PYR-41
Based on 26 publication(s) in Google Scholar
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.84%
- CAS 番号: 418805-02-4
- 分子式: C17H13N3O7
- 分子量:371.30
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Covalent Screening Library
HY-L036
-
Oxygen Sensing Compound Library
HY-L045
-
Ubiquitination Compound Library
HY-L050
-
Anti-Liver Cancer Compound Library
HY-L101
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Mitophagy Compound Library
HY-L180
-
Bioactive Compound Library Max
HY-L181
-
Covalent Screening Library Plus
HY-L036P
-
Bioactive Compound Library
HY-L001
-
Amino Acid Metabolism Compound Library
HY-L189
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
MedChemExpress（MCE）の使用を引用している文献 PYR-41
More- Cell Host Microbe. 2024 Jun 27:S1931-3128(24)00198-7. [Abstract]
- Nat Neurosci. 2023 May;26(5):751-764. [Abstract]
- Autophagy. 2025 Aug;21(8):1644-1661. [Abstract]
- Nat Commun. 2025 Oct 29;16(1):9554. [Abstract]
- J Clin Invest. 2025 Dec 1;135(23):e195279. [Abstract]
- Cell Death Differ. 2023 Jan;30(1):168-183. [Abstract]
- Chem Eng J. 2023 Nov 1, 475, 146449.
- Biomater Res. 2026 Apr 29.
- Diabetes. 2022 May 1;71(5):921-933. [Abstract]
- Int J Biol Macromol. 2026 Mar 11.
- Cell Prolif. 2021 Jan;54(1):e12919. [Abstract]
- Cells. 2022 Apr 8;11(8):1265. [Abstract]
- Int Immunopharmacol. 2020 Oct;87:106763. [Abstract]
- Mbio. 2020 Apr 14;11(2):e00467-20. [Abstract]
- Eur J Med Res. 2025 Sep 26;30(1):859. [Abstract]
- FASEB J. 2023 Oct;37(10):e23210. [Abstract]
- Pest Manag Sci. 2025 Nov 24. [Abstract]
- J Virol. 2025 Nov 25:e0164825. [Abstract]
- J Biol Chem. 2025 May 15:110242. [Abstract]
- PLoS Genet. 2025 Jul 10;21(7):e1011794. [Abstract]
- Chem Asian J. 2024 Sep 2:e202400824. [Abstract]
- Mol Cell Biol. 2018 Jul 16;38(15). pii: e00024-18. [Abstract]
- bioRxiv. 2026 Jan 29.
- bioRxiv. 2024 June 12.
- Research Square Preprint. 2024 Mar 20.
- Research Square Preprint. 2023 Sep 11.
Customer Validation & Images
-
WB
-
Histological Imaging/Staining
-
WB
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
生物活性
IC50: < 10 μM (E1)
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
22 μM
Compound: PYR-41
|
Cytotoxicity against human HEK293 cells assessed as cell viability measured by Cell titre glo assay
Cytotoxicity against human HEK293 cells assessed as cell viability measured by Cell titre glo assay
|
[PMID: 34246753] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 418805-02-4
-
性状 Solid
-
分子量 371.30
-
分子式 C17H13N3O7
-
Color Brown to reddish brown
-
SMILES
O=C(N1)/C(C(N1C2=CC=C(C=C2)C(OCC)=O)=O)=C/C3=CC=C([N+]([O-])=O)O3
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (26)
-
Journal Impact Factor
-
Most Recent
-
Cell Host Microbe
The antagonistic role of an E3 ligase pair in regulating plant NLR-mediated autoimmunity and fungal pathogen resistance. [Abstract]2024 Jun 27:S1931-3128(24)00198-7. PMID: 38955187
PYR-41 purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2024 Jun 27:S1931-3128(24)00198-7. [Abstract]
The treatment of PYR-41 (50 μM; 24 h), an E1 inhibitor, reduced PUB44-mediated CRCK3 ubiquitylation in N. benthamiana.
PYR-41 purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2024 Jun 27:S1931-3128(24)00198-7. [Abstract]
The PYR-41 (50 μM; 10 h) treatment reduced CRCK3 internalization of p35S::gCRCK3-GFP/WT transgenic plants.
-
Nat Neurosci
Emergence of consciousness from anesthesia through ubiquitin degradation of KCC2 in the ventral posteromedial nucleus of the thalamus. [Abstract]2023 May;26(5):751-764. PMID: 36973513
PYR-41 purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2023 May;26(5):751-764. [Abstract]
PYR-41 (10 μg/0.5 μL, each side) significantly reversed the downregulated KCC2 in the VPM of anesthetized mice.
PYR-41 purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2023 May;26(5):751-764. [Abstract]
PYR-41 (10 μg/0.5 μL, each side) treatment enhanced the effect of anesthesia, manifested as increased duration and depth of LORR and MRS in mice.
PYR-41 purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2023 May;26(5):751-764. [Abstract]
PYR-41 (10 μg/0.5 μL, each side) treatment prolonged time from the MRS to the RRR in C57BL/6J mice.
-
Autophagy
The alpha-coronavirus E protein inhibits the JAK-STAT pathway signaling by triggering STAT2 degradation through OPTN- and NBR1-mediated selective autophagy. [Abstract]2025 Aug;21(8):1644-1661. PMID: 40091174 -
Nat Commun
Nanomaterial signatures program biomolecular condensates via triphasic separation for chemoplasticity remodeling. [Abstract]2025 Oct 29;16(1):9554. PMID: 41162367 -
J Clin Invest
LC3-dependent intercellular transfer of phosphorylated STAT1/2 elicits CXCL9+ macrophages and enhances radiation-induced antitumor immunity. [Abstract]2025 Dec 1;135(23):e195279. PMID: 41321309 -
Cell Death Differ
FAAH served a key membrane-anchoring and stabilizing role for NLRP3 protein independently of the endocannabinoid system. [Abstract]2023 Jan;30(1):168-183. PMID: 36104448 -
-
-
Diabetes
Hepatokine ERAP1 Disturbs Skeletal Muscle Insulin Sensitivity Via Inhibiting USP33-Mediated ADRB2 Deubiquitination. [Abstract]2022 May 1;71(5):921-933. PMID: 35192681 -
-
Cell Prolif
Inhibition of deubiquitination by PR-619 induces apoptosis and autophagy via ubi-protein aggregation-activated ER stress in oesophageal squamous cell carcinoma. [Abstract]2021 Jan;54(1):e12919. PMID: 33129231 -
Cells
2022 Apr 8;11(8):1265. PMID: 35455946 -
Int Immunopharmacol
Ubiquitin specific protease 5 negatively regulates the IFNs-mediated antiviral activity via targeting SMURF1. [Abstract]2020 Oct;87:106763. PMID: 32683298
PYR-41 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2020 Oct;87:106763. [Abstract]
293 T cells are pretreated with DMSO or PYR41 for 3 h, and then PYR41 inhibitor is added followed by stimulation with IFNα and VSV. After 24 h, VSVG protein expression level is determined by Western blotting analyses.
-
Mbio
A Sensitive Yellow Fever Virus Entry Reporter Identifies Valosin-Containing Protein (VCP/p97) as an Essential Host Factor for Flavivirus Uncoating. [Abstract]2020 Apr 14;11(2):e00467-20. PMID: 32291299 -
Eur J Med Res
RHBDD1 induces cell cycle arrest in TP53-mutant NSCLC cells by promoting endoplasmic reticulum-associated degradation of p53 and DNA-PKcs. [Abstract]2025 Sep 26;30(1):859. PMID: 41013641 -
FASEB J
PYR-41, an inhibitor of ubiquitin-activating enzyme E1, attenuates 2,4-dinitrochlorobenzene-induced atopic dermatitis-like skin lesions in mice. [Abstract]2023 Oct;37(10):e23210. PMID: 37738047 -
Pest Manag Sci
Targeting the E1 ubiquitin-activating enzyme Uba1 impairs male fertility in Bactrocera dorsalis. [Abstract]2025 Nov 24. PMID: 41287186 -
J Virol
SUMOylation-dependent degradation of nucleocapsid is responsible for Pestivirus uncoating. [Abstract]2025 Nov 25:e0164825. PMID: 41288382 -
J Biol Chem
Machine learning-based multimodal radiomics and transcriptomics models for predicting radiotherapy sensitivity and prognosis in esophageal cancer. [Abstract]2025 May 15:110242. PMID: 40381695 -
PLoS Genet
2025 Jul 10;21(7):e1011794. PMID: 40638681 -
Chem Asian J
Selective Protein Degradation through Tetrazine Ligation of Genetically Incorporated Unnatural Amino Acids. [Abstract]2024 Sep 2:e202400824. PMID: 39221720 -
Mol Cell Biol
Monoubiquitination of Cancer Stem Cell Marker CD133 at Lysine 848 Regulates Its Secretion and Promotes Cell Migration. [Abstract]2018 Jul 16;38(15). pii: e00024-18. PMID: 29760280
PYR-41 purchased from MedChemExpress. Usage Cited in: Mol Cell Biol. 2018 Jul 16;38(15). pii: e00024-18. [Abstract]
Western blotting assays demonstrate that treatment of 20 μM PYR-41 or 20 μM PYZD-4409 inhibits ubiquitination and CD133 secretion. Hsp90 and β-actin are used as loading controls.
-
-
-
-
溶剤 & 溶解度
DMSO : 50 mg/mL (134.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
-
データシート (278 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Yang Y, et al. Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics. Cancer Res. 2007 Oct 1;67(19):9472-81. [Content Brief]
[2]. Kapuria V, et al. Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity. Biochem Pharmacol. 2011 Aug 15;82(4):341-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6932 mL | 13.4662 mL | 26.9324 mL | 67.3310 mL |
| 5 mM | 0.5386 mL | 2.6932 mL | 5.3865 mL | 13.4662 mL | |
| 10 mM | 0.2693 mL | 1.3466 mL | 2.6932 mL | 6.7331 mL | |
| 15 mM | 0.1795 mL | 0.8977 mL | 1.7955 mL | 4.4887 mL | |
| 20 mM | 0.1347 mL | 0.6733 mL | 1.3466 mL | 3.3666 mL | |
| 25 mM | 0.1077 mL | 0.5386 mL | 1.0773 mL | 2.6932 mL | |
| 30 mM | 0.0898 mL | 0.4489 mL | 0.8977 mL | 2.2444 mL | |
| 40 mM | 0.0673 mL | 0.3367 mL | 0.6733 mL | 1.6833 mL | |
| 50 mM | 0.0539 mL | 0.2693 mL | 0.5386 mL | 1.3466 mL | |
| 60 mM | 0.0449 mL | 0.2244 mL | 0.4489 mL | 1.1222 mL | |
| 80 mM | 0.0337 mL | 0.1683 mL | 0.3367 mL | 0.8416 mL | |
| 100 mM | 0.0269 mL | 0.1347 mL | 0.2693 mL | 0.6733 mL |
PYR-41 関連分類
HY-13296 関連分類
Powered by Bioz