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532281 IRE1 Inhibitor IV, KIRA6 - CAS 1589527-65-0 - Calbiochem

KIRA6, IRE1a Kinase Inhibitor

IRE1 Inhibitor IV, KIRA6 - CAS 1589527-65-0 - Calbiochem: Malzeme Güvenlik Bilgi Formu (MSDS) veya SDS, Analiz Sertifikası (COA) ve Kalite Uygunluk Sertifikası (COQ), dosyalar, broşürler ve diğer dokümanlar.

Synonyms: 1-(4-(8-Amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea, Kinase-Inhibiting RNase Attenuator 6, IRE1α Kinase Inhibitor

Primary Target: IRE1α kinase
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532281
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Overview

Key Spec Table

CAS #Empirical Formula
1589527-65-0C₂₈H₂₅F₃N₆O

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      		 Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, bioavailable, non-toxic, imidazopyrazinyl-naphthalenyl-phenylurea based compound that acts as a potent, ATP-competitive, reversible, and selective inhibitor of IRE1α kinase (IC50 = 600 nM). Exhibits good selectivity over ERK2, JNK2, JNK3, PIM1, PAK4, and PKA (IC50 > 10 µM). Stabilizes the kinase domain of IRE1α in an inactive conformation and blocks its oligomerization and thereby reduces RNase domain activity. Shown to block brefeldin A-(Cat. Nos. 203729 & 500583) induced ER stress and apoptosis in INS-1 cells and tunicamycin (Cat. Nos. 654380 & 504570)-induced apoptosis in β-cells derived from C57BL/6 mice. Affords significant cytoprotection in combination with STF-083010 (Cat. No. 412510, 1 µM) and KIRA6 (50 nM). Systemic administration of KIRA6 in the Akita diabetic mice is shown to reduce their blood glucose levels, improve glucose tolerance, and conserve their β-cell function. Preserves photoreceptor function in a transgenic rat model (P23H) of chronic ER stress-induced retinal degeneration, when administered intravitreally. Displays desirable pharmacokinetic properties with t1/2 = 3.9 h and moderate clearance rate of 22.4 ml/min/kg in BABL/c mice (10 mg/kg, i.p.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532281
      Brand Family Calbiochem®
      Synonyms1-(4-(8-Amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea, Kinase-Inhibiting RNase Attenuator 6, IRE1α Kinase Inhibitor
      References
      ReferencesGhosh, R., et al. 2014. Cell. 158, 534.
      Product Information
      CAS number1589527-65-0
      FormOff-white to brown powder
      Hill FormulaC₂₈H₂₅F₃N₆O
      Chemical formulaC₂₈H₂₅F₃N₆O
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetIRE1α kinase
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      5.32281.0001 04055977260038