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

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.

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NVS-CECR2-1 Chemical Structure

NVS-CECR2-1 Chemical Structure

CAS No. : 1992047-61-6

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Customer Review

Based on 1 publication(s) in Google Scholar

NVS-CECR2-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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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].

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

NVS-CECR2-1 Related Antibodies

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.
Appearance

Solid

Color

White to off-white

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)

Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (134.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0174 mL 10.0872 mL 20.1743 mL
5 mM 0.4035 mL 2.0174 mL 4.0349 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.40%

SDS (252 KB)

COA (252 KB) HNMR (445 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0174 mL 10.0872 mL 20.1743 mL 50.4358 mL
5 mM 0.4035 mL 2.0174 mL 4.0349 mL 10.0872 mL
10 mM 0.2017 mL 1.0087 mL 2.0174 mL 5.0436 mL
15 mM 0.1345 mL 0.6725 mL 1.3450 mL 3.3624 mL
20 mM 0.1009 mL 0.5044 mL 1.0087 mL 2.5218 mL
25 mM 0.0807 mL 0.4035 mL 0.8070 mL 2.0174 mL
30 mM 0.0672 mL 0.3362 mL 0.6725 mL 1.6812 mL
40 mM 0.0504 mL 0.2522 mL 0.5044 mL 1.2609 mL
50 mM 0.0403 mL 0.2017 mL 0.4035 mL 1.0087 mL
60 mM 0.0336 mL 0.1681 mL 0.3362 mL 0.8406 mL
80 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6304 mL
100 mM 0.0202 mL 0.1009 mL 0.2017 mL 0.5044 mL
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NVS-CECR2-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NVS-CECR2-11992047-61-6Epigenetic Reader DomainApoptosisnon-BETBromodomainBRDcateyesyndromechromosomeregioncandidateSW48HT29HCT116H460SV-HUC-1HeLaU2OSHEK293Inhibitorinhibitorinhibit

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