1. Cell Cycle/DNA Damage
  2. IRE1
  3. Kira8 Hydrochloride

Kira8 Hydrochloride (Synonyms: AMG-18 Hydrochloride)

Cat. No.: HY-114368A
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Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

For research use only. We do not sell to patients.

Kira8 Hydrochloride Chemical Structure

Kira8 Hydrochloride Chemical Structure

CAS No. : 2250019-92-0

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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].

IC50 & 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.
Molecular Weight

637.58

Formula

C₃₁H₃₀Cl₂N₆O₃S

CAS No.

2250019-92-0

SMILES

O=S(C1=CC=CC=C1Cl)(NC2=C3C=CC(C)=C(C3=CC=C2)OC4=NC=CC=C4C5=NC(N[[email protected]]6CNCCC6)=NC=C5)=O.[H]Cl

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Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Kira8 Hydrochloride
Cat. No.:
HY-114368A
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