计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
GNE-049
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
充氩,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
GNE-049 is a highly potent and selective CBP inhibitor with an IC 50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC 50 s of 12 nM and 4200 nM, respectively
In Vitro
GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement, GNE-049 is shown to inhibit the expression of MYC (MV4-11 cell line) with an EC 50 of 14 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GNE-049 demonstrates acceptable PK in mouse, rat, dog, and monkey. Determination of potency versus a selection of bromodomains revealed that GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1). GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. Adverse central nervous system (CNS)-related signs (e.g., marked hyperactivity and vocalization) are observed in several of the rats at the 250 mg/kg dose level. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in brain to unbound drug concentration in plasma (K p,uu ) 3 h post dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IC50: 1.1 nM (CBP), 12 nM (BRET), 4200 nM (BRD4(1))
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
GNE-049
生化机理
GNE-049 是一种强效、选择性 CBP 抑制剂，在 TR-FRET 试验中的 IC 50 为 1.1 nM。GNE-049 还能抑制 BRET 和 BRD4(1)，其 IC 50 s 分别为 12 nM 和 4200 nM。
储存条件
充氩,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(=O)N1CCC2=C(C1)C(=NN2C3CCOCC3)N4CCCC5=CC(=C(C=C54)C(F)F)C6=CN(N=C6)C
PubChem CID
分子量
510.58
技术文档
高级数据
关联靶点（人）
EP300
Tchem
组蛋白乙酰转移酶 p300(Histone acetyltransferase p300)
(1 活性数据)
CREBBP
Tchem
CREB结合蛋白(CREB-binding protein)
(3 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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