Bioactivity | NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism[1]. |
Invitro | NVS-CECR2-1 (1-4 μM; 72 hours) decreases the viability of all cancer cells[1]. NVS-CECR2-1 (1-6 μM; 72 hours) increases apoptosis in a dose-dependent manner[1]. NVS-CECR2-1 (10 μM; 2 hours) inhibits chromatin binding of CECR2 BRD within SW48 cells. NVS-CECR2-1 (5, 10, 15 μM; 2 hours) dissociates CECR2 from chromatin in a dose-dependent manner without affecting BRG1[1]. NVS-CECR2-1 (0.5-4 μM; 10 days) inhibits the clonogenic ability of SW48 cells in a dose dependent manner and its IC50 value is estimated to be 0.64 μM[1]. NVS-CECR2-1 inhibits chromatin binding of CECR2 BRD and displaces CECR2 from chromatin within cells[1]. Cell Viability Assay[1] Cell Line: |
Name | NVS-CECR2-1 |
CAS | 1992047-61-6 |
Formula | C27H37N5O2S |
Molar Mass | 495.68 |
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]. Seul Gi Park, et al. Cytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells. Sci Rep. 2020 Oct 1;10(1):16330. |