Amgen IRE1α Inhibitor

Amgen IRE1α Inhibitor Chemische Eigenschaften,Einsatz,Produktion Methoden

• Verwenden

  Amgen IRE1α Inhibitor is an inhibitor of IRE1α. IRE1α is a sensor of unfolded protein accumulation that triggers the unfolded protein response.

• Biologische Aktivität

  KIRA8 is an ATP-competitive, potent and selective IRE1α kinase inhibitor (IRE1α/β Ki = 2/120 nM) th at attenuates IRE1α endonuclease activity (IRE1α/β IC50 = 5/55 nM) with good kinome selectivity. KIRA8 inhibits thapsigargin-induced UPR (IC50 = 99 nM; HT1080 XBP1-Luc cells) and shows therapeutic efficacy in murine models of type 1 diabetes (T1D), pulmonary fibrosis, multiple myeloma (MM), and pancreatic neuroendocrine tumors (PanNET) in vivo (30-50 mg/kg/day i.p.).

• 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.

Amgen IRE1α Inhibitor Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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