1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme

PYR-41 

Cat. No.: HY-13296 Purity: >98.0%
Data Sheet SDS Handling Instructions

PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with no or little activity at E2.

For research use only. We do not sell to patients.
PYR-41 Chemical Structure

PYR-41 Chemical Structure

CAS No. : 418805-02-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
5 mg $60 In-stock
10 mg $100 In-stock
50 mg $380 In-stock
100 mg $720 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with no or little activity at E2.

IC50 & Target

IC50: < 10 μM (E1)

In Vitro

PYR-41 increases total sumoylation in cells in addition to blocking ubiquitylation. PYR-41 attenuates cytokine-mediated nuclear factor-κB activation. PYR-41 also prevents the downstream ubiquitylation and proteasomal degradation of IκBα. Furthermore, PYR-41 inhibits degradation of p53 and activates the transcriptional activity of this tumor suppressor[1]. PYR-41 (50 μM) promotes accumulation of ubiquitinated proteins. PYR-41 causes a concentration-dependent (10-50 μM) decline in DUB activity in Z138 cells after 4 h. PYR-41 potently inhibits USP5 DUB activity, even at the lowest concentration (10 μM). PYR-41 potently (10-50 μM) inhibits the activity of various DUBs, determined to represent USP9x, USP5, USP14, UCH37 and UCH-L3. Co-treatment of Z138 cells with DTT and PYR-41 completely abolishes the accumulation of ubiquitinated proteins[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.6932 mL 13.4662 mL 26.9324 mL
5 mM 0.5386 mL 2.6932 mL 5.3865 mL
10 mM 0.2693 mL 1.3466 mL 2.6932 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

371.3

Formula

C₁₇H₁₃N₃O₇

CAS No.

418805-02-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 46 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
PYR-41
Cat. No.:
HY-13296
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