KDM5-IN-48 ( KDM5-IN-48 | KDM5 IN 48 | KDM5IN48 | KDM5 inhibitor-48 | KDM5 inhibitor 48 )

产品货号. M12424 CAS No. 1628210-26-3

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

产品询价大包装询价加入购物车

产品名称

KDM5-IN-48
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

一种有效的、选择性的、口服生物可利用的 KDM5 抑制剂，对 KDM5A、KDM5B 和 KDM5C 的生化 IC50 分别为 15.1、4.7 和 65.5 nM。
产品描述

A potent, selective and orally bioavailable KDM5 inhibitor with biochemical IC50 of 15.1, 4.7 and 65.5 nM for KDM5A, KDM5B and KDM5C, respectively; displays significantly less potent against other KDM enzymes (KDM4C IC50=1.9 uM); increases H3K4Me3 level in PC9 cells with EC50 of 0.34 uM; possesses suitable physiochemical properties and displays excellent PK profile in mice.
体外实验

KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A.
体内实验

When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo.
同义词

KDM5-IN-48 | KDM5 IN 48 | KDM5IN48 | KDM5 inhibitor-48 | KDM5 inhibitor 48
通路

Chromatin/Epigenetic
靶点

Histone Demethylase
受体

Histone Demethylase
研究领域

——
适应症

——

CAS Number

1628210-26-3
分子量

324.3803
分子式

C17H20N6O
纯度

>98% (HPLC)
溶解度

DMSO: ≥ 30 mg/mL
SMILES

N#CC1=C2NC(C3=CN(C(C)(C)C)N=C3)=C(C(C)C)C(N2N=C1)=O
化学全称

Pyrazolo[1,5-a]pyrimidine-3-carbonitrile, 5-[1-(1,1-dimethylethyl)-1H-pyrazol-4-yl]-4,7-dihydro-6-(1-methylethyl)-7-oxo-

1. Liang J, et al. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41.

计算器

产品手册

关联产品

P3FI-63

P3FI-63 is a selective KDM3B inhibitor (IC50: 7 μM) with antitumor activity for the study of fusion-positive rhabdomyosarcoma and other transcriptionally addictive cancers.
JIB-04

JIB-04 是一种泛选择性 Jumonji 组蛋白去甲基酶抑制剂。
E67-2

E67-2 是 H3K9 Jumonji 去甲基化酶 KIAA1718 (KDM7A) 的有效选择性抑制剂，IC50 为 3.4 uM。