| Bioactivity | WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC)[1]. |
| Target | IC50: 338.79 nM (LSD1).IC50: 14.81 nM (DCN1-UBC12 Protein-protein interaction). |
| Invitro | WS-384 (1-32 μM; 24-72 h) 以时间和剂量依赖方式抑制了 A549 和 H1975 细胞的生长，IC50 在 2.15-6.67 μM 之间，具有抗癌活性[1]。WS-384 (1-8 μM; 48 h) 在 A549 和 H1975 细胞中通过抑制 cullin 1 的类泛素化修饰和减少 CDKN1A 启动子处的 H3K4 去甲基化，来增加 p21 的基因和蛋白的表达水平，从而诱导细胞周期阻滞在 G2/M 期和细胞凋亡。WS-384 (1-8 μM; 48 h)也可以引起 DNA 损伤[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> WS-384 相关抗体: Apoptosis Analysis[1] Cell Line: |
| In Vivo | WS-384 (25-50 mg/kg; p.o.; Once daily for 36 consecutive days) 在 BALB/c 裸鼠异种移植模型中能有效抑制 NSCLC 肿瘤的生长，且毒性较低[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C18H21BrClN9S2 |
| Molar Mass | 542.91 |
| 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]. Li A, et al. Discovery of WS-384, a first-in-class dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor for the treatment of non-small cell lung cancer. Biomed Pharmacother. 2024;173:116240. |