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Merck

SML0974

Sigma-Aldrich

(+/-)-JQ1

≥98% (HPLC)

Synonym(e):

N-(2′,5′-Dimethoxy[1,1′-biphenyl]-4-yl)-3-fluoro-4-pyridinecarboxamide, (+/-)-SGCBD01, [(R,S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulen-6-yl]-acetic acid tert-butyl ester

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About This Item

Empirische Formel (Hill-System):
C23H25ClN4O2S
CAS-Nummer:
Molekulargewicht:
456.99
MDL-Nummer:
UNSPSC-Code:
51111800
PubChem Substanz-ID:
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Arzneimittelkontrolle

regulated under CDSA - not available from Sigma-Aldrich Canada

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear (warmed)

Lagertemp.

2-8°C

SMILES String

CC1=NN=C2N1C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=NC2CC(OC(C)(C)C)=O

InChI

1S/C23H25ClN4O2S/c1-12-13(2)31-22-19(12)20(15-7-9-16(24)10-8-15)25-17(11-18(29)30-23(4,5)6)21-27-26-14(3)28(21)22/h7-10,17H,11H2,1-6H3

InChIKey

DNVXATUJJDPFDM-UHFFFAOYSA-N

Anwendung

(±)-JQ1 has been used to study its effect on adipogenesis, by analyzing the its impact on the regulation of genes involved in this process especially peroxisome proliferator-activated receptor (PPAR-g), the CCAAT/enhancer-binding protein (C/EBPa) and, STAT5A and B. JQ1 has been used in drug binding assays as a chemical inhibitor of BRD4 to study the CRBN’s substrate recruiting function in mouse and human.

Biochem./physiol. Wirkung

(±)-JQ1 is a Brd4 inhibitor. JQ1 is known to suppress cell proliferation and therefore, can be used as a therapeutic drug for a number of cancers including multiple myeloma and acute myeloid leukemia.
The human BET family, which includes BRD2, BRD3, BRD4 and BRDT, play a role in regulation of gene transcription. (+/-)-JQ1 ((+/-)SGCBD01) is a selective BET bromodomain (BRD) inhibitor that inhibits Brd4 (Bromodomain-containing 4). Brd4 forms complexes with chromatin via two tandem bromodomains (BD1 and BD2) that bind to acetylated lysine residues in histones and Brd4 association with acetylated chromatin is believed to regulate the recruitment of elongation factor b and additional transcription factors to specific promoter regions. The nuclear protein in testis (NUT) gene is known to form fusions with Brd4 that create a potent oncogene, leading to rare, but highly lethal tumors referred to as NUT midline carcinomas (NMC). JQ1 inhibits recruitment and binding of Brd4 to TNFα and E-selectin promoter elements, and accelerates recovery time in FRAP (fluorescence recovery after photobleaching) assays using GFP-Brd4. Thus JQ1/SGCBD01 is a useful tool to study the role of Brd4 in transcriptional initiation. For full characterization details, please visit the SGCBD01/JQ1 probe summary on the Structural Genomics Consortium (SGC) website.

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

Leistungsmerkmale und Vorteile

(+/-) JQ-1 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.

Sonstige Hinweise

JQ1 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the JQ1 probe summary on the Chemical Probes Portal website.
Racemic mixture

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Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon.
Akuffo A A, et al.
The Journal of Biological Chemistry (2018)
Yunlu Jia et al.
Blood cancer journal, 11(2), 32-32 (2021-02-14)
Multiple myeloma (MM) is an aggressive plasma cell neoplasm characterized by genomic heterogeneity. Superenhancers (SEs) are defined as large clusters of enhancers in close genomic proximity, which regulate genes for maintaining cellular identity and promote oncogenic transcription to which cancer
Hiroki Michida et al.
Cell reports, 31(9), 107724-107724 (2020-06-04)
NF-κB is a transcription factor that activates super enhancers (SEs) and typical enhancers (TEs) and triggers threshold and graded gene expression, respectively. However, the mechanisms by which NF-κB selectively participates in these enhancers remain unclear. Here we show using mouse
Sonali Das et al.
STAR protocols, 4(1), 102004-102004 (2023-01-14)
Isolation of extraordinarily long-length super-enhancers (SEs) using typical chromatin immune precipitation (ChIP) techniques can lead to DNA breakage due to uncontrolled cross-linking. We present a redefined ChIP technique for SE purification. After controlled paraformaldehyde-based cross-linking, glycine was used to quench
Ying Liang et al.
Nature communications, 13(1), 7329-7329 (2022-11-29)
Technologies for gene activation are valuable tools for the study of gene functions and have a wide range of potential applications in bioengineering and medicine. In contrast to existing methods based on recruiting transcriptional modulators via DNA-binding proteins, we developed

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