LW6 HIF-1α inhibitor; LW8|cas:934593-90-5|西域试剂

LW6 HIF-1α inhibitor; LW8,98.93%

产品编号：Bellancom-13671| CAS NO：934593-90-5| 分子式：C₂₆H₂₉NO₅| 分子量：435.51

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-13671	￥660.00	杭州北京（现货）
Bellancom-13671	￥920.00	杭州北京（现货）
Bellancom-13671	￥2000.00	杭州北京（现货）
Bellancom-13671	￥3580.00	杭州北京（现货）
Bellancom-13671	￥6000.00	杭州北京（现货）

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LW6 HIF-1α inhibitor; LW8

产品介绍

LW6 (HIF-1α inhibitor) 是新颖的 HIF-1 抑制剂，IC₅₀ 值为 4.4 μM。LW6 降低 HIF-1α 蛋白表达，而不影响 HIF-1β 表达。

生物活性

LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC₅₀ of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.

体外研究

LW6 affects the stability of the HIF-1α protein. LW6 promotes the degradation of wild type HIF-1α, but not of a DM-HIF-1α with modifications of P402A and P564A, at hydroxylation sites in the oxygen-dependent degradation domain. LW6 induces the expression of von Hippel-Lindau (VHL), which interacts with prolyl-hydroxylated HIF-1α for proteasomal degradation. In the presence of LW6, knockdown of VHL does not abolish HIF-1α protein accumulation, indicating that LW6 degraded HIF-1α via regulation of VHL expression. In MDCKII-BCRP cells overexpressing BCRP, LW6 enhances significantly the cellular accumulation of mitoxantrone, a BCRP substrate. LW6 also down-regulates BCRP expression at concentrations of 0.1-10 µM. LW6 inhibits the expression of HIF 1α induced by hypoxia in A549 cells at 20 µM, independently of the von Hippel Lindau protein. LW6 induces hypoxia selective apoptosis together with a reduction in the mitochondrial membrane potential^[4].

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

体内研究

In mice carrying xenografts of human colon cancer HCT116 cells, LW6 demonstrates strong anti-tumor efficacy in vivo and causes a decrease in HIF-1α expression in frozen-tissue immunohistochemical staining.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (57.40 mM; Need ultrasonic)

DMF : 17.24 mg/mL (39.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2962 mL	11.4808 mL	22.9616 mL
5 mM	0.4592 mL	2.2962 mL	4.5923 mL
10 mM	0.2296 mL	1.1481 mL	2.2962 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: 2.5 mg/mL (5.74 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.74 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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% corn oil
Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。