Valemetostat | DS-3201 | EZH1/2 Inhibitor | AmBeed-信号通路专用抑制剂

Valemetostat {[allProObj[0].p_purity_real_show]}

货号：A662558 同义名： DS-3201; (R)-OR-S2

Valemetostat是一种蛋白甲基转移酶（PRMT）抑制剂，同时靶向EZH1和EZH2。

Valemetostat 化学结构
CAS号：1809336-39-7

Valemetostat 3D分子结构
CAS号：1809336-39-7

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Valemetostat 纯度/质量文件产品仅供科研

货号：A662558 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

Valemetostat 质控信息

组蛋白甲基转移酶亚型比较

产品名称	Histone Methyltransferase ↓ ↑	纯度
BRD4770	✔	99%+
UNC1999	+++ EZH2, IC50: 2 nM EZH1, IC50: 45 nM	99%+
EPZ005687	++ EZH2, Ki: 24 nM	98+%
EPZ015666	+++ PRMT5, Ki: 5 nM	99%+
3-Deazaneplanocin A HCl	++++ S-adenosylhomocysteine hydrolase, Ki: 50 pM	99%+
Tazemetostat	+++ EZH2, IC50: 11 nM EZH2, Ki: 2.5 nM	98%
GSK126	++ EZH2, IC50: 9.9 nM	99%+
MI-3	+ Menin-MLL, IC50: 648 nM	98%
MM-102	++ MLL1, IC50: 0.4 μM	99%
EI1	++ Ezh2 (wild-type), IC50: 15 nM EZH2 (Y641F), IC50: 13 nM	96%
SGC0946	++++ DOT1L, IC50: 0.3 nM	99%+
PFI-2 HCl	++++ SETD7, IC50: 2 nM SETD7, Ki: 0.33 nM	99%+
Pinometostat	++++ DOT1L, Ki: 80 pM	99%+
EPZ004777	+++ DOT1L, IC50: 0.4 nM	99%+
Entacapone	++ COMT, IC50: 151 nM	95%
UNC0379	+ SETD8, IC50: 7.9 μM	99%+
Menin-MLL inhibitor MI-2	+ Menin-MLL, IC50: 446 nM	98%
GSK343	+++ EZH2, IC50: 4 nM EZH1, IC50: 240 nM	99%+
BIX-01294 3HCl	+ G9a, IC50: 2.7 μM	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Valemetostat 生物活性

描述

Valemetostat is an antineoplastic agent.

Valemetostat 细胞实验

Cell Line BCBL-1 cells BC3 cells TCS627 cells ATL cell lines (TL-Om1, ATN-1) PBMCs HCT-5 cells HCT-4 cells BCBL-1 cells BC3 cells	Concentration	Treated Time	Description	References
BCBL-1 cells	1 µM	24 hours	To evaluate the activation of the KSHV lytic cycle by DS, results showed DS induced the expression of KbZIP and p64	Viruses. 2024 Sep 20;16(9):1490.
BC3 cells	1 µM	24 hours	To evaluate the activation of the KSHV lytic cycle by DS, results showed DS induced the expression of KbZIP and p64	Viruses. 2024 Sep 20;16(9):1490.
TCS627 cells	0.02 µM, 0.2 µM, 2 µM	48 hours	To evaluate the growth inhibitory potential of EZH1/2 inhibitor valemetostat on TCS627 cells, showing only 25% growth reduction at 2 µM concentration.	Cells. 2023 Dec 30;13(1):81.
ATL cell lines (TL-Om1, ATN-1)	10 nM to 100 nM	2 months	Establish resistant cell models and evaluate resistance mechanisms	Nature. 2024 Mar;627(8002):221-228.
PBMCs	0.1 μM and 1 μM	7 days	To evaluate the inhibitory effect of Valemetostat on spontaneous proliferation of PBMCs from HAM patients. Results showed that Valemetostat significantly inhibited the spontaneous proliferation of PBMCs.	Front Microbiol. 2023 Jun 12;14:1175762.
HCT-5 cells	1 μM	21 days	To evaluate the effect of Valemetostat on cell viability and apoptosis in HTLV-1-infected cell lines. Results showed that Valemetostat significantly reduced the viability of HCT-5 cells and induced early apoptosis.	Front Microbiol. 2023 Jun 12;14:1175762.
HCT-4 cells	1 μM	21 days	To evaluate the effect of Valemetostat on cell viability and apoptosis in HTLV-1-infected cell lines. Results showed that Valemetostat significantly reduced the viability of HCT-4 cells and induced early apoptosis.	Front Microbiol. 2023 Jun 12;14:1175762.
BCBL-1 cells	1 µM or 2 µM	48 hours	To evaluate the effect of Valemetostat on PEL cell survival and STAT3 activation. Results showed that Valemetostat slightly reduced PEL cell survival and slightly affected STAT3 phosphorylation and c-Myc expression.	Curr Issues Mol Biol. 2024 Mar 14;46(3):2468-2479.
BC3 cells	1 µM or 2 µM	48 hours	To evaluate the effect of Valemetostat on PEL cell survival and STAT3 activation. Results showed that Valemetostat slightly reduced PEL cell survival and slightly affected STAT3 phosphorylation and c-Myc expression.	Curr Issues Mol Biol. 2024 Mar 14;46(3):2468-2479.

Cell Line

BCBL-1 cells BC3 cells TCS627 cells ATL cell lines (TL-Om1, ATN-1) PBMCs HCT-5 cells HCT-4 cells BCBL-1 cells BC3 cells

Concentration

Treated Time

Description

References

BCBL-1 cells

1 µM

24 hours

To evaluate the activation of the KSHV lytic cycle by DS, results showed DS induced the expression of KbZIP and p64

Viruses. 2024 Sep 20;16(9):1490.

BC3 cells

1 µM

24 hours

To evaluate the activation of the KSHV lytic cycle by DS, results showed DS induced the expression of KbZIP and p64

Viruses. 2024 Sep 20;16(9):1490.

TCS627 cells

0.02 µM, 0.2 µM, 2 µM

48 hours

To evaluate the growth inhibitory potential of EZH1/2 inhibitor valemetostat on TCS627 cells, showing only 25% growth reduction at 2 µM concentration.

Cells. 2023 Dec 30;13(1):81.

ATL cell lines (TL-Om1, ATN-1)

10 nM to 100 nM

2 months

Establish resistant cell models and evaluate resistance mechanisms

Nature. 2024 Mar;627(8002):221-228.

PBMCs

0.1 μM and 1 μM

7 days

To evaluate the inhibitory effect of Valemetostat on spontaneous proliferation of PBMCs from HAM patients. Results showed that Valemetostat significantly inhibited the spontaneous proliferation of PBMCs.

Front Microbiol. 2023 Jun 12;14:1175762.

HCT-5 cells

1 μM

21 days

To evaluate the effect of Valemetostat on cell viability and apoptosis in HTLV-1-infected cell lines. Results showed that Valemetostat significantly reduced the viability of HCT-5 cells and induced early apoptosis.

Front Microbiol. 2023 Jun 12;14:1175762.

HCT-4 cells

1 μM

21 days

Front Microbiol. 2023 Jun 12;14:1175762.

BCBL-1 cells

1 µM or 2 µM

48 hours

To evaluate the effect of Valemetostat on PEL cell survival and STAT3 activation. Results showed that Valemetostat slightly reduced PEL cell survival and slightly affected STAT3 phosphorylation and c-Myc expression.

Curr Issues Mol Biol. 2024 Mar 14;46(3):2468-2479.

BC3 cells

1 µM or 2 µM

48 hours

Curr Issues Mol Biol. 2024 Mar 14;46(3):2468-2479.

Valemetostat 动物实验

Species SCIDbg mice	Animal Model MCL patient-derived xenograft model	Administration	Dosage	Frequency	Description	References
SCIDbg mice	MCL patient-derived xenograft model	Oral	200 mg/kg	Twice daily for 3 weeks	OR-S1 significantly inhibited MCL tumor growth, whereas ibrutinib did not.	Cancer Sci. 2021 Jun;112(6):2314-2324

Species

SCIDbg mice

Animal Model

MCL patient-derived xenograft model

Administration

Dosage

Frequency

Description

References

SCIDbg mice

MCL patient-derived xenograft model

Oral

200 mg/kg

Twice daily for 3 weeks

OR-S1 significantly inhibited MCL tumor growth, whereas ibrutinib did not.

Cancer Sci. 2021 Jun;112(6):2314-2324

Valemetostat 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.20mL

10.25mL

2.05mL

1.02mL

20.49mL

4.10mL

2.05mL

Valemetostat 技术信息

CAS号	1809336-39-7
分子式	C₂₆H₃₄ClN₃O₄
分子量	488.02
SMILES Code	O=C(C1=CC(Cl)=C(O[C@](C)([C@H]2CC[C@H](N(C)C)CC2)O3)C3=C1C)NCC4=C(C)C=C(C)NC4=O
MDL No.	MFCD31692361

别名	DS-3201; (R)-OR-S2; DS-3201b
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 75 mg/mL(153.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

Valemetostat {[allProObj[0].p_purity_real_show]}

Valemetostat 纯度/质量文件产品仅供科研

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Valemetostat 质控信息

Valemetostat 生物活性

Valemetostat 细胞实验

Valemetostat 动物实验

Valemetostat 实验方案

Valemetostat 技术信息

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Valemetostat 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Valemetostat 质控信息

Valemetostat 生物活性

Valemetostat 细胞实验

Valemetostat 动物实验

Valemetostat 实验方案

Valemetostat 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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