1. Cell Cycle/DNA Damage
  2. IRE1

Kira8 

Cat. No.: HY-114368
Handling Instructions

Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase.

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

Kira8 Chemical Structure

Kira8 Chemical Structure

CAS No. : 1630086-20-2

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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[[email protected]@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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Product Name:
Kira8
Cat. No.:
HY-114368
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Kira8

Cat. No.: HY-114368