WDR5-IN-4

Name: WDR5-IN-4
Brand: MedChemExpress
SKU: HY-111753
Rating: 5.0 (3 reviews)

Cat. No.: HY-111753 Purity: 98.13%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

WDR5-IN-4 is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a K_d of 0.1 nM. WDR5-IN-4 displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.

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

WDR5-IN-4 Chemical Structure

CAS No. : 2407457-36-5

Size	Price	Stock	Quantity
1 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of WDR5-IN-4:

WDR5-IN-4 TFA Get quote

3 Publications Citing Use of MCE WDR5-IN-4

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•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Kd: 0.1 nM (WIN)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHP-134	GI₅₀	2.7 μM Compound: 1	Antiproliferative activity against human CHP134 cells expressing wild type p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay Antiproliferative activity against human CHP134 cells expressing wild type p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay	[PMID: 31858797]
Daudi	GI₅₀	6.8 μM Compound: 1	Antiproliferative activity against human Daudi cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay Antiproliferative activity against human Daudi cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay	[PMID: 31858797]
K562	GI₅₀	17000 nM Compound: 1	Antiproliferative activity against human K562 cells assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay Antiproliferative activity against human K562 cells assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay	[PMID: 31858797]
MOLM-13	GI₅₀	900 nM Compound: 1	Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay	[PMID: 31858797]
MV4-11	GI₅₀	600 nM Compound: 1	Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay	[PMID: 31858797]
Raji	GI₅₀	16 μM Compound: 1	Antiproliferative activity against human Raji cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay Antiproliferative activity against human Raji cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay	[PMID: 31858797]
Ramos	GI₅₀	7.1 μM Compound: 1	Antiproliferative activity against human Ramos cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay Antiproliferative activity against human Ramos cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay	[PMID: 31858797]
SW480	GI₅₀	> 29 μM Compound: 1	Antiproliferative activity against human SW480 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay Antiproliferative activity against human SW480 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay	[PMID: 31858797]
SW-620	GI₅₀	6.5 μM Compound: 1	Antiproliferative activity against human SW620 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay Antiproliferative activity against human SW620 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay	[PMID: 31858797]

Molecular Weight

498.38

Formula

C₂₅H₂₂Cl₂FN₅O

CAS No.

2407457-36-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC=C(CNC(C2=CC(CN3C(N(C)C=C3)=N)=CC(C4=C(C)N=C(F)C=C4)=C2)=O)C=C1Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (200.65 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	2.0065 mL	10.0325 mL	20.0650 mL
5 mM	0.4013 mL	2.0065 mL	4.0130 mL
10 mM	0.2007 mL	1.0033 mL	2.0065 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (5.02 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 (5.02 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 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 98.13%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (249 KB) HNMR (137 KB) RP-HPLC (139 KB) LCMS (112 KB)

Handling Instructions (2659 KB)

References

[1]. Aho ER, et al. Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep. 2019 Mar 12;26(11):2916-2928.e13. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0065 mL	10.0325 mL	20.0650 mL	50.1625 mL
	5 mM	0.4013 mL	2.0065 mL	4.0130 mL	10.0325 mL
	10 mM	0.2007 mL	1.0033 mL	2.0065 mL	5.0163 mL
	15 mM	0.1338 mL	0.6688 mL	1.3377 mL	3.3442 mL
	20 mM	0.1003 mL	0.5016 mL	1.0033 mL	2.5081 mL
	25 mM	0.0803 mL	0.4013 mL	0.8026 mL	2.0065 mL
	30 mM	0.0669 mL	0.3344 mL	0.6688 mL	1.6721 mL
	40 mM	0.0502 mL	0.2508 mL	0.5016 mL	1.2541 mL
	50 mM	0.0401 mL	0.2007 mL	0.4013 mL	1.0033 mL
	60 mM	0.0334 mL	0.1672 mL	0.3344 mL	0.8360 mL
	80 mM	0.0251 mL	0.1254 mL	0.2508 mL	0.6270 mL
	100 mM	0.0201 mL	0.1003 mL	0.2007 mL	0.5016 mL

WDR5-IN-4 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-IN-42407457-36-5Histone MethyltransferaseInhibitorinhibitorinhibit

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WDR5-IN-4

Customer Review

Other Forms of WDR5-IN-4:

WDR5-IN-4 Related Antibodies

3 Publications Citing Use of MCE WDR5-IN-4

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

WDR5-IN-4 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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