For research use only.

Catalog No.S7129

24 publications

PYR-41 Chemical Structure

CAS No. 418805-02-4

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

Selleck's PYR-41 has been cited by 24 publications

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Biological Activity

Description PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. PYR-41 induce apoptosis.
Ubiquitin-activating Enzyme E1 [1]
(Cell-free assay)
<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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HI5 insect cells NFq4VnJHfW6ldHnvckBie3OjeR?= M{TZNFMxKG2rbh?= Mon4TY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIFfTWE11[WepZXSgbJVu[W5iVVHFMYNifGGueYrl[EBWSUVvVXKgeIhqd2W|dHXyJIlvfGW{bXXkbYF1\SCob4LtZZRqd25iZYjwdoV{e2WmIHnuJGhKPSCrboPlZ5Qh[2WubIOgZYZ1\XJiM{CgcYlveyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqeyxiSVO1NF0yOCEQvF2= M2PxXlI{OzZyMkG1
HI5 insect cells NX\BV257TnWwY4Tpc44h[XO|YYm= MWXJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiR2PUMZRi\2enZDDoeY1idiCXQVWtZ4F1[Wy7enXkJHs{OlCfLVHNVFpc[S1|MmDdMWFVWCCneHPoZY5o\SCneIDy[ZN{\WRiaX6gTGk2KGmwc3XjeEBk\WyuczDifUBVVENiYX7hcJl{cXNuIFnDOVA:Pi52IN88US=> NWTZbo1XOjN|NkCyNVU>
insect cells M4S2S2Z2dmO2aX;uJIF{e2G7 NFPte5JKdmirYnn0bY9vKG:oIH3veZNmKHKnY3;tZolv[W62IFjpd|YufGGpZ3XkJHVCTS2lYYThcJl7\WRiVVHFMXVjKHSqaX;ld5RmeiCrboTldo1m\GmjdHWg[o9zdWG2aX;uJIV5eHKnc4Pl[EBqdiCrboPlZ5Qh[2WubIOgZpkhW0SVLWDBS2Uh[W6jbInzbZMtKEmFNUC9NVAh|ryP MkHnNlM{PjB{MUW=

... Click to View More Cell Line Experimental Data


Solubility (25°C)

In vitro DMSO 74 mg/mL (199.29 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 371.3


CAS No. 418805-02-4
Storage powder
in solvent
Synonyms N/A
Smiles CCOC(=O)C1=CC=C(C=C1)N2C(=O)C(=CC3=CC=C(O3)[N+](=O)[O-])C(=O)N2

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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E1 Activating Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID