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| Company Name: |
BOC Sciences |
| Tel: |
16314854226 |
| Email: |
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| | GSK-J4 Hydrochloride Basic information |
| Product Name: | GSK-J4 Hydrochloride | | 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;1797983-09-5 (HCl);Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate hydrochloride;Histone Demethylase,diabetic,Th17,mice,cells,inflammation,Th1,H3K27me3/me2,dendritic,GSKJ4 Hydrochloride,TGF-β,inhibit,Inhibitor,GSK J4 Hydrochloride,demethylase,GSK-J4,GSK-J-4 Hydrochloride;GSK-J4 Hydrochloride, 10 mM in DMSO;ethyl 3-((2-(pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoate hydrochloride | | CAS: | 1797983-09-5 | | MF: | C24H28ClN5O2 | | MW: | 453.96442 | | EINECS: | | | Product Categories: | | | Mol File: | 1797983-09-5.mol |  |
| | GSK-J4 Hydrochloride Chemical Properties |
| storage temp. | under inert gas (nitrogen or Argon) at 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 |
| | GSK-J4 Hydrochloride Usage And Synthesis |
| 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. GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 with an IC50 value greater than 50 μM in vitro. 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). | | 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 | | 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 |
| | GSK-J4 Hydrochloride Preparation Products And Raw materials |
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