Valemetostat (DS-3201)

Catalog No.S8926 Batch:S892603

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Technical Data

Formula

C26H34ClN3O4

 
Molecular Weight 488.02 CAS No. 1809336-39-7
Solubility (25°C)* In vitro DMSO 98 mg/mL (200.81 mM)
Ethanol 98 mg/mL (200.81 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.
Targets
EZH1 [1] EZH2 [1]
In vitro

Valemetostat significantly reducs ATL cell viability compared with the others. Valemetostat significantly reactivates the expression of the highly H3K27me3-accumulated EZH1/2 target genes in an ex vivo culture of primary ATL cells. Valemetostat shows superior anti-growth effects compared with EZH2-selective inhibitor in malignant lymphoma cell lines.[1].

Protocol (from reference)

Selleck's Valemetostat (DS-3201) has been cited by 7 publications

Lineage-specific canonical and non-canonical activity of EZH2 in advanced prostate cancer subtypes [ Nat Commun, 2024, 15(1):6779] PubMed: 39117665
Inhibiting EZH2 targets atypical teratoid rhabdoid tumor by triggering viral mimicry via both RNA and DNA sensing pathways [ Nat Commun, 2024, 15(1):9321] PubMed: 39472584
A novel EZH1/2 dual inhibitor inhibits GCB DLBCL through cell cycle regulation and M2 tumor-associated macrophage polarization [ J Biol Chem, 2024, 300(11):107788] PubMed: 39303914
Cytotoxicity of bendamustine, alone and in combination with novel agents, toward adult T-cell leukemia cells [ PLoS One, 2024, 19(9):e0309533] PubMed: 39348376
5-AZA Upregulates SOCS3 and PTPN6/SHP1, Inhibiting STAT3 and Potentiating the Effects of AG490 against Primary Effusion Lymphoma Cells [ Curr Issues Mol Biol, 2024, 46(3):2468-2479] PubMed: 38534772
Epigenetic plasticity safeguards heterochromatin configuration in mammals [ Nucleic Acids Res, 2023, gkad387] PubMed: 37178005
Exercise-induced histone H3 trimethylation at lysine 27 facilitates the adaptation of skeletal muscle to exercise in mice [ J Physiol, 2022, 600(14):3331-3353] PubMed: 35666835

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.