KIRA6

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.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 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.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 (1nM-100μM) 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, 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 in 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 [2].KIRA6 (intraperitoneal injection; 5 mg/kg; 37 days) shows significant amelioration of random 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.

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Others

Other Targets

IRE1α

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1589527-65-0

518.53

C28H25F3N6O

>98% (HPLC)

DMSO:5 mg/mL (9.64 mM);Ethanol:2 mg/mL (3.86 mM; Need ultrasonic)

CC(C)(C)C1=NC(=C2N1C=CN=C2N)C1=CC=C(NC(=O)NC2=CC=CC(=C2)C(F)(F)F)C2=CC=CC=C12

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(-20℃)

With Ice Pack

≥ 2 years