NVS-CECR2-1

• CAT Number: I011288
• CAS Number: 1992047-61-6
• Molecular Formula: C27H37N5O2S
• Molecular Weight: 495.68
• Purity: ≥95%
• Synonyms: N-cyclopropyl-2-propylsulfonyl-6-[1-(2,2,6,6-tetramethylpiperidin-4-yl)indol-5-yl]pyrimidin-4-amine
• InChI: InChI=1S/C27H37N5O2S/c1-6-13-35(33,34)25-29-22(15-24(30-25)28-20-8-9-20)18-7-10-23-19(14-18)11-12-32(23)21-16-26(2,3)31-27(4,5)17-21/h7,10-12,14-15,20-21,31H,6,8-9,13,16-17H2,1-5H3,(H,28,29,30)
• InChIKey: XVECNLUKQDKOST-UHFFFAOYSA-N
• SMILES: CCCS(=O)(=O)C1=NC(=CC(=N1)NC2CC2)C3=CC4=C(C=C3)N(C=C4)C5CC(NC(C5)(C)C)(C)C

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].
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].

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.
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