Kira8

SKU: orb1309509

Description

Kira8

Research Area

Cell Biology

Key Properties

• CAS Number: 1630086-20-2
• MW: 601.12
• Purity: 98.07%
• Formula: C₃₁H₂₉ClN₆O₃S
• SMILES: Cc1ccc2c(NS(=O)(=O)c3ccccc3Cl)cccc2c1Oc1ncccc1-c1ccnc(N[C@H]2CCCNC2)n1
• Target: IRE1
• Solubility: DMSO:65 mg/mL (108.13 mM);H2O:insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.33 mM)

Bioactivity

• Target IC50:
  IRE1α:5.9 nM(IRE1α RNase)
• In Vivo:
  One week of treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) causes obvious reductions in islet XBP1 splicing and TXNIP mRNAs. It also preserves Ins1/Ins2, BiP, and MANF mRNAs. Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), obviously reduction of hyperglycemia becomes apparent over several weeks.
• In Vitro:
  Kira8 more effectively causes IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2. Kira8 blocks IRE1α oligomerization and effectively inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AMG 18, AMG18, AMG-18, Inhibitor, Inositol requiring enzyme 1, Kira 8, Kira8, Kira-8, inhibit, IRE1α, IRE1, IRE1α RNase

Compound Identifiers

PubChem CID

118721244