NI-57 is a potent inhibitor of the bromodomains of BRPF proteins, which are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes. These complexes act as transcriptional regulators and are crucial for maintaining Hox gene expression and the development of various tissues, the axial skeleton, and the hematopoietic system. NI-57 selectively binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry.
1883548-89-7
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Basic information
- Product Name: NI-57
- 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-
- CAS NO:1883548-89-7
- Molecular Formula: C19H17N3O4S
- Molecular Weight: 383.42098
- EINECS: 604-604-1
- Product Categories: N/A
- Mol File: 1883548-89-7.mol
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Chemical Properties
- Melting Point: N/A
- Boiling Point: 580.1±60.0 °C(Predicted)
- Flash Point: N/A
- Appearance: /
- Density: 1.43±0.1 g/cm3(Predicted)
- Refractive Index: N/A
- Storage Temp.: N/A
- Solubility: ≤25mg/ml in DMSO;30mg/ml in dimethyl formamide
- PKA: 7.89±0.20(Predicted)
- CAS DataBase Reference: NI-57(CAS DataBase Reference)
- NIST Chemistry Reference: NI-57(1883548-89-7)
- EPA Substance Registry System: NI-57(1883548-89-7)
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Safety Data
- Hazard Codes: N/A
- Statements: N/A
- Safety Statements: N/A
- WGK Germany:
- RTECS:
- HazardClass: N/A
- PackingGroup: N/A
- Hazardous Substances Data: 1883548-89-7(Hazardous Substances Data)
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1883548-89-7 Usage
Uses
1. Used in Pharmaceutical Industry:NI-57 is used as a bromodomain inhibitor for targeting BRPF proteins, which play a significant role in gene expression and tissue development. By inhibiting these proteins, NI-57 can potentially be used in the development of therapies for various diseases and conditions related to the dysregulation of gene expression and tissue development.
2. Used in Research and Development:
NI-57 is used as a research tool for studying the role of BRPF proteins in gene regulation and their involvement in various biological processes. It can help researchers understand the molecular mechanisms underlying the function of these proteins and their potential as therapeutic targets.
3. Used in Drug Discovery and Development:
NI-57 is used as a lead compound in the development of new drugs targeting BRPF proteins. Its selective inhibition of these proteins can guide the design and synthesis of more potent and specific inhibitors, which may have improved therapeutic potential.
4. Used in Chromatin Biology:
NI-57 is used as a tool to study the role of BRPF proteins in chromatin biology, particularly in the context of their interaction with histone acetyltransferase complexes and their influence on gene expression.
5. Used in Epigenetics:
NI-57 is used to investigate the epigenetic mechanisms involving BRPF proteins, which can provide insights into the regulation of gene expression and the potential for targeted epigenetic therapies.
6. Used in Cancer Research:
NI-57 is used as a potential therapeutic agent in cancer research, as dysregulation of BRPF proteins may contribute to the development and progression of various types of cancer. Inhibiting these proteins could potentially help in the treatment of cancer by restoring normal gene expression patterns and cellular function.
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.Check Digit Verification of cas no
The CAS Registry Mumber 1883548-89-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,8,8,3,5,4 and 8 respectively; the second part has 2 digits, 8 and 9 respectively.Calculate Digit Verification of CAS Registry Number 1883548-89:
(9*1)+(8*8)+(7*8)+(6*3)+(5*5)+(4*4)+(3*8)+(2*8)+(1*9)=237
237 % 10 = 7
So 1883548-89-7 is a valid CAS Registry Number.
1883548-89-7Upstream product
1883548-89-7Downstream Products
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NI-57
