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PBIT

Chemical Structure : PBIT

CAS No.:

PBIT (KDM5 inhibitor PBIT)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 241.31
Formula C14H11NOS
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(p-Tolyl)benzo[d]isothiazol-3(2H)-one

References

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

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