2. Epigenetics
  3. WDR5
  4. WDR5-0103

WDR5-0103  (Synonyms: WD-Repeat Protein 5-0103)

Cat. No.: HY-19347 Purity: 99.93%
SDS
COA
Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

WDR5-0103 Chemical Structure

WDR5-0103 Chemical Structure

CAS No. : 890190-22-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

WDR5-0103 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE WDR5-0103

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

In Vitro

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.

WDR5-0103 Related Antibodies

Cell Viability Assay[2]

Cell Line: KB-3-1, KB-V1, S1 and S1-MI-80 cancer cells
Concentration: 10 μM
Incubation Time: 72 hours
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).
In Vivo

WDR5-0103 (2.5 mg/kg; intraperitoneal injection; once a day; for 3 days) can reduce the level of H3K4me3, improve cognitive deficits and restore synaptic function in P301S transgenic Tau mice[3].
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.

Animal Model: P301S transgenic Tau mice (both male and female, 5-6 months old)[3]
Dosage: 2.5 mg/kg (dissolved in DMSO and diluted with saline, DMSO concentration of working solution < 0.2%)
Administration: Intraperitoneal injection, once a day, for 3 days
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.
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]
Dosage: 2.5 mg/kg (dissolved in DMSO and diluted with saline, DMSO concentration of working solution < 0.2%)
Administration: Intraperitoneal injection, three times
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.
Molecular Weight

383.44

Formula

C21H25N3O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(OC)C1=CC=C(N2CCN(C)CC2)C(NC(C3=CC=CC(OC)=C3)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6080 mL 13.0399 mL 26.0797 mL
5 mM 0.5216 mL 2.6080 mL 5.2159 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.93%

SDS (459 KB)

COA (250 KB) HNMR (262 KB) LCMS (256 KB)

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 2.6080 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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WDR5-0103 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WDR5-0103890190-22-4WD-Repeat Protein 5-0103WDR5WD repeat protein-5WD40 repeat domain protein 5Inhibitorinhibitorinhibit

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