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GSK J5

Catalog No.
B5686
inactive isomer of GSK J4, KDM inhibitor
Grouped product items
SizePriceStock Qty
5mg
$167.00
In stock
10mg
$288.00
In stock
50mg
$1,219.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceOff-white solid
StorageStore at RT
M.Wt417.5
Cas No.1394854-51-3
FormulaC24H27N5O2
Solubilityinsoluble in H2O; ≥17.3 mg/mL in EtOH with ultrasonic; ≥19.5 mg/mL in DMSO
Chemical Nameethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-3-yl)pyrimidin-4-yl)amino)propanoate
SDFDownload SDF
Canonical SMILESCCOC(CCNC1=CC(N2CCC3=CC=CC=C3CC2)=NC(C4=CN=CC=C4)=N1)=O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control