GSK J4 HCl
- CAS No.
- 1373423-53-0
- Chemical Name:
- GSK J4 HCl
- Synonyms
- GSK-J4;GSK J4;CS-1667;CS-2143;GSK J4 HCl;6-Triiodophenol;GSK J4 free base;GSKJ4HCL(free base);GSK J4 HCl USP/EP/BP;GSK J4 HCl (GSKJ4 HCl)
- CBNumber:
- CB62665155
- Molecular Formula:
- C24H27N5O2
- Molecular Weight:
- 417.5
- MDL Number:
- MFCD22683852
- MOL File:
- 1373423-53-0.mol
- MSDS File:
- SDS
Boiling point | 581.2±50.0 °C(Predicted) |
---|---|
Density | 1.216±0.06 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMSO: soluble20mg/mL, clear |
pka | 5.95±0.10(Predicted) |
form | Tan semi-solid |
color | white to beige |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
InChIKey | WBKCKEHGXNWYMO-UHFFFAOYSA-N |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H319-H315-H335 |
Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P |
Hazard Codes | Xi |
Risk Statements | 36/37/38 |
Safety Statements | 26 |
WGK Germany | 3 |
GSK J4 HCl price More Price(16)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML0701 | GSK-J4 ≥98% (HPLC) | 1373423-53-0 | 5mg | $117 | 2024-03-01 | Buy |
Sigma-Aldrich | 420205 | Histone Lysine Demethylase Inhibitor VIII, GSK-J4 | 1373423-53-0 | 10mg | $245 | 2024-03-01 | Buy |
Sigma-Aldrich | SML0701 | GSK-J4 ≥98% (HPLC) | 1373423-53-0 | 25mg | $469 | 2024-03-01 | Buy |
Tocris | 4594 | GSKJ4 ≥99%(HPLC) | 1373423-53-0 | 50 | $876 | 2021-12-16 | Buy |
TRC | G797555 | GSKJ4 | 1373423-53-0 | 10mg | $165 | 2021-12-16 | Buy |
GSK J4 HCl Chemical Properties,Uses,Production
Description
GSK-J4 (1373423-53-0) is a histone demethylase JMJD3/UTX inhibitor. Inhibits demethylation of histone H3K27. Reduces LPS-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable, ethyl ester of GSK J1 (cat.# 10-1393).1 GSK-J4 rescues newborn pups from embryonic lethality in BRAF knockin mice which recapitulate major features of RASopathies.2
Uses
GSK-J4 has been used to study the effect of KDM2B (Jumonji (JmjC) domain histone 3 lysine 36 (H3K36) di-demethylase) inhibition on the survival and DNA repair potential of glioblastoma cells. It has also been used in sulforhodamine B (SRB) cell growth assay and cell viability assay.
Definition
ChEBI: 3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid ethyl ester is an organonitrogen heterocyclic compound.
Biochem/physiol Actions
GSK-J4 is cell permeable prodrug rapidly hydrolysed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. The prodrug GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. For characterization details for GSK-J4 and full characterization details for GSK-J1, please visit the GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
storage
Room temperature
References
1) Kruidenier et al. (2012), Selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404 2) Inoue et al. (2014) New Braf knockin mice provide a pathogenic mechanism of developmental defects and therapeutic approach in cardio-facio-cutaneous syndrome; Hum. Mol. Genet.,?23?6553
![4424-20-8](/CAS/GIF/4424-20-8.gif)
![1373423-17-6](/CAS/20150408/GIF/1373423-17-6.gif)
![1373423-53-0](/CAS/20150408/GIF/1373423-53-0.gif)
GSK J4 HCl Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 60 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | fandachem@gmail.com | China | 9332 | 55 |
Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29825 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 24330 | 58 |
Chemia Biotechnology(Shanghai) Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10522 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Related articles
- GSK-J4 HCl: Mechanism And Bioactivity studies
- GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases?JMJD3/KDM6B?and?UTX/KDM6A?with?IC50s of 8.6 and 6.6 μM, respect....
- Jan 5,2023
View Lastest Price from GSK J4 HCl manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2019-12-24 | ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
1373423-53-0
|
US $1.00 / KG | 1KG | Min98% HPLC | g/kg/ton | Career Henan Chemical Co |
-
- ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
1373423-53-0
- US $1.00 / KG
- Min98% HPLC
- Career Henan Chemical Co
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