Valemetostat

• Description:

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

• 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.

• CAS Number:

  1809336-39-7