PBIT (2514-30-9) is a potent and selective inhibitor of JARID1 (IC50 = 3, 4.9 and 6 μM for JARID1B, 1A and 1C, respectively). The JARID1 (Jumonji AT-Rich Interactive Domain 1) family of lysine demethylases demethylates the trimethylated lysine 27 in histone H3 (H3K4me3). PBIT is selective for JARID1 over UTX and JMJD3. Treatment of cells with PBIT inhibits the demethylation of H3K4me3. It inhibits proliferation of breast cancer cell lines expressing high levels of JARID1B1. PBIT(2514-30-9)是一种有效的JARID1选择性抑制剂,对JARID1B、1A和1C的IC50分别为3、4.9和6 μM。 赖氨酸去甲基化酶的JARID1家族(Jumonji AT-Rich Interactive Domain 1)将组蛋白H3 (H3K4me3)中的三甲基化赖氨酸27去甲基化。 PBIT对于JARID1是选择性的,而不是UTX和JMJD3。 PBIT处理细胞可抑制H3K4me3的去甲基化。 它能抑制高水平JARID1B1表达的乳腺癌细胞系的增殖。
References/Citations:
1) Sayegh et al. (2013), Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen; J. Biol. Chem., 288 9408
CAS:
2514-30-9
Catalog Number:
10-1595
Activity:
JARID1 lysine demethylase inhibitor
Chemical Name:
2-(4-Methylphenyl)-1,2-benzisothiazol-3(2H)-one
Molecular Weight:
241.31
Molecular Formula:
C14H11NOS
Solubility:
Soluble in DMSO (up to 24 mg/ml) or in Ethanol (up to 5 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT
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