KIRA6|cas:1589527-65-0|西域试剂

KIRA6,99.68%

产品编号：Bellancom-19708| CAS NO：1589527-65-0| 分子式：C₂₈H₂₅F₃N₆O| 分子量：518.53

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货号	价格	库存与货期
Bellancom-19708	￥1200.00	杭州北京（现货）
Bellancom-19708	￥1800.00	杭州北京（现货）
Bellancom-19708	￥6300.00	杭州北京（现货）
Bellancom-19708	￥9800.00	杭州北京（现货）

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KIRA6

产品介绍

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。

生物活性

KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC₅₀ of 0.6 µM. KIRA6 can trigger an apoptotic response.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	HMC-1.1 cells
Concentration:	10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:	72 hours
Result:	Inhibited cell viability from 30 nM.

Western Blot Analysis

Cell Line:	HMC-1.1 cells
Concentration:	10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:	1 hours
Result:	Reduced expression of phosphorylated KIT, STAT5 and ERK1/2.

RT-PCR

Cell Line:	INS-1 IRE1α (WT) cells
Concentration:	1 μM
Incubation Time:	0 hour, 12 hours, 24 hours, 48 hours
Result:	Inhibited Ins1 mRNA expression.

Apoptosis Analysis

Cell Line:	INS-1 IRE1α (WT) cells
Concentration:	1-10 μM
Incubation Time:	72 hours
Result:	Reduced 1NM-PP1 potentiation of Ins1 apoptosis during ER stress.

体内研究
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Ins2+/Akita mice
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections
Result:	Attenuates b cell functional loss, increased insulin levels.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Ins2+/Akita mice
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections
Result:	Attenuates b cell functional loss, increased insulin levels.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Ins2+/Akita mice
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections
Result:	Attenuates b cell functional loss, increased insulin levels.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (48.21 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9285 mL	9.6426 mL	19.2853 mL
5 mM	0.3857 mL	1.9285 mL	3.8571 mL
10 mM	0.1929 mL	0.9643 mL	1.9285 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (0.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (0.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (0.96 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。