For research use only. Not for therapeutic Use.
VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity[1].
VPC-18005 is found to inhibit pETS-luc reporter activity in PNT1B-ERG and VCaP cells with IC50 values of 3 and 6 μM, respectively[1].
VPC-18005 could suppress ERG reporter activity without exhibiting overt cytotoxicity[1].
VPC-18005 inhibits migration and invasion of ERG-overexpressing cells in vitro[1].
VPC-18005 can antagonize the metastatic potential of ERG-expressing prostate cells[1].
The exposure of larvae to 1 or 10 µM of VPC-18005 produced a 20–30% decrease in the dissemination of cancer cells in zebrafsh[2].
| Catalog Number | I045526 |
| CAS Number | 2242480-48-2 |
| Synonyms | 2-[(2Z)-4-oxo-2-[(Z)-(4-propan-2-ylphenyl)methylidenehydrazinylidene]-1,3-thiazolidin-5-yl]acetic acid |
| Molecular Formula | C15H17N3O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C15H17N3O3S/c1-9(2)11-5-3-10(4-6-11)8-16-18-15-17-14(21)12(22-15)7-13(19)20/h3-6,8-9,12H,7H2,1-2H3,(H,19,20)(H,17,18,21)/b16-8- |
| InChIKey | DTEAZCJUKPARQD-PXNMLYILSA-N |
| SMILES | CC(C)C1=CC=C(C=C1)C=NN=C2NC(=O)C(S2)CC(=O)O |
| Reference | [1]. 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. [2]. 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. |
