WDR5-0103
Based on 2 publication(s) in Google Scholar
WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with a Kd of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases.
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- Pureza: 99.94%
- No. CAS: 890190-22-4
- Fòrmula: C21H25N3O4
- Peso molecular:383.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Epigenetics Compound Library
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Publications Citing Use of MedChemExpress (MCE) WDR5-0103
More
Actividad biológica
WDR5-0103 (5-20 μM; 72 hours) can sensitize ABCB1- or ABCG2-overexpressing multidrug-resistant cancer cells to conventional cytotoxic drugs in a concentration-dependent manner in experiments with multiple cell lines[2].
WDR5-0103 (1-10 μM; 72 hours) does not alter the protein expression of ABCB1 or ABCG2 in multidrug-resistant cancer cells[2].
WDR5-0103 (10 μM; 48 hours) can significantly restore drug-induced apoptosis in ABCB1- or ABCG2-overexpressing multidrug-resistant cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KB-3-1, KB-V1, S1 and S1-MI-80 cancer cells
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Concentration:10 μM
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Incubation Time:72 hours
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Result:Significantly restored drug-induced apoptosis in ABCB1-overexpressing KB-V1 cells and ABCG2-overexpressing S1-MI-80 cells when co-treated with apoptotic inducers (Colchicine (HY-16569) for KB-V1 and Topotecan (HY-13768A) for S1-MI-80).
WDR5-0103 (2.5 mg/kg; intraperitoneal injection; three times) can reduce the level of H3K4me3 in the prefrontal cortex and improve cognitive function in 5xFAD mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:P301S transgenic Tau mice (both male and female, 5-6 months old)[3]
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Dosage:2.5 mg/kg (dissolved in DMSO and diluted with saline, DMSO concentration of working solution < 0.2%)
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Administration:Intraperitoneal injection, once a day, for 3 days
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Result:In behavioral tests, the discrimination ratio in the novel object recognition test and the spatial memory index in the Barnes maze test were significantly improved, indicating the amelioration of cognitive deficits.
Western blot analysis showed that the decreased levels of synaptic GluR1, NR1, and NR2A subunits were remarkably restored.
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Animal Model:5xFAD mice (both male and female, 5-6 months old; transgenic mice carrying five familial AD mutations on human amyloid precursor protein and human presenilin 1, a model of Alzheimer's disease)[3]
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Dosage:2.5 mg/kg (dissolved in DMSO and diluted with saline, DMSO concentration of working solution < 0.2%)
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Administration:Intraperitoneal injection, three times
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Result:Reduced the level of H3K4me3 in the prefrontal cortex of 5xFAD mice. In behavioral tests, the discrimination ratio in the novel object recognition test and the spatial memory index in the Barnes maze test were significantly improved, indicating the improvement of cognitive function.
Chemical Information
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No. CAS 890190-22-4
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Appearance Solid
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Peso molecular 383.44
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Fòrmula C21H25N3O4
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Color Light yellow to yellow
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SMILES
O=C(OC)C1=CC=C(N2CCN(C)CC2)C(NC(C3=CC=CC(OC)=C3)=O)=C1
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Synonyms
WD-Repeat Protein 5-0103
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Cancer Commun (Lond)
Nicotinamide N-methyltransferase negatively regulates metastasis-promoting property of cancer-associated fibroblasts in lung adenocarcinoma. [Abstract]2025 Feb;45(2):110-137. PMID: 39623600 -
Reproduction
Fibroblast Growth Factor 9 Promotes Rat Leydig Cell Development via H3K4me3 Histone Modifications. [Abstract]2026 Jun 19:xaag076. PMID: 42320039
Solvente y solubilidad
DMSO : 50 mg/mL (130.40 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, 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 (6.52 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.52 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (459 KB)
- English - EN (459 KB)
- Français - FR (459 KB)
- Deutsch - DE (459 KB)
- Norwegian - NO (459 KB)
- Español - ES (459 KB)
- Swedish - SV (459 KB)
- Italian - IT (459 KB)
- Korean - KR (459 KB)
- Portuguese - PT (459 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159. [Content Brief]
[2]. Wu CP, et al. The WD repeat-containing protein 5 (WDR5) antagonist WDR5-0103 restores the efficacy of cytotoxic drugs in multidrug-resistant cancer cells overexpressing ABCB1 or ABCG2. Biomed Pharmacother. 2022 Oct;154:113663. [Content Brief]
[3]. Cao Q, et al. Targeting histone K4 trimethylation for treatment of cognitive and synaptic deficits in mouse models of Alzheimer's disease. Sci Adv. 2020 Dec 9;6(50):eabc8096. [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, 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 | 2.6080 mL | 13.0398 mL | 26.0797 mL | 65.1992 mL |
| 5 mM | 0.5216 mL | 2.6080 mL | 5.2159 mL | 13.0398 mL | |
| 10 mM | 0.2608 mL | 1.3040 mL | 2.6080 mL | 6.5199 mL | |
| 15 mM | 0.1739 mL | 0.8693 mL | 1.7386 mL | 4.3466 mL | |
| 20 mM | 0.1304 mL | 0.6520 mL | 1.3040 mL | 3.2600 mL | |
| 25 mM | 0.1043 mL | 0.5216 mL | 1.0432 mL | 2.6080 mL | |
| 30 mM | 0.0869 mL | 0.4347 mL | 0.8693 mL | 2.1733 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6520 mL | 1.6300 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.3040 mL | |
| 60 mM | 0.0435 mL | 0.2173 mL | 0.4347 mL | 1.0867 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8150 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6520 mL |
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