CAS NO: | 1883548-89-7 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 383.4 |
Cas No. | 1883548-89-7 |
Formula | C19H17N3O4S |
Solubility | ≤25mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | 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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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.