1. Epigenetics
    Apoptosis
  2. Epigenetic Reader Domain
    Apoptosis
  3. NVS-CECR2-1

NVS-CECR2-1 

目录号: HY-110374 纯度: >99.0%
产品使用指南

NVS-CECR2-1 是一种非 BET 家族的 Bromodomain (BRD) 抑制剂,是一种有效的,选择性的猫眼综合征染色体区域候选物 2 (CECR2) 抑制剂。NVS-CECR2-1 以高亲和力结合 CECR2 BRD (IC50=47 nM; KD=80 nM)。NVS-CECR2-1 表现出癌细胞毒性作用,并通过靶向 CECR2 以及非 CECR2 依赖性机制诱导癌细胞的凋亡。

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NVS-CECR2-1 Chemical Structure

NVS-CECR2-1 Chemical Structure

CAS No. : 1992047-61-6

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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[1].

IC50 & Target[1]

CECR2

47 nM (IC50)

CECR2

80 nM (Kd)

BRD4

>37 μM (IC50)

BRD7

5.5 μM (IC50)

BRD9

2.3 μM (IC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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.
Molecular Weight

495.68

Formula

C₂₇H₃₇N₅O₂S

CAS No.

1992047-61-6

SMILES

CC1(C)CC(N2C=CC3=C2C=CC(C4=CC(NC5CC5)=NC(S(=O)(CCC)=O)=N4)=C3)CC(C)(C)N1

Shipping

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)

References

Purity: >99.0%

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Keywords:

NVS-CECR2-1Epigenetic Reader DomainApoptosisnon-BETBromodomainBRDcateyesyndromechromosomeregioncandidateSW48HT29HCT116H460SV-HUC-1HeLaU2OSHEK293Inhibitorinhibitorinhibit

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