| Bioactivity | SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases[1]. |
| Invitro | SET2 (20 μM；24 小时) 消除表达 TRPV2 的 PC-3M 细胞的迁移[1]。SET2 (20 μM；24 小时) 抑制瞬时共转染 TRPV2 和 LPAR1 的 HEK293T 细胞中的 2-APB 诱发电流[1]。SET2 (20 μM；24 小时) 抑制 LPA (0.1 μM；3 分钟) 诱导的细胞质钙增加和 LPA 诱导的 PC-3M 细胞迁移[1]。 Cell Migration Assay [1] Cell Line: |
| Name | SET2 |
| CAS | 2313525-20-9 |
| Formula | C17H21F3N4O2S |
| Molar Mass | 402.43 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Chai H, et al. Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel. J Med Chem. 2019 Feb 14;62(3):1373-1384. |