NI-57
目录号 : GC16763
A BRPF bromodomain inhibitor
Cas No.:1883548-89-7
Sample solution is provided at 25 µL, 10mM.
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NI-57 is a potent inhibitor of the bromodomain of the BRPFs that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively [1].
The bromodomain and PHD finger-containing protein 1, 2, 3 (BRPF1/2/3) are scaffolding subunit of the MOZ/MORF histone acetyltransferase complexes that links together KAT6A/B, ING5 and hEAF6 in the tetrameric assembly. BRPF1 (BR140 or Peregrin) is important in the maintenance of expression levels of Hox genes and the development of axial skeleton, multiple tissues and the hematopoietic system [2][3].
NI-57 is a potent inhibitor of the bromodomain of the BRPFs and acts as a chemical probe for the bromodomains of the BRPF family of proteins (BRPF1/2/3). As determined by isothermal titration calorimetry, NI-57 binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively. As measured by both biophysical and biochemical methods, NI-57 exhibited selective against other non-Class IV bromodomains, including the BETs. In the BRPF2 FRAP assay, NI-57 at 1 μM prevented binding of full-length BRPF2 to chromatin [1].
References:
[1]. http://www.thesgc.org/chemical-probes/NI-57
[2]. Klein BJ, Lalonde ME, Cté J, et al. Crosstalk between epigenetic readers regulates the MOZ/MORF HAT complexes. Epigenetics. 2014 Feb;9(2):186-93.
[3]. Ullah M, Pelletier N, Xiao L, et al. Molecular architecture of quartet MOZ/MORF histone acetyltransferase complexes. Mol Cell Biol. 2008 Nov;28(22):6828-43.
Kinase experiment: | 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]. |
References: [1]. Igoe N, et al. Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins. J Med Chem. 2017 Aug 24;60(16):6998-7011. | |
| Cas No. | 1883548-89-7 | SDF | |
| 化学名 | 4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-benzenesulfonamide | ||
| Canonical SMILES | COC1=CC(C#N)=CC=C1S(NC2=CC=C(N(C)C(C(C)=C3)=O)C3=C2)(=O)=O | ||
| 分子式 | C19H17N3O4S | 分子量 | 383.4 |
| 溶解度 | ≤25mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet