| Bioactivity | LY1 is a potent, selective and covalent inhibitor against both SARS-CoV-2 PLpro and Mpro with Kd values of 1.5 μM and 2.3 μM for Mpro C145A protein and PLpro C111A protein, respectively. LY1 potent against the viral proteases, with IC50s of 0.12 μM and 0.99 μM against Mpro and PLpro. LY1 shows high selectivity over other kinases, human proteases and metalloenzyme[1]. |
| Target | Kd: 1.5 μM (Mpro C145A protein) and 2.3 μM (PLpro C111A protein).IC50: 0.12 μM (Mpro protease) and 0.99 μM (PLpro protease). |
| Invitro | 在 SARS-CoV-2 感染的 Vero E6 细胞中，5 μM 的 LY1 导致病毒核蛋白 (NP) 水平显着降低 。使用 15 μM LY1 观察到病毒 RdRP RNA 水平降低 99.99%[1]。LY1 对组织蛋白酶 B 和组织蛋白酶 L 的 IC50 值分别为 8.8 μM 和 2.2 μM[1]。 |
| In Vivo | 在为期 8 周的毒性研究中，给大鼠口服高达 300 mg/kg 的 LY1，持续 4 周，然后再恢复 4 周； 在任何一组中都没有观察到体重和食物消耗的显着变化[1]。 |
| Name | LY1 |
| CAS | 2883813-32-7 |
| Formula | C20H19ClN4O3S |
| Molar Mass | 430.91 |
| 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]. Wenying Yu, et al. Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2. J Med Chem. 2022 Dec 22;65(24):16252-16267. |