| Bioactivity | EBET-1055 is a bromodomain and extra-terminal (BET) protein degrader (EBET) composed of a BET inhibitor (EBET-590, HY-161387), an E3 ubiquitin ligase ligand and connectors. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures[1]. |
| Invitro | EBET-1055 (1 nM, 10 nM; 2 d) 在小鼠 CAF 与 PC-3 或 PC-42 癌细胞的共培养时，抑制 CAF 受诱导而出现的 IL-6 和 LIF 分泌[1]。EBET-1055 具有潜在抗炎或抗纤维化活性。STAT3 信号介导炎症性 CAF (iCAF) 表型，SMAD 信号介导肌成纤维细胞 CAF (myCAF) 表型；而 EBET-1055 (1-100 nM; 24 h) 可能抑制 BRD 蛋白与 STAT3 和 SMAD3 相互作用，抑制肌成纤维细胞分化，并降低小鼠纤维化肾中 SMAD3 和 STAT3 的磷酸化水平[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> EBET-1055 相关抗体: Western Blot Analysis[1] Cell Line: |
| Formula | C51H54N8O9 |
| Molar Mass | 923.02 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Nakazawa Y, et al. Delivery of a BET protein degrader via a CEACAM6-targeted antibody-drug conjugate inhibits tumour growth in pancreatic cancer models. Nat Commun. 2024 Mar 11;15(1):2192. |