Valemetostat

Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values [1][2][3].

Product Specifications

CAS Number

[1809336-39-7]

Product Name Alternative

DS-3201

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Valemetostat.html

Purity

99.84

Solubility

DMSO : 70 mg/mL (ultrasonic)

Smiles

CC1=C(O[C@@](C)([C@]2([H])CC[C@@H](N(C)C)CC2)O3)C3=C(Cl)C=C1C(NCC(C4=O)=C(C=C(C)N4)C)=O

Molecular Formula

C26H34ClN3O4

Molecular Weight

488.02

Precautions

H302, H315, H319, H335

References & Citations

[1]Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW.|[2]Shimizu J, Kawano F. Exercise-induced histone H3 trimethylation at lysine 27 facilitates the adaptation of skeletal muscle to exercise in mice. J Physiol. 2022 Jul;600 (14) :3331-3353.|[3]Yamagishi M, et al. Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas. Cell Rep. 2019 Nov 19;29 (8) :2321-2337.e7.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

EZH1

Citation 01

Cancer Res. 2025 May 15;85 (10) :1803-1818.|Cells. 2023 Dec 30;13 (1) :81.|Am J Pathol. 2025 Jun;195 (6) :1124-1140.|Protein Cell. 2025 Jun 20;16 (6) :439-457.