1630086-20-2

1630086-20-2 structure

Name: Kira8
Chemical Name: Kira8
CAS Number: 1630086-20-2
Molecular Formula: C₃₁H₂₉ClN₆O₃S
Molecular Weight: 601.12
Catalog: Signaling Pathways Cell Cycle/DNA Damage IRE1
Create Date: 2019-03-03 12:19:00
Modify Date: 2026-07-06 17:02:39
Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase[1].

Name	Kira8
Synonyms	Amgen IRE1± Inhibitor Kira8, 10 mM in DMSO (S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8 Kira8 ，E2652 KIRA8 (AMG-18) (S)-2-Chloro-N-[6-methyl-5-[[3-[2-(3-piperidylamino)-4-pyrimidinyl]-2-pyridyl]oxy]-1-naphthyl]benzenesulfonamide IRE-1 INHIBITOR Amgen IRE1α Inhibitor Amgen IRE1a Inhibitor Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]

Description	Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase[1].
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> IRE1 Research Areas >> Inflammation/Immunology
Target	IRE1α[1]
In Vitro	KIRA8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. KIRA8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2[1].
In Vivo	Kira8 efficaciously reverses established diabetes in NOD mice by sparing β-cells and preserving their physiological function. KIRA8 is first tested in 3-week-old male pre-diabetic Akita mice by i.p. daily dosing of 50 mg/kg, whereupon significant reduction of hyperglycemia became apparent over several weeks. Then KIRA8 (50 mg/kg) is tested in the complex NOD. Showing target engagement, one week treatment of pre-diabetic NODs with KIRA8 leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserved Ins1/Ins2, BiP and MANF mRNAs[1].
References	[1]. Morita S, et al. Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes. Cell Metab. 2017 Apr 4;25(4):883-897.e8.