RBN012759
规格
| Cas Number | 2360851-29-0 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 76 mg/mL (200.81 mM); Ethanol: 5 mg/mL (13.21 mM); Water: Insoluble; |
| 简短描述 | PARP抑制剂 |
| 英文简短描述 | PARP Inhibitors |
| 过滤标签 | 表观遗传学,PARP,Cell Cycle/DNA Damage |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | RBN012759 是一种强效的 PARP14 选择性抑制剂，对人催化结构域和小鼠催化结构域的 IC50 分别为 <3 nM 和 5 nM。RBN012759 有助于抗肿瘤免疫反应。 |
| 英文描述 |
Information RBN012759 RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response. Targets human PARP14 (Cell-free assay); mouse PARP14 (Cell-free assay) <3 nM; 5 nM In vitro RBN012759 is a sufficiently soluble, highly permeable, low efflux and potent inhibitor of human and mouse PARP14 with high PARP family selectivity. RBN012759 treatment of human primary macrophages decreases the MAR/PAR signal corresponding to PARP14 self-MARylation and stabilizes PARP14 protein in a dose-dependent manner. Treatment of primary human macrophages with RBN012759 leads to decreased IL-4 driven M2-like gene expression, suggesting that PARP14 inhibition results in a less immunosuppressive phenotype. In vivo RBN012759 has moderate clearance and oral bioavailability in mice. RBN012759 is well-tolerated in mice with repeat dosing up to 500 mg/kg BID (75-fold coverage of the PARP14 mouse). |