Bioactivity | PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673))[1]. |
Invitro | PROTAC XPO1 degrader-1 (Compound 2c) 在 MV4-11 急性髓系白血病 (AML) 细胞中能有效降解 XPO1 蛋白,其 DC50 为 23.67 nM[1]。PROTAC XPO1 degrader-1 具有显著的抗细胞增殖作用,对 MV4-11 和 MOLM-13 细胞的 IC50 值分别为 0.142 μM 和 0.186 μM[1]。PROTAC XPO1 degrader-1 (100-500 nM; 24 h) 通过 caspase 途径有效诱导 MV4-11 细胞凋亡[1]。PROTAC XPO1 degrader-1 (100-200 nM; 24 h) 可以将 MV4-11 细胞周期阻滞在 G1 期[1]。PROTAC XPO1 degrader-1 (50 nM; 24 h) 在 MV4-11 细胞中可降低细胞迁移[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PROTAC XPO1 degrader-1 相关抗体: Apoptosis Analysis[1] Cell Line: |
Formula | C33H35ClF3N7O7 |
Molar Mass | 734.12 |
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]. Chen G, et al. Discovery of novel XPO1 PROTAC degraders for the treatment of acute myeloid leukemia[J]. European Journal of Medicinal Chemistry, 2025, 283: 117182. |