PYZD-4409
Based on 2 publication(s) in Google Scholar
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
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- Purity: 98.0%
- CAS No.: 423148-78-1
- 화학식: C14H7ClFN3O5
- 분자량:351.67
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) PYZD-4409
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Biological Activity
IC50: 20 μM (ubiquitin-activating enzyme UBA1)[1]
PYZD-4409 (10-40 μM; 72 hours; myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells) induces cell death with a LD50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20 μM. PYZD-4409 is preferentially cytotoxic to malignant cells over normal hematopoietic cells[1].
PYZD-4409 (50 μM; 4 hours; K562 leukemia cells) treatment blocks the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34[1].
PYZD-4409 (0-25 μM; 24 hours; K562 leukemia cells) significantly increases both mRNA and protein levels of Grp78 and Hsp70. In addition, PYZD-4409 increases levels of phospho-JNK and phospho-p38 mitogen-activated protein kinase, which have also been linked to ER stress and the unfolded protein response[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells
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Concentration:10 μM, 20 μM, 30 μM, 40 μM
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Incubation Time:72 hours
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Result:Induced cell death with a LD50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20 μM.
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Cell Line:K562 leukemia cells
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Concentration:50 μM
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Incubation Time:4 hours
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Result:Blocked the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34.
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Cell Line:K562 cells
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Concentration:0 μM, 10 μM, 25 μM
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Incubation Time:24 hours
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Result:Significantly increased both mRNA and protein levels of Grp78 and Hsp70.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male severe combined immunodeficient (SCID) mice with MDAY-D2 murine leukemia cells[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; daily on alternate days; for 16 days
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Result:Delayed tumor growth and decreased tumor weight without untoward toxicity.
Chemical Information
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CAS No. 423148-78-1
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Appearance Solid
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분자량 351.67
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화학식 C14H7ClFN3O5
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Color Light brown to black
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SMILES
FC1=CC=C(N2C(/C(C(N2)=O)=C\C3=CC=C([N+]([O-])=O)O3)=O)C=C1Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Commun Biol
Proteolysis targeting chimera (PROTAC)-driven antibody internalization of oncogenic cell surface receptors. [Abstract]2024 Dec 31;7(1):1719. PMID: 39741170 -
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
PYZD-4409 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.
용액&용해도
DMSO : ≥ 35 mg/mL (99.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (7.11 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
순도&문서
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Data Sheet (284 KB)
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SDS (479 KB)
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- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8436 mL | 14.2179 mL | 28.4357 mL | 71.0894 mL |
| 5 mM | 0.5687 mL | 2.8436 mL | 5.6871 mL | 14.2179 mL | |
| 10 mM | 0.2844 mL | 1.4218 mL | 2.8436 mL | 7.1089 mL | |
| 15 mM | 0.1896 mL | 0.9479 mL | 1.8957 mL | 4.7393 mL | |
| 20 mM | 0.1422 mL | 0.7109 mL | 1.4218 mL | 3.5545 mL | |
| 25 mM | 0.1137 mL | 0.5687 mL | 1.1374 mL | 2.8436 mL | |
| 30 mM | 0.0948 mL | 0.4739 mL | 0.9479 mL | 2.3696 mL | |
| 40 mM | 0.0711 mL | 0.3554 mL | 0.7109 mL | 1.7772 mL | |
| 50 mM | 0.0569 mL | 0.2844 mL | 0.5687 mL | 1.4218 mL | |
| 60 mM | 0.0474 mL | 0.2370 mL | 0.4739 mL | 1.1848 mL | |
| 80 mM | 0.0355 mL | 0.1777 mL | 0.3554 mL | 0.8886 mL |
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