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  3. NI-57

NI-57 

Cat. No.: HY-19537 Purity: 99.89%
Handling Instructions

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.

For research use only. We do not sell to patients.

NI-57 Chemical Structure

NI-57 Chemical Structure

CAS No. : 1883548-89-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
25 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 680 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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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]

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].

In Vivo

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (217.26 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2608 mL 1.3041 mL 2.6081 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

383.42

Formula

C₁₉H₁₇N₃O₄S

CAS No.

1883548-89-7

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

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Product Name:
NI-57
Cat. No.:
HY-19537
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NI-57

Cat. No.: HY-19537