PBIT | 2-p-tolyl-1,2-Benzisothiazolin-3-one | JARID1B Inhibitor

PBIT {[allProObj[0].p_purity_real_show]}

货号：A626958

PBIT是一种特异性抑制Jumonji AT-rich Interactive Domain 1 (JARID1)酶的抑制剂。PBIT通过约3 μM的IC50值抑制JARID1B（KDM5B或PLU1）组蛋白去甲基化酶。PBIT还抑制JARID1A和JARID1C，IC50分别为6 μM和4.9 μM。

PBIT 化学结构
CAS号：2514-30-9

PBIT 3D分子结构
CAS号：2514-30-9

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PBIT 纯度/质量文件产品仅供科研

货号：A626958 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

PBIT 质控信息

组蛋白去甲基酶亚型比较

产品名称	KDM1 ↓ ↑	KDM2 ↓ ↑	KDM3 ↓ ↑	KDM4 ↓ ↑	KDM5 ↓ ↑	KDM6 ↓ ↑	纯度
OG-L002	+++ LSD1, IC50: 20 nM						99%+
ORY-1001	+++ LSD1, IC50: 20 nM						98%
SP-2509	++++ LSD1, IC50: 13 nM						98+%
GSK2879552 2HCl	+ LSD1, Ki: 1.7 μM						99%+
T-3775440 HCl	++++ LSD1, IC50: 2.1 nM						99%
GSK-LSD1 2HCl	+++ LSD1, IC50: 16 nM						98%
Pulrodemstat benzenesulfonate	✔						99%+
IOX1		+ KDM2A, IC50: 1.8 μM	+++ KDM3A, IC50: 0.1 μM	++ KDM4E, IC50: 2.3 μM KDM4C, IC50: 0.6 μM	+ KDM5C, IC50: 19 μM	+ KDM6B, IC50: 1.6 μM	99%
PFI-90			✔				99%+
ML324				+ JMJD2, IC50: 920 nM			99%+
NCGC00244536				++++ KDM4, IC50: 10 nM			99%
KDM4D-IN-1				++ KDM4D, IC50: 0.41 μM			99%+
GSK467					++++ KDM5B, Ki: 10 nM		99%
GSK-J1						+++ JMJD3, IC50: 60 nM	99%+
(Z)-JIB-04				++ JMJD2E, IC50: 340 nM JMJD2A, IC50: 1100 nM	++ JARID1A, IC50: 230 nM	++ JMJD3, IC50: 855 nM	97%
CPI-455					++++ KDM5A, IC50: 10 nM	++++ KDM5, IC50: 10 nM	98%
JIB-04				++ JMJD2E, IC50: 435 nM JMJD2D, IC50: 290 nM	++ JARID1A, IC50: 230 nM	++ JMJD3, IC50: 855 nM	98%
GSK-J4 HCl						+++ JMJD3, IC50: 60 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

PBIT 生物活性

描述

PBIT is a specific inhibitor of JARID1. It inhibits the histone demethylase activity of JARID1B (also known as KDM5B or PLU1), with an IC50 of approximately 3 μM. PBIT also inhibits JARID1A and JARID1C, with IC50 values of 6 μM and 4.9 μM, respectively. PBIT suppresses the proliferation of cells expressing high levels of JARID1B. The inhibition of cell proliferation by PBIT is dependent on the level of JARID1B, specifically at concentrations of 1-10 μM in UACC-812 cells and 2.5-10 μM in MCF7 and MCF10A cells over a period of 72 hours^[1].

PBIT 细胞实验

Cell Line HeLa cells RWPE-1 cells LNCaP-MDV3100 cells PC-3 cells C4–2B cells LNCaP cells UACC-812 cells MCF7 cells	Concentration	Treated Time	Description	References
HeLa cells	10 or 30 µM	24 hours	PBIT treatment prevented the JARID1B overexpression-induced decrease of H3K4me3.	J Biol Chem. 2013 Mar 29;288(13):9408-17
RWPE-1 cells	1–20 µM	72 hours	To assess the effect of PBIT on the proliferation of RWPE-1 cells, results showed that PBIT significantly decreased the viability of RWPE-1 cells.	Exp Cell Res. 2024 Apr 1;437(1):113991
LNCaP-MDV3100 cells	1–20 µM	72 hours	To assess the effect of PBIT on the proliferation of LNCaP-MDV3100 cells, results showed that PBIT significantly decreased the viability of LNCaP-MDV3100 cells.	Exp Cell Res. 2024 Apr 1;437(1):113991
PC-3 cells	1–20 µM	72 hours	To assess the effect of PBIT on the proliferation of PC-3 cells, results showed that PBIT significantly decreased the viability of PC-3 cells.	Exp Cell Res. 2024 Apr 1;437(1):113991
C4–2B cells	1–20 µM	72 hours	To assess the effect of PBIT on the proliferation of C4–2B cells, results showed that PBIT significantly decreased the viability of C4–2B cells.	Exp Cell Res. 2024 Apr 1;437(1):113991
LNCaP cells	1–20 µM	72 hours	To assess the effect of PBIT on the proliferation of LNCaP cells, results showed that PBIT significantly decreased the viability of LNCaP cells.	Exp Cell Res. 2024 Apr 1;437(1):113991
UACC-812 cells	10 µM	72 hours	PBIT treatment significantly inhibited the proliferation of UACC-812 cells.	J Biol Chem. 2013 Mar 29;288(13):9408-17
MCF7 cells	10 µM	72 hours	PBIT treatment significantly increased global levels of H3K4me3.	J Biol Chem. 2013 Mar 29;288(13):9408-17

Cell Line

HeLa cells RWPE-1 cells LNCaP-MDV3100 cells PC-3 cells C4–2B cells LNCaP cells UACC-812 cells MCF7 cells

Concentration

Treated Time

Description

References

HeLa cells

10 or 30 µM

24 hours

PBIT treatment prevented the JARID1B overexpression-induced decrease of H3K4me3.

J Biol Chem. 2013 Mar 29;288(13):9408-17

RWPE-1 cells

1–20 µM

72 hours

To assess the effect of PBIT on the proliferation of RWPE-1 cells, results showed that PBIT significantly decreased the viability of RWPE-1 cells.