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.
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.
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.
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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.
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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
Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
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.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,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.
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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.