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/ Nordihydroguaiaretic acid

去甲二氢愈创木酸 /Nordihydroguaiaretic acid {[allProObj[0].p_purity_real_show]}

货号：A867405 同义名： NDGA;NSC 4291

Nordihydroguaiaretic Acid is a naturally occuring mTORC1 inhibitor.

Nordihydroguaiaretic acid 化学结构 CAS号：500-38-9
Nordihydroguaiaretic acid 化学结构
CAS号：500-38-9
Nordihydroguaiaretic acid 3D分子结构
CAS号：500-38-9
Nordihydroguaiaretic acid 化学结构 CAS号：500-38-9
Nordihydroguaiaretic acid 3D分子结构 CAS号：500-38-9
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Nordihydroguaiaretic acid 纯度/质量文件 产品仅供科研

货号：A867405 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 mTOR ↓ mTORC1 ↓ mTORC2 ↓ 其他靶点 纯度
AZD-8055 ++++

mTOR (truncated), IC50: 0.13 nM

mTOR (full length), IC50: 0.8 nM

 		99%+
Gedatolisib ++++

mTOR, IC50: 1.6 nM

 		98%
GSK1059615 ++

mTOR, IC50: 12 nM

 		98%
Vistusertib +++

mTOR, IC50: 2.8 nM

 		99%+
Torin 1 +++

mTOR, IC50: 4.32 nM

 		+++

mTORC1, IC50: 2 nM

 		++

mTORC2, IC50: 10 nM

 		DNA-PK 99%+
Dactolisib +++

mTOR (p70S6K), IC50: 6 nM

 		98+%
PI-103 +

mTOR, IC50: 30 nM

 		99%+
WAY-600 ++

mTOR, IC50: 9 nM

 		99%
Voxtalisib +

mTOR, IC50: 157 nM

 		99%+
PF-04691502 ++

mTOR, Ki: 16 nM

 		98+%
Onatasertib ++

mTOR, IC50: 16 nM

 		DNA-PK 99%+
Chrysophanol ✔ EGFR 98%
Samotolisib ✔ DNA-PK 99%+
Torkinib +++

mTOR, IC50: 8 nM

 		PDGFR,DNA-PK 99%+
Everolimus 99%+
WYE-354 +++

mTOR, IC50: 5 nM

 		98%
Tacrolimus ✔ 98%
PP121 ++

mTOR, IC50: 13 nM

 		VEGFR,PDGFR 99%+
Torin 2 ++++

mTOR, IC50: 0.25 nM

 		DNA-PK 99%+
Rapamycin ++++

mTOR, IC50: ~0.1 nM

 		98%
GDC-0349 +++

mTOR, Ki: 3.8 nM

 		98%
XL388 ++

mTOR, IC50: 9.9 nM

 		+++

mTORC1, IC50: 8 nM

 		+

mTORC2, IC50: 166 nM

 		99%+
WYE-687 +++

mTOR, IC50: 7 nM

 		98+%
Apitolisib +

mTOR, Ki app: 17 nM

 		98%+
WYE-132 ++++

mTOR, IC50: 0.19 nM

 		99%+
Sapanisertib ++++

mTOR, Ki: 1.4 nM

 		99%+
BGT226 maleate ✔ 99%+
ETP-46464 ++++

mTOR, IC50: 0.6 nM

 		DNA-PK 98%
PI3K-IN-1 +

mTOR, IC50: 157 nM

 		98+%
Zotarolimus +++

FKBP-12, IC50: 2.8 nM

 		99+%
OSI-027 +++

mTOR, IC50: 4 nM

 		+

mTORC1, IC50: 22 nM

 		+

mTORC2, IC50: 65 nM

 		99%+
Ridaforolimus ++++

mTOR, IC50: 0.2 nM

 		99%+
Temsirolimus +

mTOR, IC50: 1.76 μM

 		99%
CZ415 ++

mTOR, pIC50: 8.07

 		99%+
SF2523 +

mTOR, IC50: 280 nM

 		DNA-PK 99%+
KU-0063794 ++

mTORC1, IC50: ~10 nM

 		++

mTORC2, IC50: ~10 nM

 		99%+
Omipalisib ++++

mTORC1, Ki: 0.18 nM

 		++++

mTORC2, Ki: 0.3 nM

 		99%+
Palomid 529 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Nordihydroguaiaretic acid 生物活性

靶点

  • p300/CBP

  • lipoxygenase
描述 Nordihydroguaiaretic acid (NDGA), a natural dicatechol, a selective 5LOX inhibitor, was one of the most potent non-cytotoxic antagonists tested (IC50 8 +/- 3 mM). Oral NDGA (2500 p.p.m.) significantly extended lifespan and slowed motor dysfunction in this mouse, when administration was begun relatively late in life (90 days). NDGA extended median total lifespan of G93A-SOD1 mice by 10%, and life expectancy following start of treatment was extended by 32%[3]. Feeding ob/ob mice a chow diet supplemented with either low (0.83 g/kg diet) or high-dose (2.5 g/kg diet) NDGA for 16 wk significantly improved plasma triglyceride (TG), inflammatory chemokine levels, hyperinsulinemia, insulin sensitivity, and glucose intolerance[4]. NDGA suppresses NRP1 function by downregulating its expression, which leads to attenuated cell motility, cell adhesion to ECM and FAK signaling in cancer cells. Moreover, due to its cross-cell type activity on NRP1 suppression, NDGA also impairs angiogenesis function of endothelial cells and fibronectin assembly by fibroblasts, both of which are critical to promote metastasis. NDGA effectively suppresses tumor metastasis in nude mice model[5].

Nordihydroguaiaretic acid 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02575794 High Grade Glioma (III or IV) Phase 1 Recruiting December 15, 2022 United States, Alabama ... 展开 >> UAB Comprehensive Cancer Center Not yet recruiting Birmingham, Alabama, United States, 35294-3410 Contact: Thiru Pillay, RN    205-934-1842    thiru@uab.edu    Principal Investigator: Burt Nabors, MD          United States, California Jonsson Comprehensive Cancer Center at UCLA Not yet recruiting Los Angeles, California, United States, 90095 Contact: Timothy Cloughesy, MD    310-825-5321    TCloughesy@mednet.ucla.edu    Principal Investigator: Timothy Cloughesy, MD          United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Recruiting Baltimore, Maryland, United States, 21231 Contact: Quinn qta@jhmi.edu, RN    410-955-8837    qta@jhmi.edu    Contact: Trisha Surakus    410-502-9864    tsuraku1@jhmi.edu    Sub-Investigator: Matthias Holdhoff, MD          Principal Investigator: Stuart Grossman, MD          United States, Massachusetts Dana Farber Cancer Institute Not yet recruiting Boston, Massachusetts, United States, 02215 Contact: Jennifer Barrs    617-632-6119    JenniferA_Barrs@DFCI.HARVARD.EDU    Principal Investigator: Patrick Wen, MD          United States, Michigan Josephine Ford Cancer Center at Henry Ford Hospital Recruiting Detroit, Michigan, United States, 48202 Contact: Amy Williamson, RN       awillia12@hfhs.org    Contact: Emily Krozek, MHSA       Ekrozek1@hfhs.org    Principal Investigator: Tobias Walbert, MD          United States, North Carolina Wake Forest University Comprehensive Cancer Center Not yet recruiting Winston-Salem, North Carolina, United States, 27157 Contact: Clinical Trials Office    336-713-6771       Principal Investigator: Glenn Lesser, MD          United States, Ohio Cleveland Clinic Taussig Cancer Center Not yet recruiting Cleveland, Ohio, United States, 44195 Contact: Cancer Center-Cares    216-444-7923       Sub-Investigator: David Peereboom, MD          United States, Pennsylvania Abrams Cancer Center of the University of Pennsylvania Not yet recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Clinical Trials Office-Abrams Cancer Center    800-474-9892       Principal Investigator: Arati Desai, MD          Hillman Cancer Center at University of Pittsburgh Cancer Institute Not yet recruiting Pittsburgh, Pennsylvania, United States, 15232 Contact: Clinical Trials Office - UPMC Cancer Centers    412-647-8073       Principal Investigator: Frank Lieberman, MD 收起 <<
NCT00664677 Leukemias Acu... 展开 >>te Myeloid Leukemia (AML) Acute Lymphocytic Leukemia (ALL) Adult T Cell Leukemia (ATL) Chronic Myeloid Leukemia (CML-BP) Chronic Lymphocytic Leukemia (CLL) Myelodysplastic Syndrome (MDS) Chronic Myelomonocytic Leukemia (CMML) 收起 << Phase 1 Terminated(Funding constraints... 展开 >>) 收起 << - United States, North Carolina ... 展开 >> UNC, Lineberger Comprehensive Cancer Center Chapel Hill, North Carolina, United States, 27599 收起 <<
NCT00664586 Refractory Solid Tumors ... 展开 >> Lymphoma 收起 << Phase 1 Terminated(Funding constraints... 展开 >>) 收起 << - United States, Tennessee ... 展开 >> The Sarah Cannon Cancer Center Nashville, Tennessee, United States, 37203 收起 <<

Nordihydroguaiaretic acid 参考文献

[1]Zhang H, Shen WJ, et al. Nordihydroguaiaretic acid improves metabolic dysregulation and aberrant hepatic lipid metabolism in mice by both PPARα-dependent and -independent pathways. Am J Physiol Gastrointest Liver Physiol. 2013 Jan 1;304(1):G72-86.

[2]Zhang Y, Xu S, et al. mTORC1 is a target of nordihydroguaiaretic acid to prevent breast tumor growth in vitro and in vivo. Breast Cancer Res Treat. 2012 Nov;136(2):379-88.

[3]West M, Mhatre M, Ceballos A, Floyd RA, Grammas P, Gabbita SP, Hamdheydari L, Mai T, Mou S, Pye QN, Stewart C, West S, Williamson KS, Zemlan F, Hensley K. The arachidonic acid 5-lipoxygenase inhibitor nordihydroguaiaretic acid inhibits tumor necrosis factor alpha activation of microglia and extends survival of G93A-SOD1 transgenic mice. J Neurochem. 2004 Oct;91(1):133-43

[4]Zhang H, Shen WJ, Cortez Y, Kraemer FB, Azhar S. Nordihydroguaiaretic acid improves metabolic dysregulation and aberrant hepatic lipid metabolism in mice by both PPARα-dependent and -independent pathways. Am J Physiol Gastrointest Liver Physiol. 2013 Jan 1;304(1):G72-86

[5]Li X, Fan S, Pan X, Xiaokaiti Y, Duan J, Shi Y, Pan Y, Tie L, Wang X, Li Y, Li X. Nordihydroguaiaretic acid impairs prostate cancer cell migration and tumor metastasis by suppressing neuropilin 1. Oncotarget. 2016 Dec 27;7(52):86225-86238

Nordihydroguaiaretic acid 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.54mL

3.31mL

1.65mL

33.07mL

6.61mL

3.31mL

Nordihydroguaiaretic acid 技术信息

CAS号500-38-9
分子式C18H22O4
分子量 302.36
别名 NDGA;NSC 4291
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 250 mg/mL(826.82 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Nordihydroguaiaretic acid | NDGA;NSC 4291 | Lipoxygenase Inhibitor | mTOR | AmBeed-信号通路专用抑制剂 | Nordihydroguaiaretic acid 纯度/质量文件 | Nordihydroguaiaretic acid 亚型比较 | Nordihydroguaiaretic acid 生物活性 | Nordihydroguaiaretic acid 临床数据 | Nordihydroguaiaretic acid 参考文献 | Nordihydroguaiaretic acid 实验方案 | Nordihydroguaiaretic acid 技术信息

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