Kira8 Hydrochloride
Names
[ CAS No. ]:
2250019-92-0
[ Name ]:
Kira8 Hydrochloride
Biological Activity
[Description]:
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1].
[Related Catalog]:
[Target]
IRE1α[1] IC50: 5.9 nM (IRE1α RNase)[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]
Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks[1]. One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs[1]. Animal Model: Male Ins2+/Akita mice[1] Dosage: 50 mg/kg Administration: Injected i.p.; daily; for 35 days Result: Significant reduction of hyperglycemia became apparent over several weeks.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C31H30Cl2N6O3S
[ Molecular Weight ]:
637.58