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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-NSD1 inhibitor BT5
NSD1 inhibitor BT5

Chemical Structure : NSD1 inhibitor BT5

CAS No.: 2351225-46-0

NSD1 inhibitor BT5 (BT5)

货号: PC-72299Not For Human Use, Lab Use Only.

NSD1 inhibitor BT5 is a covalent, small molecule inhibitor of NSD1 histone methyltransferase with IC50 of 1.4 uM, shows no covalent binding to NSD2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NSD1 inhibitor BT5 is a covalent, small molecule inhibitor of NSD1 histone methyltransferase with IC50 of 1.4 uM, shows no covalent binding to NSD2.
BT5 displays liitle to no affinity against selected epigenetic enzymes, including 10 HDACs, 4 sirtuins and 6 HATs revealed no significant activity of BT5 at 50 uM.
BT5 demonstrates on-target activity in cells and blocks proliferation of NUP98-NSD1 cells with GI50 of 0.8-1.3 uM, human leukemia cell lines (K562, MOLM13 and SET2) with GI 50 of 6 uM.
BT5 inhibits NSD1 SET domain and impairs the activity of NUP98-NSD1 in leukemia cells, reduces the H3K36me2 level but not H3K36me3.
BT5 impairs colony formation in NUP98-NSD1 patient sample MLL-ENL translocation, reduces HOXA9 and MEIS1 expression, without cytotoxicity on normal CD34+ bone marrow progenitor cells.

物理化学性质&存储条件

分子量 221.278
分子式 C10H11N3OS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-amino-6-(2-methylaziridin-1-yl)-1,3-benzothiazol-4-ol

参考文献

1. Huang H, et al. Nat Chem Biol. 2020 Dec;16(12):1403-1410.

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