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GSK-J4 Hydrochloride

GSK-J4 Hydrochloride ??? ???
?? ??:
1797983-09-5
???:
GSK-J4 Hydrochloride
???(??):
1797983-09-5 (HCl);GSK-J4 Hydrochloride;TYXWLTBYINKVNT-UHFFFAOYSA-N;GSK-J4 Hydrochloride, 10 mM in DMSO;Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride;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
CBNumber:
CB12700565
???:
C24H28ClN5O2
??? ??:
453.96442
MOL ??:
1797983-09-5.mol

GSK-J4 Hydrochloride ??

?? ??
under inert gas (nitrogen or Argon) at 2-8°C
???
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)
??? ??
??? ??
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Light yellow to yellow
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  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
????(GHS): GHS hazard pictograms
?? ?: Danger
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H290 ??? ???? ? ?? ?? ????? ?? 1 ?? GHS hazard pictograms P234, P390, P404
H314 ??? ?? ??? ?? ??? ??? ????? ?? ????? ?? 1A, B, C ?? GHS hazard pictograms P260,P264, P280, P301+P330+ P331,P303+P361+P353, P363, P304+P340,P310, P321, P305+ P351+P338, P405,P501
??????:
P234 ??? ???? ?????.
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P280 ????/???/???/?????? ?????.
P301+P330+P331 ???? ?? ?????. ??? ?? ?? ???.
P303+P361+P353 ??(?? ????)? ??? ??? ?? ??? ??? ????? ??? ?? ????/?????.
P363 ?? ??? ??? ??? ?????.
P390 ????? ???? ?? ???? ??????.
P405 ???? ?????.
P406 ??? ???? ?????/...???? ??
P501 ...? ??? / ??? ?? ???.

GSK-J4 Hydrochloride C??? ??, ??, ??

??

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).

??

GSK-J4 Hydrochloride is a histone demethylase JMJD3/UTX inhibitors which blocks demethylation of histone H3K27.

GSK-J4 Hydrochloride ?? ?? ? ???

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GSK-J4 Hydrochloride ?? ??

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