LP99 是一种表观遗传探针，是一种有效的选择性 BRD7 和 BRD9 溴结构域抑制剂，对 BRD9 的 Kd 为 99 nM。
| Cas No. | 1808951-93-0 |
| 化学名 | N-[(2R,3S)-2-(4-chlorophenyl)-1-(1,2-dihydro-1,4-dimethyl-2-oxo-7-quinolinyl)-6-oxo-3-piperidinyl]-2-methyl-1-propanesulfonamide |
| Canonical SMILES | CC(C1=CC=C(N2C(CC[C@H](NS(CC(C)C)(=O)=O)[C@H]2C3=CC=C(Cl)C=C3)=O)C=C1N4C)=CC4=O |
| 分子式 | C26H30ClN3O4S |
| 分子量 | 516.1 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS (pH 7.2) (1:9): 0.1 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 | LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry. It is selective for BRD7/9 over a panel of 48 BRDs at concentrations up to 10 uM determined using differential scanning fluorimetry. It inhibits BRD7 interactions with histones H3.3 and H4 with IC50 values of 3.7 and 3.3 uM, respectively, in a bioluminescence resonance energy transfer (BRET) assay in HEK293 cells. Similarly, it inhibits BRD9 from interacting with H3.3 and H4 with IC50 values of 5.1 and 6.2 uM, respectively. It also decreases the level of IL-6 secreted from LPS-stimulated THP-1 cells. See the Structural Genomics Consortium (SGC) website for more information. |
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