BRD7-IN-1是一种修饰的BI7273衍生物(BRD7/9抑制剂)，通过与VHL配体连接形成PROTACVZ185(VZ185抑制BRD7/9的DC50分别是4.5nM、1.8nM)。
| Cas No. | 2448414-48-8 |
| Canonical SMILES | CN1C=C(C2=CC(OC)=C(CN3CCNCC3)C(OC)=C2)C(C=CN=C4)=C4C1=O.Cl.Cl |
| 分子式 | C22H28Cl2N4O3 |
| 分子量 | 467.39 |
| 溶解度 | Soluble in DMSO |
| 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 | BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively)[1].
BRD7, BRD9[1] [1]. Zoppi V, et al. Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7. J Med Chem. 2019 Jan 24;62(2):699-726. |
