WDR5-0102
Based on 1 Customer Validation
WDR5-0102 is an inhibitor of WDR5. WDR5-0102 specifically targets the WIN site of WDR5, disrupts the WDR5-MLL1 interaction, and reduces the histone methyltransferase activity of MLL1. WDR5-0102 exerts dose-dependent toxicity on MDSC-like cells and reduces their osteopontin levels, while showing extremely low cytotoxicity to pancreatic cancer cells. WDR5-0102 can be used in the research of related diseases such as acute myeloid leukemia, lymphoid leukemia, biphenotypic leukemia and pancreatic cancer.
For research use only. We do not sell to patients.
- Purity: 97.07%
- CAS No.: 824960-50-1
- Formula: C18H19ClN4O3
- Molecular Weight:374.82
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
WDR5-0102 inhibits recombinant human MLL1-WDR5 histone methyltransferase activity with an IC50 of 61.49 μM[2].
WDR5-0102 (25-100 μM; 24 h) decreases OPN protein levels in UN-KC-6141 mouse pancreatic tumor cells in vitro in a dose-dependent manner after 24 hours of incubation[2].
WDR5-0102 (0-100 μM; 24 h) exhibits minimal cytotoxicity to UN-KC-6141 mouse pancreatic tumor cells after 24 hours of incubation, with only a slight reduction in viability at 100 μM[2].
WDR5-0102 (0-100 μM; 24 h) exhibits minimal cytotoxicity to PANC02-H7 mouse pancreatic tumor cells after 24 hours of incubation, with only a slight reduction in viability at 100 μM[2].
WDR5-0102 (25-100 μM; 24 h) decreases OPN protein levels in J774M mouse MDSC-like cells in vitro in a dose-dependent manner after 24 hours of incubation[2].
WDR5-0102 (0-100 μM; 24 h) exhibits dose-dependent cytotoxicity to J774M mouse MDSC-like cells after 24 hours of incubation, reducing viability to ~60% at 100 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:UN-KC-6141 mouse pancreatic tumor cells
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Concentration:25-100 μM
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Incubation Time:24 h
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Result:Decreased OPN protein levels in UN-KC-6141 cells in a dose-dependent manner.
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Cell Line:UN-KC-6141 mouse pancreatic tumor cells
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Concentration:0-100 μM
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Incubation Time:24 h
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Result:Exhibited minimal cytotoxicity at 0, 25, and 50 μM.
Reduced cell viability to ~80% at 100 μM.
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Cell Line:PANC02-H7 mouse pancreatic tumor cells
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Concentration:0-100 μM
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Incubation Time:24 h
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Result:Exhibited minimal cytotoxicity at 0, 25, and 50 μM.
Reduced cell viability to ~80% at 100 μM.
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Cell Line:J774M mouse MDSC-like cells
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Concentration:25-100 μM
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Incubation Time:24 h
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Result:Decreased OPN protein levels in J774M cells in a dose-dependent manner.
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Cell Line:J774M mouse MDSC-like cells
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Concentration:0-100 μM
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Incubation Time:24 h
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Result:Reduced cell viability to ~90% at 25 μM.
Reduced cell viability to ~80% at 50 μM.
Reduced cell viability to ~60% at 100 μM.
Exhibited dose-dependent cytotoxicity.
Chemical Information
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CAS No. 824960-50-1
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Appearance Solid
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Molecular Weight 374.82
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Formula C18H19ClN4O3
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Color Light brown to brown
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SMILES
O=C(C1=C(Cl)C=CC=C1)NC2=CC([N+]([O-])=O)=CC=C2N3CCN(CC3)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL (133.40 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 1.67 mg/mL (4.46 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[2]. Lu C, et al. WDR5-H3K4me3 epigenetic axis regulates OPN expression to compensate PD-L1 function to promote pancreatic cancer immune escape. J Immunother Cancer. 2021;9(7):e002624. [Content Brief]
[3]. Ye X, et al. The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening. Bioorg Med Chem Lett. 2019;29(4):638-645. [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 (protect from light). 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 | 2.6679 mL | 13.3397 mL | 26.6795 mL | 66.6987 mL |
| 5 mM | 0.5336 mL | 2.6679 mL | 5.3359 mL | 13.3397 mL | |
| 10 mM | 0.2668 mL | 1.3340 mL | 2.6679 mL | 6.6699 mL | |
| 15 mM | 0.1779 mL | 0.8893 mL | 1.7786 mL | 4.4466 mL | |
| 20 mM | 0.1334 mL | 0.6670 mL | 1.3340 mL | 3.3349 mL | |
| 25 mM | 0.1067 mL | 0.5336 mL | 1.0672 mL | 2.6679 mL | |
| 30 mM | 0.0889 mL | 0.4447 mL | 0.8893 mL | 2.2233 mL | |
| 40 mM | 0.0667 mL | 0.3335 mL | 0.6670 mL | 1.6675 mL | |
| 50 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3340 mL | |
| 60 mM | 0.0445 mL | 0.2223 mL | 0.4447 mL | 1.1116 mL | |
| 80 mM | 0.0333 mL | 0.1667 mL | 0.3335 mL | 0.8337 mL | |
| 100 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6670 mL |
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