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PBIT

Chemical Structure : PBIT

CAS No.:

PBIT (KDM5 inhibitor PBIT)

货号: PC-21987Not For Human Use, Lab Use Only.

PBIT is a specific small molecule inhibitor of JARID1 family of histone lysine demethylases (KDM5) with IC50 of 3 uM for JARID1B (KDM5B or PLU1), inhibits H3K4me3 demethylation in vitro and in vivo.

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

生物&药学活性

PBIT is a specific small molecule inhibitor of JARID1 family of histone lysine demethylases (KDM5) with IC50 of 3 uM for JARID1B (KDM5B or PLU1), inhibits H3K4me3 demethylation in vitro and in vivo.
PBIT inhibits removal of H3K4me3 by JARID1B in cells.
PBIT nhibits proliferation of cells expressing higher levels of JARID1B.
PBIT also inhibit other members of the JARID1 family, does not inhibit the H3K27me3 demethylases ubiquitously transcribed tetratricopeptide repeat protein, X-linked (UTX) or JmjC domain-containing protein 3 (JMJD3).
PBIT is also a potent inhibitor of JARID1A and JARID1C, with IC50 values of 6 and 4.9 μm, respectively.
PBIT is able to modulate H3K4me3 levels in cells and attenuate proliferation of UACC-812 breast cancer cells.

物理化学性质&存储条件

分子量 241.31
分子式 C14H11NOS
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-(p-Tolyl)benzo[d]isothiazol-3(2H)-one

参考文献

1. Sayegh J, et al. J Biol Chem. 2013 Mar 29;288(13):9408-17.

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