GSK J5
- Product Name
- GSK J5
- CAS No.
- 1394854-51-3
- Chemical Name
- GSK J5
- Synonyms
- GSK-J5;GSK J5;CS-2752;GSK-J5|||GSKJ5;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;β-Alanine, N-[2-(3-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-, ethyl ester;N-[2-(3-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine ethyl ester
- CBNumber
- CB22668284
- Molecular Formula
- C24H27N5O2
- Formula Weight
- 417.50348
- MOL File
- 1394854-51-3.mol
GSK J5 Property
- 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
N-Bromosuccinimide Price
- Product number
- G797560
- Product name
- GSKJ5
- Packaging
- 10mg
- Price
- $205
- Updated
- 2021/12/16
- Product number
- A8792
- Product name
- GSKJ5HCl
- Packaging
- 5mg
- Price
- $146
- Updated
- 2021/12/16
- Product number
- CM161409
- Product name
- ethyl3-((2-(pyridin-3-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoate
- Purity
- 95%
- Packaging
- 10mg
- Price
- $611
- Updated
- 2021/12/16
- Product number
- CD11265845
- Product name
- GSKJ5
- Purity
- 95+%
- Packaging
- 10mg
- Price
- $654
- Updated
- 2021/12/16
- Product number
- CD11265845
- Product name
- GSKJ5
- Purity
- 95+%
- Packaging
- 50mg
- Price
- $1962
- Updated
- 2021/12/16
GSK J5 Chemical Properties,Usage,Production
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.
GSK J5 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK J5 Suppliers
- Tel
- --
- Fax
- --
- customerservice@tocris.co.uk
- Country
- United Kingdom
- ProdList
- 5726
- Advantage
- 77