| Identification | Back 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 Properties | Back Directory | [Boiling point ]
581.2±50.0 °C(Predicted) | [density ]
1.216±0.06 g/cm3(Predicted) | [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 | [pka]
5.87±0.10(Predicted) | [color ]
Off-white |
| Hazard Information | Back 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. | [IC 50]
Schistosome | [storage]
Store at RT |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|