1. Cell Cycle/DNA Damage
  2. IRE1

Kira8 

目录号: HY-114368
产品使用指南

Kira8 是一种单选择性 IRE1α 抑制剂,可以变构减弱 IRE1α RNase 活性,IC50 为 5.9 nM。

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Kira8 Chemical Structure

Kira8 Chemical Structure

CAS No. : 1630086-20-2

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Description

Kira8 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.
References
Molecular Weight

601.12

Formula

C₃₁H₂₉ClN₆O₃S

CAS No.

1630086-20-2

SMILES

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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
Kira8
目录号:
HY-114368
需求量:

Kira8

Cat. No.: HY-114368