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’s RNase 活性 。

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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’s RNase[1].

IC50 & 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6636 mL 8.3178 mL 16.6356 mL
5 mM 0.3327 mL 1.6636 mL 3.3271 mL
10 mM 0.1664 mL 0.8318 mL 1.6636 mL
*Please refer to the solubility information to select the appropriate solvent.
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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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Inquiry Information

产品名称:
Kira8
目录号:
HY-114368
需求量:

Kira8

Cat. No.: HY-114368