NVS-CECR2-1

SKU: orb2900996

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.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1992047-61-6
• MW: 495.68
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₇N₅O₂S
• SMILES: O=S(=O)(C1=NC(=CC(=N1)C2=CC=C3C(C=CN3C4CC(NC(C)(C)C4)(C)C)=C2)NC5CC5)CCC
• Target: Apoptosis
• Solubility: In Vitro: DMSO : 66.67 mg/mL (134.50 mM; Ultrasonic )

Bioactivity

• In Vitro:
  Cell Viability Assay Cell line: Colon (SW48, HT29 and HCT116), lung (H460), uroepithelium (SV-HUC-1), cervix (HeLa) and bone (U2OS), human embryonic kidney (HEK) 293 T cells. Concentration: 1, 1.5, 2, 2.5, 3, 4 μM Incubation time: 72 hours. Result: Decreased the viability of all cancer cells analyzed in a dose dependent manner. Showed a dose-dependent cytotoxicity on HEK 293 T cells. Apoptosis Analysis Cell line: SW48 cells. Concentration: 0.5, 1, 1.5, 2, 4, 6 μM Incubation time: 72 hours. Result: Increased apoptosis in a dose-dependent manner, with more than 80% cells undergoing apoptosis at 6 μM, and had virtually no effect on necrosis.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Apoptosis