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ChemicalBook--->CAS DataBase List--->1394854-51-3

1394854-51-3

1394854-51-3 Structure

1394854-51-3 Structure
IdentificationBack Directory
[Name]

GSK J5
[CAS]

1394854-51-3
[Synonyms]

GSK J5
GSK-J5
CS-2752
Ethyl N-[2-(3-pyridinyl)-6-(1,2,4,5-tetrahydro-3h-3-benzazepin-3- Yl)-4-pyrimidinyl]-β-alaninate
N-[2-(3-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine ethyl ester
N-[2-(3-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine ethyl ester
[Molecular Formula]

C24H27N5O2
[MDL Number]

MFCD27991275
[MOL File]

1394854-51-3.mol
[Molecular Weight]

417.503
Chemical PropertiesBack Directory
[storage temp. ]

Store at RT
[solubility ]

insoluble in H2O; ≥17.3 mg/mL in EtOH with ultrasonic; ≥19.5 mg/mL in DMSO
[form ]

solid
[color ]

Off-white
Hazard InformationBack Directory
[Uses]

GSK J5 is a inactive isomer of GSK J4 (G797555), which is a cell permeable inhibitor of the histone demethylase JMJD3/UTX.
[Biological Activity]

gsk j5 is an inactive isomer of gsk j4 and a cell-permeable ester derivative of inactive control gsk j2. lysine-specific demethylase 6b (kdm6b), also known as jumonji domain-containing protein d3 (jmjd3), was overexpressed in patients with aml and these patients have a poor prognosis. kdm6b-specific pharmacological inhibitor gsk-j4 had a significant anti-proliferative effect in aml cell lines and freshly isolated bm monocytes (mncs) from aml patients, while h3k27me3 levels were also increasing. gsk-j4 also caused apoptosis and cell cycle arrest in vitro, and reduced tumor burden in vivo in aml xenograft mouse models. it is worth noting that injection of gsk-j4 attenuated disease progression in a human aml xenograft mouse model. treatment with gsk-j4 mainly resulted in downregulation of dna replication and cell cycle-related pathways, and prevents the expression of hox, a key cancer gene. chip-qpcr verified the increased h3k27me3 enrichment in the hox gene transcription initiation site [1].[1]. li y, zhang m, sheng m, zhang p, chen z, xing w, bai j, cheng t, yang fc, zhou y. therapeutic potential of gsk-j4, a histone demethylase kdm6b/jmjd3 inhibitor, for acute myeloid leukemia. j cancer res clin oncol. 2018 jun;144(6):1065-1077. doi: 10.1007/s00432-018-2631-7. epub 2018 mar 28. pubmed pmid: 29594337; pubmed central pmcid: pmc5948279.
[storage]

Store at RT
Spectrum DetailBack Directory
[Spectrum Detail]

GSK J5(1394854-51-3)MS
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