| Bioactivity | GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer[1]. |
| Target | Ki: 11.97 nM (BRD3 BD1); 2.35 nM (BRD3 BD2) .IC50: 6.31 nM (MV4-11 cell); 95.2 nM (MM.1 S cell) . |
| Invitro | GXF-111 (Compound 24) 对 BRD3 BD1 和 BRD3 BD2 具有结合亲和力，Ki 值分别为 11.97 nM 和 2.35 nM[1]。GXF-111 在 MV4-11 和 MM.1 S 细胞系中具有细胞活性，IC50 值分别为 6.31 nM 和 95.2 nM[1]。GXF-111 (2, 10 nM; 24 h) 对 MM.1 S 细胞中 BET 家族蛋白的降解具有有效的细胞生长抑制活性[1]。GXF-111 (4 days) 在 7 种人类癌细胞系中具有抗增殖活性，IC50 值范围为 6.31 nM 至 17.25 μM[1]。 Western Blot Analysis[1] Cell Line: |
| Name | GXF-111 |
| Formula | C42H42ClN7O3 |
| Molar Mass | 728.28 |
| 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]. Yan Z, et al. Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines. Eur J Med Chem. 2023;254:115381. |