW ubiquitinated proteins. PYR-41 also has equal or greater inhibitory activity against several deubiquitinases (DUBs) in intact cells and purified USP5 in vitro. PYR-41 also mediates cross-linking of specific protein kinases (Bcr-Abl, Jak2) to inhibit their signaling activity. [1]
Kinase Assay	Rabbit or mouse E1 (apper 250 ng) is incubated with 32P-ubiquitin in 1× reaction buffer [50 mM Tris (pH 7.4), 0.2 mM ATP, 0.5 mM MgCl2] at room temperature for 15 min. In some experiments, the His-tagged mouse E1 is bound to TALON cobalt affinity resin before carrying out incubations and reactions. Mouse E1 and 32P-ubiquitin are added to the beads in 1× reaction buffer and incubated as for E1 reactions. Samples are heated in nonreducing SDS-PAGE sample buffer and resolved by SDS-PAGE. Thioesters with ubiquitin are visualized by Storm PhosphoImager.

Synonyms	PYR41, PYR 41
Molecular Weight	371.3
Formula	C17H13N3O7
CAS No.	418805-02-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 37.1 mg/mL (100 mM)

References and Literature

1. Yang Y, et al. Cancer Res, 2007, 67(19), 9472-9481. 2. Kapuria V, et al. Biochem Pharmacol, 2011, 82(4), 341-349.

Citations

1. Kosmider O, Possémé C, Templé M, et al.VEXAS syndrome is characterized by inflammasome activation and monocyte dysregulation.Nature Communications.2024, 15(1): 910.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Human Metabolite Library Bioactive Compound Library Anti-Aging Compound Library Apoptosis Compound Library Covalent Inhibitor Library Bioactive Compounds Library Max Autophagy Compound Library HIF-1 Signaling Pathway Compound Library

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Keywords

PYR-41 418805-02-4 Apoptosis Ubiquitination E1/E2/E3 Enzyme E3 ligating enzyme PYR41 E1 activating enzyme PYR 41 Inhibitor Ubiquitin conjugating enzyme E2 conjugating enzyme Ubiquitin activating enzyme Ubiquitin ligase inhibit inhibitor

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