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PBIT

Catalog No.
C3584
JARID1 family demethylases inhibitor
Grouped product items
SizePriceStock Qty
5mg
$97.00
Ship with 5-10 days
10mg
$173.00
Ship with 5-10 days
25mg
$383.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 6, 3, 4.9, and 28 μM for JARID1A, JARID1B, JARID1C, and JARID1D, respectively

PBIT is a JARID1 family demethylases inhibitor.

JARID1B (also known as KDM5B or PLU1), a member of the JARID1 family of histone lysine demethylases, is identified for the demethylation of trimethylated lysine 27 in histone H3 that is a mark for actively transcribed genes. JARID1B is overexpressed in several cancers, such as prostate cancer, breast cancer, and lung cancer. Additionally, JARID1B is reported for mammary tumor formation in syngeneic or xenograft mouse models and JARID1B-expressing melanoma cells are related with increased self-renewal character.

In vitro: In previous study, PBIT was identified as JmjC histone demethylase inhibitor, which inhibited JARID1B with an in vitro IC50 of about 3 μM. Consistent with its inhibitory effect on JARID1B, PBIT treatment was able to inhibit the removal of H3K4me3 by JARID1B in cells. In addition, PBIT could inhibit the proliferation of cells expressing higher levels of JARID1B. These results suggested that PBIT could be regarded as a lead compound that could be further optimized for cancer therapy [1].

In vivo: Currently, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] J.  Sayegh, J. Cao, M. R. Zou, et al. Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. The Journal of Biological Chemisty 288(13), 9408-9417 (2013).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt241.3
Cas No.2514-30-9
FormulaC14H11NOS
Synonyms2-​p-​tolyl-1,​2-​Benzisothiazolin-​3-​one
Solubility≤1mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical Name2-​(4-​methylphenyl)​-1,​2-benzisothiazol-​3(2H)​-​one
SDFDownload SDF
Canonical SMILESO=C1C2=CC=CC=C2SN1C3=CC=C(C)C=C3
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

PBIT