| Bioactivity | OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) [1]. |
| Invitro | OTUB2-IN-1 (0-40 μM; 2 h) 能够以剂量依赖性方式降低肿瘤细胞 (NCI-H358，SK-MES-1和 NCI-H226) 中的 PD-L1 水平，但是它不能影响 OTUB2 的稳定性[1]。OTUB2-IN-1 (0-50 μM; 1 h) 不干扰 OTUB2 和 PD-L1 之间的蛋白质相互作用[1]。OTUB2-IN-1 (10 μM; 0-4 d) 对 B16-F10 肿瘤细胞的活力没有明显的抑制作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> OTUB2-IN-1 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | OTUB2-IN-1 (20 mg/kg; i.p.; 每天一次持续五天), 在植入 B16-F10细胞的小鼠中，提示其具有增强肿瘤细胞免疫识别和免疫应答的潜能[1]。OTUB2-IN-1 （20 mg/kg; i.p.; 每天一次持续五天） 在植入 LL/2 细胞的小鼠中,降低 YAP 和磷酸化的 p65 的表达; 在植入 B16-F10 细胞的小鼠中降低了磷酸化 Akt 的表达； 在植入 KLN205 细胞的小鼠中中降低了磷酸化 p65 的表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C19H18N2O6S2 |
| Molar Mass | 434.49 |
| 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]. Ren W et al. Pharmaceutical targeting of OTUB2 sensitizes tumors to cytotoxic T cells via degradation of PD-L1. Nat Commun. 2024 Jan 2;15(1):9. |