Description
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.
Product information
CAS Number: 1992047-61-6
Molecular Weight: 495.68
Formula: C27H37N5O2S
Chemical Name: N-cyclopropyl-2-(propane-1-sulfonyl)-6-[1-(2,2,6,6-tetramethylpiperidin-4-yl)-1H-indol-5-yl]pyrimidin-4-amine
Smiles: CCCS(=O)(=O)C1=NC(=CC(NC2CC2)=N1)C1C=C2C=CN(C3CC(C)(C)NC(C)(C)C3)C2=CC=1
InChiKey: XVECNLUKQDKOST-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
NVS-CECR2-1 (1-4 μM; 72 hours) decreases the viability of all cancer cells. NVS-CECR2-1 (1-6 μM; 72 hours) increases apoptosis in a dose-dependent manner. 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. 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. NVS-CECR2-1 inhibits chromatin binding of CECR2 BRD and displaces CECR2 from chromatin within cells.
Products are for research use only. Not for human use.
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