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Merck
CN

SML0992

Sigma-Aldrich

Bromosporine

≥98% (HPLC)

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别名:
N-[6-(3-Methanesulfonamido-4-methylphenyl)-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-yl]carbamate
经验公式(希尔记法):
C17H20N6O4S
分子量:
404.44
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 20 mg/mL, clear

储存温度

2-8°C

SMILES字符串

CC(C(NS(C)(=O)=O)=C1)=CC=C1C2=NN3C(C(NC(OCC)=O)=C2)=NN=C3C

InChI

1S/C17H20N6O4S/c1-5-27-17(24)18-15-9-14(21-23-11(3)19-20-16(15)23)12-7-6-10(2)13(8-12)22-28(4,25)26/h6-9,22H,5H2,1-4H3,(H,18,24)

InChI key

UYBRROMMFMPJAN-UHFFFAOYSA-N

生化/生理作用

Bromodomains (BRDs) are protein-interaction modules that "read" ε-N-lysine acetylation motifs, such as those found in the N-terminal tails of histones. BRDs have been identified in chromatin-modifying enzymes (such as histone acetyltransferases (HATs)) as well as in transcription factors that regulate genes for cell cycle progression, signal transduction, apoptosis, and inflammation. Proteins containing bromodomains have been implicated in various diseases, such as cancers, inflammatory diseases and neurological diseases. Bromosporine is a broad spectrum BRD inhibitor. In HeLa cells, bromosporine accelerates FRAP recovery of BRD4 and CREBBP at 1μM. For full characterization details, please visit the Bromosporine probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

特点和优势

Bromosporine is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

相关产品

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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Hanyu Pan et al.
Oncotarget, 8(55), 94104-94116 (2017-12-08)
The long-lived latent HIV-1 reservoir is the major barrier for complete cure of Acquired Immune Deficiency Syndrome (AIDS). Here we report that a novel bromodomain and extraterminal domain (BET) inhibitor bromosporine which can broadly target BETs, is able to potently
Berkley E Gryder et al.
Cancer discovery, 7(8), 884-899 (2017-04-28)
Alveolar rhabdomyosarcoma is a life-threatening myogenic cancer of children and adolescent young adults, driven primarily by the chimeric transcription factor PAX3-FOXO1. The mechanisms by which PAX3-FOXO1 dysregulates chromatin are unknown. We find PAX3-FOXO1 reprograms the
Alexander N Phillipou et al.
SLAS discovery : advancing life sciences R & D, 25(2), 163-175 (2019-12-26)
Malfunctions in the basic epigenetic mechanisms such as histone modifications, DNA methylation, and chromatin remodeling are implicated in a number of cancers and immunological and neurodegenerative conditions. Within GlaxoSmithKline (GSK) we have utilized a number of variations of the NanoBRET
Ming Jang Chua et al.
International journal for parasitology. Drugs and drug resistance, 8(2), 189-193 (2018-04-10)
Bromodomain-containing proteins (BDPs) are involved in the regulation of eukaryotic gene expression. Compounds that bind and/or inhibit BDPs are of interest as tools to better understand epigenetic regulation, and as possible drug leads for different diseases, including malaria. In this
Flore Mietton et al.
Nature communications, 8, 15482-15482 (2017-05-19)
Invasive fungal infections cause significant morbidity and mortality among immunocompromised individuals, posing an urgent need for new antifungal therapeutic strategies. Here we investigate a chromatin-interacting module, the bromodomain (BD) from the BET family of proteins, as a potential antifungal target

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