PeptideDB

NVS-CECR2-1

CAS: 1992047-61-6 F: C27H37N5O2S W: 495.68

NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region,
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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.