|3-(2-(4-(金刚烷-1-基)苯氧基)乙酰胺基)-4-羟基苯甲酸甲酯|CsnPharm

CAS No.: 934593-90-5

Methyl 3-(2-(4-(adamantan-1-yl)phenoxy)acetamido)-4-hydroxybenzoate Catalog No. CSN20474

Synonyms: HIF-1α inhibitor;LW8;HIF-1alpha inhibitor

LW6 is a HIF-1 inhibitor with an IC50 of 4.4 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HIF1

IC50:4.4μM
描述The response of mammalian cells to hypoxia is mediated by a family of transcription factors known as HIF (hypoxia-inducible factors). The subunits of HIF, HIF-1α can be degraded rapidly under normoxia. LW6 is a dual inhibitor of HIF-1α and MDH2, which can inhibit activity of HIF-1α with IC₅₀ value of 2.64 ± 0.16 μM (measured by HRE-luciferase activity). LW6 can potently inhibit HIF-1α accumulation by degrading HIF-1α on concentration of 10 μM in HCT116 cells under hypoxia, with no effect on transcription levels during hypoxia. LW6 inhibited the MDH2 activity in a concentration-dependent manner with IC₅₀ value of 6.3 μM, without affecting the MDH2 expression. This HIF-1α inhibitory activity of LW6 may due to the interaction and suppression of MDH2 (malate dehydrogenase 2, a 36 kDa mitochondrial enzyme that catalyzes the malate/NAD⁺ conversion to oxaloacetate/ NADH during the TCA cycle and functions as a respiratory substrate in the mitochondrial ETC) by LW6^[1]. The activity of LW6 against HIF-1α may also due to it promotes proteasomal degradation of HIF-1α via upregulation of VHL. Treatment with LW6 for 13 days, 20 mg/kg, QD, i.p., significantly inhibited HCT116 tumor growth up to 53.6% in a xenograft tumor model compared with the control group^[2].
作用机制The action of LW6 against HIF-1α may due to it can promote proteasomal degradation of HIF-1α via upregulation of VHL, as well as inhibit and bind to MDH2^[1]^[2].
动物研究
剂量
Rat (p.o.): 10 mg/kg^[3], 20 mg/kg^[4]; Mice^[2] (i.p.): 10 mg/kg, 20 mg/kg

给药途径
p.o., i.p.
参考文献

动物研究
剂量	Rat (p.o.): 10 mg/kg^[3], 20 mg/kg^[4]; Mice^[2] (i.p.): 10 mg/kg, 20 mg/kg
给药途径	p.o., i.p.

[1] Lee K, Ban HS, et al. Identification of malate dehydrogenase 2 as a target protein of the HIF-1 inhibitor LW6 using chemical probes. Angew Chem Int Ed Engl. 2013 Sep 23;52(39):10286-9.
[2] Lee K, Kang JE, 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

934593-90-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H29NO5

运输

蓝冰

分子量

435.51

别名

HIF-1α inhibitor;LW8;HIF-1alpha inhibitor;Hypoxia-Inducible Factor-1α Inhibitor;Hypoxia-Inducible Factor-1alpha Inhibitor;CAY-10585

溶解度

DMSO	13.0 mg/mL (29.8 mM)
Water	Insoluble
Ethanol	1.0 mg/mL (2.3 mM)

动物实验配方

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Methyl 3-(2-(4-(adamantan-1-yl)phenoxy)acetamido)-4-hydroxybenzoate Catalog No. CSN20474

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