| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G656242-1ml |
1ml |
期货  |
|
| 规格或纯度 | 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。 |
| 储存温度 | 充氩,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
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)) |
| 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 | 121373418 |
| 分子量 | 510.58 |
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