| Identification | Back Directory | [Name]
NI-57 | [CAS]
1883548-89-7 | [Synonyms]
CS-2795
NI57;NI 57
BRPF inhibitor NI57
Benzenesulfonamide, 4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C19H17N3O4S | [MOL File]
1883548-89-7.mol | [Molecular Weight]
383.42 |
| Chemical Properties | Back Directory | [Boiling point ]
580.1±60.0 °C(Predicted) | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≤25mg/ml in DMSO;30mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
7.89±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators. BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system. NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry. It is selective for BRPFs over other bromodomains. NI-57 shows accelerated FRAP recovery at 1 μM in the BRPF2 FRAP assay, preventing binding of full-length BRPF2 to chromatin. See the Structural Genomics Consortium (SGC) website for more information. | [Uses]
The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators. BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system. | [in vivo]
NI-57 has favorable oral bioavailability in mice[1]. | [storage]
Store at -20°C | [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. |
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Twochem Co.Ltd.
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021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
Energy Chemical
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400-0056266 |
| Website: |
www.energy-chemical.com |
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cjbscvictory
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13348960310 13348960310 |
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www.weikeqi-biotech.com/ |
| Company Name: |
InvivoChem
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13549236410 |
| Website: |
https://www.invivochem.cn/ |
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