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KIRA6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KIRA6图片
CAS NO:1589527-65-0
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议

产品介绍
KIRA6 是一种 IRE1α RNase 激酶的有效抑制剂,IC50为0.6 μM。它可以触发细胞凋亡反应。

产品描述

KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.

体外活性

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 [1]. 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].

体内活性

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 [2].

细胞实验

Cell Line: HMC-1.1 cells. Concentration: 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM. Incubation Time: 72 hours [1]

动物实验

Animal Model: Male Ins2+/Akita mice. Dosage: 5 mg/kg. Administration: Intraperitoneal injection, 5 mg/kg, 21 or 18 days post injections [2]

Cas No.

1589527-65-0

分子式

C28H25F3N6O

分子量

518.53

储存和溶解度

Ethanol:2 mg/mL (3.86 mM),Need ultrasonic
DMSO:5 mg/mL (9.64 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years