| Bioactivity | LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model[1]. |
| Invitro | LLK203 (0-100 μM；36小时) 对 MCF-7 细胞具有高抑制活性 (IC50=3.4 μM)，比 ML364 (IC50=9.3 μM) 靶向性更强。与 ML364 (HY-100900) 相比，LLK203 对 USP2 的活性增加了 4 倍，USP8 活性增加了 9 倍[1]。LLK203 (10-50 μM；24 小时) 可增加 MCF-7 细胞凋亡细胞的比例，并大部分保持在 G1 期[1]。LLK203 (2-50 μM；24 小时) 可以以剂量依赖性方式降解各种蛋白质 (MDM2、Cyclin D1、Her2、ERα)[1]。LLK203 (2-50 μM；持续 7 天) 在 10 μM 浓度下表现出强大的抑制克隆形成的能力[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> LLK203 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | LLK203 (20 mg/kg；腹腔；每天；持续 23 天) 显着减少 4T1 荷瘤小鼠模型中的肿瘤生长[1]。Pharmacokinetic Parameters of LLK203 in male Sprague-Dawley rats[1]. |
| CAS | 2758090-62-7 |
| Formula | C28H23N3O4S3 |
| Molar Mass | 561.69 |
| 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]. Yucheng Tian, et al. The discovery of potent USP2/USP8 dual-target inhibitors for the treatment of breast cancer via structure guided optimization of ML364. European Journal of Medicinal Chemistry. Volume 268, 15 March 2024, 116275. |