I-CBP112 (hydrochloride) 是 CBP/P300 的选择性抑制剂，可直接结合其溴结构域（Kds 分别为 142 和 625 nM）。 I-CBP112 在体外和体内以剂量依赖性方式显着降低 MLL-AF9(+) 急性髓细胞白血病细胞的白血病起始潜能。 I-CBP112 增加 BET 溴结构域抑制剂 JQ1 以及多柔比星的细胞毒活性。
| Cas No. | 2147701-33-3 |
| Canonical SMILES | COC1=C(OC)C=C(C2=CC(OC[C@H]3CCCN(C)C3)=C(OCCN(C(CC)=O)C4)C4=C2)C=C1.Cl |
| 分子式 | C27H36N2O5•HCl |
| 分子量 | 505.1 |
| 溶解度 | DMF: 16 mg/ml,DMSO: 16 mg/ml,Ethanol: 16 mg/ml,PBS (pH 7.2): 10 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | cAMP-responsive element-binding protein binding protein (CREBBP) and E1A-associated protein p300 (EP300) are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development. Both CBP and EP300 contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins. I-CBP112 is a selective inhibitor of CBP and EP300 that directly binds their bromodomains (Kds = 0.142 and 0.625 μM, respectively). Developed by the Structural Genomics Consortium (SGC), this compound shows only weak cross-reactivity with the bromodomains of bromodomain and extra-terminal proteins and shows no interaction with other bromodomains. |
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