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詳細(xì)介紹 KIRA6

產(chǎn)品活性：KIRA6變構(gòu)抑制IRE1α RNase激酶活性，IC50值為0.6 M。

研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點(diǎn)：IRE1

In Vitro: KIRA6 dose-dependently inhibits IRE1α (WT) kinase activity, XBP1 RNA cleavage, Ins2 RNA cleavage and oligomerization. KIRA6 strongly inhibits JNK phosphorylation from IRE1α hyperactivation or ER stress. Also, KIRA6 dose-dependently inhibits Ins1 mRNA decay, proinsulin depletion, and apoptosis from IRE1α hyperactivation. In INS-1 cells, KIRA6 inhibits IRE1α auto-phosphorylation by Tg and XBP1 mRNA splicing by Tm in a dose-dependent manner. KIRA6 reduces ER stress-induced death of cultured cells and in pancreatic islet explants.

In Vivo: KIRA6 has negligible toxicity up to 10 μM, providing a favorable therapeutic index to test cytoprotection. KIRA6 in BALB/c mice intraperitoneally (i.p.) dosed at 10 mg/kg shows good drug plasma AUC levels with moderate clearance (22.4 mL/min/kg). Drug half-life is 3.90 hours, Cmax is 3.3 μM, and plasma levels at 4 and 8hr are 1.2 μM and 0.33 μM, respectively. Intravitreal co-injection of KIRA6 with Tm significantly reduces XBP1 splicing, TXNIP induction, and decay of the ER-localized photoreceptor-specific Rhodopsin mRNA. KIRA6 dose-dependently inhibits Rhodopsin RNA cleavage by IRE1α. Concomitant with blockage of Terminal UPR outputs, co-injection of KIRA6 in the Tm model reduces photoreceptor loss by Optical Coherence Tomography (OCT) and histology. KIRA6 substantially protects against loss of ERG responsiveness, significantly preserving both a- and b-wave amplitudes.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus | STF-083010 | 4μ8C | APY29 | MKC8866 | MKC3946 | GSK2850163 | MKC9989 | NSC95682 | 3,6-DMAD hydrochloride | B I09 | Kira8

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