上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
L-Moses dihydrochloride (Synonyms: L-45 dihydrochloride)
L-Moses (L-45) dihydrochloride 是第一个有效的选择性 p300/CBP 相关因子 (PCAF) 溴结构域 (Brd) 抑制剂,Kd 为 126 nM。
L-Moses dihydrochloride Chemical Structure
规格 | 价格 | 是否有货 | |
---|---|---|---|
5 mg | ¥5200 | 询问价格 & 货期 | |
10 mg | ¥8400 | 询问价格 & 货期 |
* Please select Quantity before adding items.
生物活性 |
L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM[1]. |
|
---|---|---|
IC50 & Target[1] |
|
|
体外研究 (In Vitro) |
L-Moses (L-45) disrupts PCAF-Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co-crystal structure of L-Moses with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. A structure using highly homologous (64 % identity) Brd from Plasmodium falciparum, PfGCN5, of which L-Moses is also a potent ligand (isothermal titration calorimetry (ITC) KD 280 nM), is successfully obtained (PDB: 5TPX). L-Moses binds in the acetylated lysines (KAc) -binding pocket of PfGCN (blue ribbon and sticks) and makes H-bonds (dotted lines) through the triazole to N1436 and the first of a network of four water molecules (red spheres)[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
|
体内研究 (In Vivo) |
L-Moses (L-45) shows no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell-permeability, and metabolic stability in human and mouse liver microsomes, supporting its potential for in vivo use[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
|
分子量 |
433.38 |
|
Formula |
C21H26Cl2N6 |
|
运输条件 |
Room temperature in continental US; may vary elsewhere. |
|
储存方式 |
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
|
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务