KIRA6

SKU: orb1296223

Description

KIRA6

Research Area

Cell Biology

Key Properties

• CAS Number: 1589527-65-0
• MW: 518.53
• Purity: 100.00%
• Formula: C₂₈H₂₅F₃N₆O
• SMILES: CC(C)(C)c1nc(-c2ccc(NC(=O)Nc3cccc(c3)C(F)(F)F)c3ccccc23)c2c(N)nccn12
• Target: IRE1
• Solubility: DMSO:5.2 mg/mL (10.03 mM);Ethanol:2 mg/mL (3.86 mM)

Bioactivity

• Target IC50:
  IRE1α:0.6 µM (cell free)
• In Vivo:
  KIRA6 (intraperitoneal injection; 5 mg/kg; 37 days) shows significant amelioration of andom glucose levels over several weeks compared to the Vehicle, both fed ad lib. KIRA6 (i.p, 5 mg/kg, 21 or 18 days post injections) increases both plasma Insulin and C-peptide levels, remains insulin-positive islet areas at a high level after stopping injections in the Akita Mouse.
• In Vitro:
  KIRA6 (10-1000 nM, 72 hours) strongly compromise the viability o the KIT-dependent cell line HMC-1.1 a the low nM concentration in a manner that coincided with KIT blockade. KIRA6 ( nM-10 μM) bounds to the cytoplasmic domain of KIT with a Kd value of 10.8 μM. KIRA6 (10-1000 nM, 1 hour) reduces signaling output of KIT, includin the phosphorylation of KIT as well as its downstream signaling modules, PSTAT5 and phosphorylated ERK1/2. KIRA6 (1 μM, 0-48 hours) inhibits Ins1 mRNA decay from IRE1α hyperactivation in a dose-dependent manner. KIRA6 (0.1-1 μM, 72 hours) dose-dependently reduces nM-PP1 potentiation of Ins1 apoptosis during ER stress in a dose-dependent manner.
• Cell Research:
  Cell Line: HMC-1. Cells. concentration 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM. Incubation Time: 72 hours
• Animal Research:
  Animal Model: Male Ins2+/Akita mice. Dosage: 5 mg/kg. Administration: Intraperitoneal injection, 5 mg/kg, 21 or 18 days post injections

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Inositol requiring enzyme 1, IRE1, IRE1α, KIRA 6, KIRA6, KIRA-6, inhibit

Compound Identifiers

PubChem CID

73425700