KIRA6,1589527-65-0

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KIRA6

CAS No. : 1589527-65-0

MCE 国际站：KIRA6

产品活性：KIRA6，小分子 IRE1α RNase 激酶抑制剂，IC₅₀ 值为0.6 µM。 KIRA6 可以触发细胞凋亡 (apoptotic) 反应。

研究领域：Cell Cycle/DNA Damage

作用靶点：IRE1

In Vitro: KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a K_d value of 10.8 ?μM.
?KIRA6 (10-1000 nM; 72 hours) strongly compromises the viability of the KIT-dependent cell line HMC-1.1 at the low nM concentration, in a manner that coincided with KIT blockade.
?KIRA6 (10-1000 nM; 1 hour) reduces signaling output of KIT,? including 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 at a dose-dependent manner.
?KIRA6 (0.1-10μM; 72 hours) dose-dependently reduces 1NM-PP1 potentiation of Ins1 apoptosis during ER stress in a dose-dependent manner.

In Vivo: KIRA6 (intraperitoneal injection; 5 mg/kg; 37 days) shows significant amelioration of random glucose levels over several weeks compared to vehicle, both fed ad lib.
?KIRA6 (intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections) increases both plasma insulin and C-peptide levels, remains insulin-positive islet areas at high level after stopping injections in the Akita Mouse.

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