Home Tools

MS67

Catalog No. T39976 CAS 2407452-77-9

MS67 is a potent and selective degrader of the WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM. It exhibits no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters. Notably, MS67 demonstrates significant anticancer properties.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

MS67, CAS 2407452-77-9

Pack Size	Availability	Price/USD	Quantity
10 mg	8-10 weeks	$ 954.00

Bulk Inquiry

This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MS67 is a potent and selective degrader of the WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM. It exhibits no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters. Notably, MS67 demonstrates significant anticancer properties.
Targets&IC50	WDR5:63 nM (Kd)
In vitro	MS67, at concentrations ranging from 0.001 to 1 μM, effectively induces the degradation of WDR5, with noticeable activity initiating at concentrations as low as 1 nM. This compound demonstrates a pronounced ability to deplete WDR5 across various cell lines, including six mixed lineage leukemia (MLL)-rearranged (MLL-r) acute myeloid leukemia (AML) and four pancreatic ductal adenocarcinoma (PDAC) cell lines, without exhibiting a hook effect and displaying a concentration-dependent efficacy in PDAC cells. Furthermore, MS67 reduces H3K4me2/3 levels in both MV4;11 and MIA PaCa-2 cells, while not affecting other histone methylation markers such as H3K9me3, H3K27me3, and H3K36me3. It suppresses WDR5-related gene expression and WDR5/MLL-induced H3K4 methylations on chromatin. The GI50 values for the most sensitive AML cell lines, MV4;11 and EOL-1, are 15 nM and 38 nM, respectively, highlighting its potency. The sensitivity to MS67 is distinct in MLL-r acute leukemia cell lines (MV4;11, EOL-1, MOLM13, KOPN8, RS4;11, and THP-1), in contrast to leukemia cell lines lacking MLL-r arrangements, such as K562, HL60, and a murine AML line transformed by Hoxa9 plus Meis1, which show insensitivity to MS67. Additionally, MS67 exhibits binding affinity to the VCB (VHL-Elongin C-Elongin B ternary complex) with a Kd of 140 nM. Western Blot Analysis further confirms MS67-induced WDR5 degradation in MV4;11 cells across various concentrations after 18 hours of incubation, showcasing significant activity at a DC50 of 3.7 nM.
In vivo	MS67, administered intraperitoneally (i.p.) at a dose of 75 mg/kg twice daily for five days a week over a period of 20 days, significantly inhibits tumor growth in vivo and extends the survival of treated mice[1]. A single i.p. injection of MS67 at 75 mg/kg yields a peak concentration (Cmax) of approximately 4.2 μM, maintaining a concentration above 0.5 μM for over 12 hours[1]. This was observed in an MV4;11 MLL-r AML xenograft mouse model, demonstrating MS67’s efficacy in inhibiting tumor growth in vivo under the specified conditions[1].

Molecular Weight	1030.14
Formula	C52H59F4N9O7S
CAS No.	2407452-77-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Xufen Yu, et al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MS67 2407452-77-9 MS-67 MS 67 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.