For research use only.

Catalog No.S7129

13 publications

PYR-41 Chemical Structure

Molecular Weight(MW): 371.3

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

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Selleck's PYR-41 has been cited by 13 publications

4 Customer Reviews

  • (D) Ubiquitination level of Htt protein was detected by immunoprecipitation with the GFP antibody and western blotting with the ubiquitin antibody from GFP-Htt(Q74)/PC12 cells treated as (C). Total Htt protein level served as the loading control. (E) GFP-Htt(Q74)/PC12 cells were treated as (C).Soluble Htt protein was detected by western blotting and quantified. Mean ± SEM, n = 5, ***p < 0.001 compared to the control group. (F) GO binding assay of GFP-Htt(Q74)/PC12 cells treated with GO, followed by Western blotting (left panel) with the ubiquitin antibody and Coomassie Brilliant Blue staining (right panel). L is the lysate before precipitation, while S and P were the supernatant and the pellet, respectively, after the precipitation. (G) Ubiquitination levels of Htt protein in supernatant lysate prepared from GO treated GFP-Htt(Q74)/PC12 cells with or without GO binding for 30 min.

    Nanoscale, 2016, 8: 18740-18750. PYR-41 purchased from Selleck.

  • (A) Serum-restricted A431 cells were pretreated with PYR-41 for 30 minutes prior to stimulation with EGF for 1 hour. Cells were lysed and incubated with UBA01 ubiquitin binding beads. Samples were separated by SDS-PAGE and analyzed by western blot for PD-L1. (B) WCL was analyzed for total PD-L1 levels and activated EGFR levels (p-EGFR). Tubulin was used as a loading control.

    Neoplasia, 2017, 19(4):346-353. PYR-41 purchased from Selleck.

  • (E) Intensities of protein bands were determined by densitometric analysis. Relative cellular levels of β2M were normalized to GAPDH levels and are presented relative to the levels in mock-infected and DMSO-treated cells (set as 1). Data are presented as means ± SD from three independent experiments. **, P < 0.01 between the indicated groups analyzed by Student's t test.

    J Virol, 2017, 91(5). PYR-41 purchased from Selleck.

  • Treatment with PYR-41 or thalidomide abrogates the endosomal recruitment of Sec61α. Murine bone marrow-derived DC (cultured for 4 d) conferred thalidomide (30 μM), PYR-41 (5 μM), or DMSO treatment prior to ovalbumin (50 μg/ml) or PBS pulse. The relocation of Sec61α from endoplasmic reticulum to endosomes was determined by confocal microscope by Rab5, calnexin, and Sec61α antibody staining. The expressions of Rab5/Sec61α and calnexin/Sec61α in the cells which are corresponding to the colocalized cells were shown (c). Nuclei were counterstained with DAPI (blue). Original magnification, ×600. Rab5: early endosome marker; calnexin: endoplasmic reticulum marker.

    J Immunol Res, 2018, 2018:5070573. PYR-41 purchased from Selleck.

Purity & Quality Control

Choose Selective E1 Activating Inhibitors

Biological Activity

Description PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
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 Ml\YSpVv[3Srb36gZZN{[Xl? M1jPdFMxKG2rbh?= NIi0R|dKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBpfW2jbjDVRWUu[2G2YXz5foVlKFWDRT3VZkB1cGmxZYP0[ZIhcW62ZYLt[YRq[XSnIH\vdo1ifGmxbjDlfJBz\XO|ZXSgbY4hUEl3IHnud4VkfCClZXzsd{Bi\nSncjCzNEBucW6|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m|LDDJR|UxRTFyIN88US=> NH7sOnMzOzN4MEKxOS=>
HI5 insect cells MVjGeY5kfGmxbjDhd5NigQ>? NIfSOZFKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBpfW2jbjDVRWUu[2G2YXz5foVlKFt|MmDdMWFOWDqdYT2zNnBeNUGWUDDlfINp[W6pZTDlfJBz\XO|ZXSgbY4hUEl3IHnud4VkfCClZXzsd{BjgSCWTFOgZY5idHm|aYOsJGlEPTB;Nj60JO69VQ>? Ml3wNlM{PjB{MUW=
insect cells MVPGeY5kfGmxbjDhd5NigQ>? Mo\vTY5pcWKrdHnvckBw\iCvb4Xz[UBz\WOxbXLpcoFvfCCKaYO2MZRi\2enZDDVRWUu[2G2YXz5foVlKFWDRT3VZkB1cGmxZYP0[ZIhcW62ZYLt[YRq[XSnIH\vdo1ifGmxbjDlfJBz\XO|ZXSgbY4hcW6|ZXP0JINmdGy|IHL5JHNFWy2SQVfFJIFv[Wy7c3nzMEBKSzVyPUGwJO69VQ>? MX:yN|M3ODJzNR?=

... 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)N2NC(=O)C(=C/C3=CC=C(O3)[N+]([O-])=O)/C2=O

In vivo Formulation Calculator (Clear solution)

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
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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