Chemical Name: 1-[4-(8-Amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl]-3-[3-(trifluoromethyl)phenyl]urea
IRE1alpha inhibitor
Molekulargewicht:
518.54
Reinheit:
>98% by HPLC NMR (Conforms)
Formulierung:
White solid
CAS Nummer:
[1589527-65-0]
Formel:
C28H25F3N6O
Anwendungsbeschreibung:
KIRA6 is an allosteric inhibitor of the endoplasmic reticulum protein IRE1alpha.1 It inhibits IRE1alpha kinase activity (IC50 = 0.60 µM), XBP1 RNA cleavage, Ins2 RNA cleavage, and oligomerization. KIRA6 prevented cell death during ER stress/UPR in vivo. It reduced stress-induced inflammation caused by immunogenic cell death via targeting of HSP60.2 KIRA6 abolished neuroinflammation and neuronal cell death caused by PAD4 overexpression in traumatic brain injury.3 It also was shown to block leukotriene biosynthesis in human phagocytes4 and inhibit mast cells5. KIRA6 blocked the induction of myeloid-derived suppressor cells and overcame resistance to anti-PD-1 therapy in 4T1 tumor cells.6
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