| Description | VPC-18005 is a luciferase inhibitor. VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain thereby disrupting the ERG binding to DNA. |
| In vitro | VPC-18005（1和10 μM）在斑马鱼模型中降低了20-30%癌细胞的扩散[1]。以5 µM浓度作用时，VPC-18005对PNT1B-ERG和VCaP细胞中的pETS-luc报告基因活性显示出IC50分别为3μM和6μM的抑制作用。VPC-18005能够拮抗ERG表达的前列腺细胞的转移潜能，并且在不显示明显细胞毒性的情况下抑制ERG报告基因活性。VPC-18005还能抑制体外ERG过表达细胞的迁移与侵袭能力[2]。 |
| molecular weight | 319.38 |
| Molecular formula | C15H17N3O3S |
| CAS | 2242480-48-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 60 mg/mL (187.86 mM), Sonication is recommended. |
| References | 1. Haneen Amawi, et al. The use of zebrafish model in prostate cancer therapeutic development and discovery. Cancer Chemother Pharmacol. 2021 Mar;87(3):311-325. 2. Miriam S Butler, et al. Discovery and characterization of small molecules targeting the DNA-binding ETS domain of ERG in prostate cancer. Oncotarget. 2017 Jun 27;8(26):42438-42454. |