LW6 (Synonyms: HIF-1α inhibitor; LW8)

目录号: HY-13671 纯度: 98.38%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

LW6 (HIF-1α inhibitor) 是新颖的 HIF-1 抑制剂，IC₅₀ 值为 4.4 μM，也是 MDH2 抑制剂。LW6 降低 HIF-1α 蛋白表达，而不影响 HIF-1β 表达。

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LW6 Chemical Structure

CAS No. : 934593-90-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥726	In-stock
1 mg	￥264	In-stock
5 mg	￥660	In-stock
10 mg	￥920	In-stock
25 mg	￥2000	In-stock
50 mg	￥3800	In-stock
100 mg	￥5700	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 26 篇科研文献

: LW6 purchased from MCE. Usage Cited in: Eur J Pharmacol. 2023 Apr 15;175725. [Abstract]; LW6 (10 μM; 48 h) reverses the hypoxia-induced decreased expression of Mfn2 and increased expression of HIF-1α in PASMCs.

: LW6 purchased from MCE. Usage Cited in: J Appl Genet. 2020 Feb;61(1):105-112. [Abstract]; The protein expression level of HIF1α was detected throughWestern blot analysis 48 h after treatment of LW6.

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HIF-1α HIF

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC₅₀ value of 4.4 μM, and it is also an inhibitor of MDH2. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.

IC₅₀ & Target

IC50: 4.4 μM (HIF-1)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
AGS	IC₅₀	0.7 μM Compound: 23	Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay	[PMID: 17328532]
HCCLM3	CC₅₀	> 50 μM Compound: 1; LW6	Cytotoxicity against human HCCLM3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HCCLM3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31556611]
HCT-116	IC₅₀	> 30 μM Compound: CAY10585	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 24900662]
HCT-116	IC₅₀	2.44 μM Compound: 1, LW6	Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay	[PMID: 23153200]
HCT-116	IC₅₀	4.4 μM Compound: LW6	Inhibition of HIF-1alpha in human HCT116 cells incubated for 12 hrs under hypoxic conditions by Western blotting and HRE-luciferase reporter assay Inhibition of HIF-1alpha in human HCT116 cells incubated for 12 hrs under hypoxic conditions by Western blotting and HRE-luciferase reporter assay	[PMID: 25356789]
HeLa	IC₅₀	> 30 μM Compound: CAY10585	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 24900662]
HeLa	IC₅₀	21 μM Compound: CAY10585	Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay	[PMID: 24900662]
Hep 3B2	IC₅₀	2.6 μM Compound: 23	Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay	[PMID: 17328532]
HepG2	IC₅₀	> 30 μM Compound: CAY10585	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 24900662]
PC-3	IC₅₀	> 30 μM Compound: CAY10585	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 24900662]

体外研究
(In Vitro)

LW6 影响 HIF-1α 蛋白的稳定性。LW6 促进野生型 HIF-1α 的降解，但不促进氧依赖性降解域羟基化位点处 P402A 和 P564A 修饰的 DM-HIF-1α 的降解。LW6 诱导 von Hippel-Lindau (VHL) 蛋白的表达，VHL 蛋白与脯氨酰羟基化的 HIF-1α 相互作用，进行蛋白酶体降解。在 LW6 存在的情况下，VHL 的敲低不会消除 HIF-1α 蛋白的积累，这表明 LW6 通过调节 VHL 表达来降解 HIF-1α^[2]。
在过表达 BCRP 的 MDCKII-BCRP 细胞中，LW6 显著增强了 BCRP 底物米托蒽醌的细胞积累。 LW6 浓度为 0.1-10 μM 时也会下调 BCRP 表达^[3]。
LW6 浓度为 20 μM 时，可抑制 A549 细胞中缺氧诱导的 HIF 1α 表达，且不依赖于 von Hippel Lindau 蛋白。LW6 可诱导缺氧选择性细胞凋亡，同时降低线粒体膜电位^[4]。

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

体内研究
(In Vivo)

在携带人类结肠癌 HCT116 细胞异种移植瘤的小鼠中，LW6 表现出有效的体内抗肿瘤功效，并在冷冻组织免疫组织化学染色中导致 HIF-1α 表达降低^[2]。

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

分子量

435.51

Formula

C₂₆H₂₉NO₅

CAS 号

934593-90-5

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (57.40 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

DMF 中的溶解度 : 17.24 mg/mL (39.59 mM; 超声助溶)

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

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

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); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.74 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.38%

选择批次：

Data Sheet (651 KB) SDS (393 KB)

COA (286 KB) RP-HPLC (256 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Naik R, et al. Synthesis and structure-activity relationship study of chemical probes as hypoxia induced factor-1α/malate dehydrogenase 2 inhibitors. J Med Chem. 2014 Nov 26;57(22):9522-38. [Content Brief]

[2]. Lee K, et al. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line. Biochem Pharmacol. 2010 Oct 1;80(7):982-9. [Content Brief]

[3]. Song JG, et al. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein. [Content Brief]

[4]. Sato M, et al. LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells. Mol Med Rep. 2015 Sep;12(3):3462-8. [Content Brief]

Cell Assay ^[2]	Inhibition of HIF-1a is assayed by a reporter assay using dualluciferase reporter assay system. HCT116 cells in 75-90% confluence are transiently co-transfected with pGL3-HRE-luciferase plasmid containing six copies of HREs from human VEGF genes and pRLSV40 encoding firefly renilla luciferase and incubated for 24 h. Cells are treated with LW6 or 17-AAG for 16 h before report assay. Luciferase activity is integrated over a 10 second period and measured using a luminometer^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice: The mice receive the following treatments using a dosing vehicle solution, containing 10% dimethylacetamide, 10% Cremophor EL and 80% of sodium carbonate buffer (pH 10), by intraperitoneal (i.p.) injection: group1(control group; six mice), vehicle solution; group2 (six mice), LW6 at a dose of 10 and 20mg/kg (QD); and group 3 (six mice), topotecan at a dose of 2mg/kg, (Q2D), which is the dose and dosing schedule that showed more than 60% inhibition of growth of HCT116 tumors. The treatments are continued for 13 days^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Naik R, et al. Synthesis and structure-activity relationship study of chemical probes as hypoxia induced factor-1α/malate dehydrogenase 2 inhibitors. J Med Chem. 2014 Nov 26;57(22):9522-38. [Content Brief] [2]. Lee K, et al. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line. Biochem Pharmacol. 2010 Oct 1;80(7):982-9. [Content Brief] [3]. Song JG, et al. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein. [Content Brief] [4]. Sato M, et al. LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells. Mol Med Rep. 2015 Sep;12(3):3462-8. [Content Brief]

LW6 相关分类

Cancer

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMF / DMSO	1 mM	2.2962 mL	11.4808 mL	22.9616 mL	57.4040 mL
	5 mM	0.4592 mL	2.2962 mL	4.5923 mL	11.4808 mL
	10 mM	0.2296 mL	1.1481 mL	2.2962 mL	5.7404 mL
	15 mM	0.1531 mL	0.7654 mL	1.5308 mL	3.8269 mL
	20 mM	0.1148 mL	0.5740 mL	1.1481 mL	2.8702 mL
	25 mM	0.0918 mL	0.4592 mL	0.9185 mL	2.2962 mL
	30 mM	0.0765 mL	0.3827 mL	0.7654 mL	1.9135 mL
DMSO	40 mM	0.0574 mL	0.2870 mL	0.5740 mL	1.4351 mL
DMSO	50 mM	0.0459 mL	0.2296 mL	0.4592 mL	1.1481 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LW6934593-90-5HIF-1α inhibitor LW8LW 6LW-6LW8LW 8LW-8HIF/HIF Prolyl-HydroxylaseApoptosisHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

LW6 (Synonyms: HIF-1α inhibitor; LW8)

Customer Review

MCE 顾客使用本产品发表的 26 篇科研文献