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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:
2514-30-9
Molecular Weight:
241.31
UNSPSC Code:
12352200
Assay:
≥99% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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assay

≥99% (HPLC)

Quality Segment

100

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
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

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

5052990001: + 5052990002:

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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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