| Bioactivity | CBP/p300 ligand 4 (Compound 4) is an orally active inhibitor for CBP/p300 bromodomain, with IC50 of 91.4 nM. CBP/p300 ligand 4 serves as a ligand for target protein XYD190 (HY-161495). XYD190 is a PROTAC degrader for CBP/p300[1]. |
| Target | IC50: 91.4 nM (CBP/p300 bromodomain) |
| Invitro | CBP/p300 ligand 4 (0-1 μM, 72-120 h) 通过降解 CBP，p300 和 c-Myc 蛋白，抑制 AML 细胞系 MV4;11，MOLM-13 和 MOLM-16 增殖，IC50 分别为 20.4，102 和 12.9 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CBP/p300 ligand 4 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | CBP/p300 ligand 4 (10 mg/kg，口服，每天一次共两周) 在 MV4;11 异种移植小鼠模型中表现出抗肿瘤活性，肿瘤生长抑制率 TGI 为 65%[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C30H31F2N5O4 |
| Molar Mass | 563.60 |
| 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]. Hu J, et al., Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity. J Med Chem. 2024 May 9;67(9):6952-6986. |