2. Epigenetics
  3. Epigenetic Reader Domain
  4. NI-57

NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF) famlily of proteins, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively.

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NI-57 Chemical Structure

NI-57 Chemical Structure

CAS No. : 1883548-89-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 In-stock
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10 mM * 1 mL in DMSO USD 110 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 170 In-stock
25 mg USD 350 In-stock
50 mg USD 550 In-stock
100 mg USD 950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

NI-57 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF) famlily of proteins, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively.

IC50 & Target

IC50: 3.1 nM (BRPF1), 46 nM (BRPF2 (BRD1)), 140 nM (BRPF3)[1]
Cellular Effect
Cell Line Type Value Description References
DMS-114 GI50
14.7 μM
Compound: 16; Nl-57
Inhibition of cell proliferation of human DMS114 cells after 72 hrs by MTS assay
Inhibition of cell proliferation of human DMS114 cells after 72 hrs by MTS assay
[PMID: 28714688]
NCI-H1703 GI50
10.4 μM
Compound: 16; Nl-57
Inhibition of cell proliferation of human NCI-H1703 cells after 72 hrs by MTS assay
Inhibition of cell proliferation of human NCI-H1703 cells after 72 hrs by MTS assay
[PMID: 28714688]
In Vitro

NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF), with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively. NI-57 binds the BRD of BRPF1 with a Kd of 31 ± 2 nM, BRD1 with a Kd of 110 ± 13 nM, and BRPF3 with a Kd of 410 ± 47 nM, whereas binding to BRD9 is weaker (Kd 1000 ± 130 nM) measured by isothermal titration calorimetry. NI-57 shows less active effect on BRD9 (IC50, 520 nM) and BRD4 (BD1) (IC50, 3700 nM), TRIM24 (IC50, 1600 nM). NI-57 also inhibits BRPF BRDs in the nucleus, but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4 μM (NCI-H1703 cells), 14.7 μM (DMS114), 15.6 μM (HRA-19), and 16.6 μM (RERF-LC-Sq1). Furthermore, Inhibition on BRPF1 of NI-57 (10 μM) reduces the gene expression of CCL-22 by 27.7 ± 9.4%[1].

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

NI-57 Related Antibodies
In Vivo

NI-57 has favorable oral bioavailability in mice[1].

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

383.42

Formula

C19H17N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(C#N)=CC=C1S(NC2=CC3=C(C=C2)N(C)C(C(C)=C3)=O)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (260.81 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 2.6081 mL 13.0405 mL 26.0811 mL
5 mM 0.5216 mL 2.6081 mL 5.2162 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.52 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.52 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).
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
References
Kinase Assay
[1]

All reagents are diluted in the recommended buffer (50 mMHEPES, 100 mM NaCl, 0.1% BSA; pH = 7.4) supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature prior to addition to plates. 4 mL of HIS-tagged protein is added to low-volume 384-well plates, followed by 4 mL of either buffer, non-biotinylated peptide, solvent or compounds (NI-57, etc.). Plates are sealed and incubated at room temperature for 30 minutes, before the addition of 4 mL biotinylated peptide, resealing and incubation for a further 30 minutes. 4 mL of streptavidin-coated donor beads (25 µg/mL) and 4 µL of nickel chelate acceptor beads (25 µg/mL) are then added under low light conditions. Plates are foil sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader using an AlphaScreenTM 680 excitation/570 emission filter set. IC50s are calculated in GraphPad Prism 5. Results for compounds (NI-57, etc.) dissolved in DMSO are normalised against corresponding DMSO controls prior to IC50 determination, which are given as the final concentration of compound in the 20 µL reaction volume[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6081 mL 13.0405 mL 26.0811 mL 65.2026 mL
5 mM 0.5216 mL 2.6081 mL 5.2162 mL 13.0405 mL
10 mM 0.2608 mL 1.3041 mL 2.6081 mL 6.5203 mL
15 mM 0.1739 mL 0.8694 mL 1.7387 mL 4.3468 mL
20 mM 0.1304 mL 0.6520 mL 1.3041 mL 3.2601 mL
25 mM 0.1043 mL 0.5216 mL 1.0432 mL 2.6081 mL
30 mM 0.0869 mL 0.4347 mL 0.8694 mL 2.1734 mL
40 mM 0.0652 mL 0.3260 mL 0.6520 mL 1.6301 mL
50 mM 0.0522 mL 0.2608 mL 0.5216 mL 1.3041 mL
60 mM 0.0435 mL 0.2173 mL 0.4347 mL 1.0867 mL
80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8150 mL
100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6520 mL
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NI-57 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:

NI-571883548-89-7NI57NI 57Epigenetic Reader DomainInhibitorinhibitorinhibit

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