| Identification | Back Directory | [Name]
GSK-J4 Hydrochloride | [CAS]
1797983-09-5 | [Synonyms]
GSK-J4 Hydrochloride
TYXWLTBYINKVNT-UHFFFAOYSA-N
Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride | [Molecular Formula]
C24H28ClN5O2 | [MDL Number]
MFCD26142638 | [MOL File]
1797983-09-5.mol | [Molecular Weight]
453.964 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO:60.83(Max Conc. mg/mL);134.0(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:7):0.1(Max Conc. mg/mL);0.22(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);66.08(Max Conc. mM)
Ethanol:55.0(Max Conc. mg/mL);121.15(Max Conc. mM)
Water:10.0(Max Conc. mg/mL);22.03(Max Conc. mM) | [form ]
A crystalline solid | [color ]
Light yellow to yellow | [InChIKey]
TYXWLTBYINKVNT-UHFFFAOYSA-N | [SMILES]
c1(N2CCc3ccccc3CC2)cc(NCCC(=O)OCC)nc(-c2ncccc2)n1.Cl |
| Hazard Information | Back Directory | [Description]
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.1,2 GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.3 Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 μM).3 | [Uses]
GSK-J4 Hydrochloride is a histone demethylase JMJD3/UTX inhibitors which blocks demethylation of histone H3K27. | [in vivo]
GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice[2].
GSK-J4 Hydrochloride (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis[3]. | Animal Model: | Eight-week-old male db/m and db/db mice on a BKS background[2] | | Dosage: | 10 mg/kg | | Administration: | i.p.; thrice-weekly for 10 weeks | | Result: | Attenuated the development of kidney disease in diabetic mice. |
| [IC 50]
KDM6 | [storage]
Store at -20°C | [References]
[1] KARL AGGER. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development[J]. Nature, 2007, 449 7163: 731-734. DOI: 10.1038/nature06145
[2] M R HüBNER D L S. Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulation.[J]. Cold Spring Harbor symposia on quantitative biology, 2010: 43-49. DOI: 10.1101/sqb.2010.75.020
[3] LAURENS KRUIDENIER. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response[J]. Nature, 2012, 488 7411: 404-408. DOI: 10.1038/nature11262
[4] BO YANG. Reepithelialization of Diabetic Skin and Mucosal Wounds Is Rescued by Treatment With Epigenetic Inhibitors.[J]. Diabetes, 2024: 120-134. DOI: 10.2337/db23-0258 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|