5.05299
Histone Lysine Demethylase Inhibitor IX, PBIT
Synonym(s):
Histone Lysine Demethylase Inhibitor IX, PBIT, 2-(4-Methylphenyl)-1,2-benzisothiazol-3(2H)-one, JHDM Inhibitor V
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About This Item
Empirical Formula (Hill Notation):
C14H11NOS
CAS Number:
Molecular Weight:
241.31
UNSPSC Code:
12352200
Assay:
≥99% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥99% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
A cell-permeable iron chelating benzisothiazolone compound with microbicide and fungicide properties that acts as a potent, selective, and reversible inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases (IC50 = 3 µM for JARID1B). Also blocks the activity of other related demethylases at higher concentration (IC50 = 6, 4.9, and 28 µM for JARID1A, JARID1C, and JMJD2E, respectively). However, it does affect the activity of unrelated UTX and JMJD3 H3K27me3 demethylases. HeLa cells overexpressing full length JARID1B show a significant reduction in H3K4Me3 activity following PBIT treatment (~10 µM). Blocks the proliferation of UACC-812 tumor cells expressing higher levels of JARDID1B, but does not significantly affect MCF7 or MCF10A cells expressing lower levels of JARDID1B.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
JARID1 Histone Demethylases
JARID1 Histone Demethylases
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Use only fresh DMSO for reconstitution.
Other Notes
Sayegh, J., et al. 2013. J. Biol. Chem.288, 9408.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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