PYR-41

Catalog No.S7129

For research use only.

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

PYR-41 Chemical Structure

CAS No. 418805-02-4

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

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. PYR-41 induce apoptosis.
Targets
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 MVHGeY5kfGmxbjDhd5NigQ>? MmHON|AhdWmw NE\ZPGdKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBpfW2jbjDVRWUu[2G2YXz5foVlKFWDRT3VZkB1cGmxZYP0[ZIhcW62ZYLt[YRq[XSnIH\vdo1ifGmxbjDlfJBz\XO|ZXSgbY4hUEl3IHnud4VkfCClZXzsd{Bi\nSncjCzNEBucW6|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m|LDDJR|UxRTFyIN88US=> NYDxOW82OjN|NkCyNVU>
HI5 insect cells MlfBSpVv[3Srb36gZZN{[Xl? M1rYSGlvcGmkaYTpc44hd2ZiTj30[ZJucW6jbDDHV3QufGGpZ3XkJIh2dWGwIGXBSU1k[XSjbIn6[YQhYzN{UG2tRW1RQlujLUOyVH0uSVSSIHX4Z4hidmenIHX4dJJme3OnZDDpckBJUTViaX7z[YN1KGOnbHzzJIJ6KFSOQzDhcoFtgXOrczygTWM2OD14LkSg{txO NUHRXlMzOjN|NkCyNVU>
insect cells NHmz[pVHfW6ldHnvckBie3OjeR?= MlW3TY5pcWKrdHnvckBw\iCvb4Xz[UBz\WOxbXLpcoFvfCCKaYO2MZRi\2enZDDVRWUu[2G2YXz5foVlKFWDRT3VZkB1cGmxZYP0[ZIhcW62ZYLt[YRq[XSnIH\vdo1ifGmxbjDlfJBz\XO|ZXSgbY4hcW6|ZXP0JINmdGy|IHL5JHNFWy2SQVfFJIFv[Wy7c3nzMEBKSzVyPUGwJO69VQ>? NXzQXmI3OjN|NkCyNVU>

Protocol (from reference)

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.

2mg/mL

Chemical Information

Molecular Weight 371.3
Formula

C17H13N3O7

CAS No. 418805-02-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C1=CC=C(C=C1)N2C(=O)C(=CC3=CC=C(O3)[N+](=O)[O-])C(=O)N2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

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.

Handling Instructions

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