WDR5-IN-1

Name: WDR5-IN-1
Brand: MedChemExpress
SKU: HY-133121
Rating: 4.5 (1 reviews)

Cat. No.: HY-133121 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a K_d of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC₅₀ of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.

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

WDR5-IN-1 Chemical Structure

CAS No. : 2408842-51-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 566	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 566	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 880	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2800	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 4500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

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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

Cellular Effect

Cell Line	Type	Value	Description	References
CHP-134	GI₅₀	0.26 μM Compound: 16	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	0.58 μM Compound: 16	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	8000 nM Compound: 16	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]
K562	GI₅₀	8000 nM Compound: 1	Anti-proliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay Anti-proliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay	[PMID: 35436124]
MOLM-13	GI₅₀	78 nM Compound: 16	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]
MOLM-13	GI₅₀	78 nM Compound: 1	Anti-proliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay Anti-proliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay	[PMID: 35436124]
MV4-11	GI₅₀	38 nM Compound: 16	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]
MV4-11	GI₅₀	38 nM Compound: 1	Anti-proliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay Anti-proliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay	[PMID: 35436124]
Raji	GI₅₀	1.2 μM Compound: 16	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	0.49 μM Compound: 16	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	> 22 μM Compound: 16	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	3.2 μM Compound: 16	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]

In Vitro

WDR5-IN-1 (1 μM; 48 hours) shows an apparent decrease in G2M phase cells^[1].
? WDR5-IN-1 (0.01-3 μM; 24-48 hours) increases p53 and p21 protein levels^[1].? WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	MV4:11 cells
Concentration:	1 µM
Incubation Time:	48 hours
Result:	Showed an approximate 4 fold increased SubG1 cells.

Western Blot Analysis^[1]

Cell Line:	MV4:11 cells
Concentration:	0.01, 0.03, 0.1, 0.3, 1, 3 µM
Incubation Time:	24, 48 hours
Result:	p53 and p21 protein levels started to increase from 8 h post treatment of compound 16 at 300 nM and continued to elevate up to 32 h.

Molecular Weight

514.59

Formula

C₃₀H₃₁FN₄O₃

CAS No.

2408842-51-1

Appearance

Solid

Color

Light yellow to brown

SMILES

COC1=CC(OC)=CC(CN2C(C(C=C(CN3C(N(C)C=C3)=N)C=C4C5=C(C)C=C(F)C=C5)=C4CC2)=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	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (194.33 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	1.9433 mL	9.7165 mL	19.4329 mL
5 mM	0.3887 mL	1.9433 mL	3.8866 mL
10 mM	0.1943 mL	0.9716 mL	1.9433 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 (4.86 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 (4.86 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.

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: ≥98.0%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (250 KB) HNMR (253 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Tian J, et al.Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.J Med Chem. 2020 Jan 23;63(2):656-675. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9433 mL	9.7165 mL	19.4329 mL	48.5824 mL
	5 mM	0.3887 mL	1.9433 mL	3.8866 mL	9.7165 mL
	10 mM	0.1943 mL	0.9716 mL	1.9433 mL	4.8582 mL
	15 mM	0.1296 mL	0.6478 mL	1.2955 mL	3.2388 mL
	20 mM	0.0972 mL	0.4858 mL	0.9716 mL	2.4291 mL
	25 mM	0.0777 mL	0.3887 mL	0.7773 mL	1.9433 mL
	30 mM	0.0648 mL	0.3239 mL	0.6478 mL	1.6194 mL
	40 mM	0.0486 mL	0.2429 mL	0.4858 mL	1.2146 mL
	50 mM	0.0389 mL	0.1943 mL	0.3887 mL	0.9716 mL
	60 mM	0.0324 mL	0.1619 mL	0.3239 mL	0.8097 mL
	80 mM	0.0243 mL	0.1215 mL	0.2429 mL	0.6073 mL
	100 mM	0.0194 mL	0.0972 mL	0.1943 mL	0.4858 mL

WDR5-IN-1 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-12408842-51-1Histone MethyltransferaseApoptosisMYCproliferativelymphomaneuroblastomaapoptosiscycleturmorigenesischromatin,Inhibitorinhibitorinhibit

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WDR5-IN-1

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WDR5-IN-1 Related Antibodies

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•Related Small Molecules:

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Purity & Documentation

References

Customer Review

WDR5-IN-1 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

WDR5-IN-1 Related Classifications

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