Valemetostat free base · Synonyms: DS-3201

Valemetostat is an EZH1/2 dual inhibitor.

For research use only. Not for human or veterinary use.

Target Histone Methyltransferase

Research area Cancer

Purity HPLC>98%; ee>99% Stock Inquire

Data Sheet SDS COA

Valemetostat structure

CAS No.: 1809336-39-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 550.00	BP-02146-100mg	In stock	Get quote
250 mg	USD 1,050.00	BP-02146-250mg	In stock	Get quote
500 mg	USD 1,580.00	BP-02146-500mg	In stock	Get quote
1 g	USD 2,400.00	BP-02146-1g	In stock	Get quote
2 g	USD 3,600.00	BP-02146-2g	Inquire	Get quote

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Description

Valemetostat (DS-3201) is an EZH1/2 dual inhibitor, used in the research of relapsed/refractory peripheral T-cell lymphoma.

Biological activity

In Vitro Valemetostat (1-1000 nM) strongly and specifically inhibits EZH1 and EZH2 with IC50 values ＜10 nM. Valemetostat (100 nM; 7 d) effectively removes H3K27me3 and also prevents unexpected gain of H3K27me3. Valemetostat (0.1-100 nM; 7 d) potently inhibits H3K27me3 by low-dose treatment in the sensitive lymphoma types. In Vivo Valemetostat (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training.

Identifiers

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
InChIKey: SSDRNUPMYCFXGM-UYPAYLBCSA-N

Specifications

MW (average): 488.0190
Formula: C₂₆H₃₄ClN₃O₄
CAS No.: 1809336-39-7
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO, not in water

Documents

References

[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.

Same target

Search Histone Methyltransferase

Same research area

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