| Bioactivity | LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575))[1]. |
| Invitro | 在 SEM 和 RPMI-8402 细胞中，LLC0424 剂量依赖性地抑制这两种细胞系的生长，IC50 值分别为 3.56 μM 和 0.56 μM[1]。LLC0424（0.001 μM-10 μM；1小时-24小时）以浓度和时间依赖性方式诱导 NSD2 降解，并以 CRBN 和蛋白酶体依赖性方式诱导 NSD2 降解。 LLC0424 还会导致 H3K36Me2 下调[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> LLC0424 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | LLC0424（60 mg/kg；静脉注射或腹腔注射；连续 5 天）在体内表现出强效的 NSD2 降解[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C45H41N7O9 |
| Molar Mass | 823.85 |
| 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]. Lianchao Liu, et al. Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader. J Med Chem. 2024 May 9;67(9):6938-6951. |