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 RNase activity with an IC50 of 5.9 nM.

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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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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[[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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Kira8
Cat. No.:
HY-114368
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Kira8

Cat. No.: HY-114368