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10

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13799	NQO1 substrate	NADPH	Metabolism
	NQO1 substrate 是一种高效的 NQO1 底物，具有潜在的抗肿瘤活性，可用于研究白血病。
T16342	KL1333 NQO1 activator 1	NADPH; Mitochondrial Metabolism	Metabolism
	KL1333 (NQO1 activator 1) 是口服NAD+调节剂，与 NAD(P)H: 醌氧化还原酶 1 作为底物反应。它改善线粒体脑肌病、乳酸酸中毒和中风样发作成纤维细胞的能量代谢和线粒体功能障碍。它对顺铂诱导的小鼠耳蜗培养耳毒性的保护作用。
T6798	Tretazicar 5-Aziridino-2,4-dinitrobenzamide,CB1954,NSC 115829	DNA Alkylator/Crosslinker; DNA Alkylation	DNA Damage/DNA Repair
	Tretazicar (NSC-115829) 是一种抗肿瘤前药，由 NAD(P)H 醌氧化还原酶 2 激活。它在酶促活化后生成细胞毒性双功能烷基剂，可以形成 DNA-DNA 链间交联。
T0153	Oltipraz 吡噻硫酮,NSC 347901,RP 35972	HIF/HIF Prolyl-Hydroxylase; HIV Protease; Reverse Transcriptase; Nrf2; HIF	Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; Metabolism; Microbiology/Virology; Proteases/Proteasome
	Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活，IC50为 10 μM，浓度 ≥ 10 μM 时完全消除 HIF-1α诱导。
T38901	Isobutyl-deoxynyboquinone IB-DNQ,Isobutyl-deoxynyboquinone
	Isobutyl-deoxynyboquinone (IB-DNQ) is a selective substrate for NAD(P)H: quinone oxidoreductase (NQO1) and is utilized in anticancer research.
T64057	Nampt-IN-8
	Nampt-IN-8 是一种 NAMPT 抑制剂 (IC50: 0.183 μM)，也是较好的 NQO1 底物。Nampt-IN-8 能够诱导活性氧 (ROS) 产生，并促使细胞凋亡 (apoptosis) 。
T61186	Antitumor agent-57
	Antitumor agent-57 (Compound 3o) is a potent NQO1-directed antitumor compound. It effectively inhibits tumor cell growth, induces ROS generation, and promotes cell apoptosis [1].
T36358	Diminutol
	Diminutol is a cell-permeable purine derivative that inhibits the NADP-dependent oxidoreductase, NQO1 (Ki = 1.72 μM), to destabilize microtubules and disrupt mitosis. At 50 μM, it directly affects tubulin polymerization in Xenopus egg extracts without interfering with the activity of Cdk1, DNA replication, or actin polymerization.
T81984	Keap1-Nrf2-IN-10
	Keap1-Nrf2-IN-10（compound 15）作为NQO1诱导剂展现出高效性。该化合物能够在γ辐照小鼠中抑制氧化应激，具体机制是通过降低肝脏MDA、ROS及NQO1水平。此外，Keap1-Nrf2-IN-10能显著提升受γ射线照射小鼠的生存率。
T83001	Antitumor agent-67
	Antitumor agent-67 (compound 3) 是一种高选择性抗肿瘤化合物，针对癌细胞具备显著选择性毒性，且对正常细胞损害低。该化合物经 NQO1 激活后，有效地释放鬼臼毒素（Podophyllotoxin），以消灭肿瘤细胞。在 HepG2 异种移植肿瘤模型中，Antitumor agent-67 展现出强效的肿瘤抑制能力而无显著毒副作用。

化合物

NQO1 substrate

Cat.No: T13799

Target: NADPH

Cat.No: T16342

Synonym: NQO1 activator 1

Target: NADPH, Mitochondrial Metabolism

Cat.No: T6798

Synonym: 5-Aziridino-2,4-dinitrobenzamide,CB1954,NSC 115829

Target: DNA Alkylator/Crosslinker, DNA Alkylation

Cat.No: T0153

Synonym: 吡噻硫酮,NSC 347901,RP 35972

Target: HIF/HIF Prolyl-Hydroxylase, HIV Protease, Reverse Transcriptase, Nrf2, HIF

Isobutyl-deoxynyboquinone

Cat.No: T38901

Synonym: IB-DNQ,Isobutyl-deoxynyboquinone

Cat.No: T64057

Antitumor agent-57

Cat.No: T61186

Cat.No: T36358

Keap1-Nrf2-IN-10

Cat.No: T81984

Antitumor agent-67

Cat.No: T83001

Cat. No.	Product Name	Target	Signaling Pathways
T5S1805	5,7-Dihydroxychromone 5,7-Dihydroxy-4H-Chromen-4-One,5,7-二羟基色酮,5,7-二羟基色原酮	Others; Virus Protease; PARP; Caspase; Nrf2	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Microbiology/Virology; Others; Proteases/Proteasome
	5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) 是一种Cudrania tricuspidata 的提取物，通过激活 Nrf2/ARE 信号对 6-OHDA 诱导的氧化应激和细胞凋亡发挥神经保护作用。它抑制 6-OHDA 诱导的 SH-SY5Y 细胞中活化的caspase-3，caspase-9以及切割的PARP 表达。
TN2272	Tigloylgomisin H	Nrf2	Immunology/Inflammation
	Tigloylgomisin H 是分离自S. chinensis 果实中的木酚素。Tigloylgomisin H 能诱导小鼠肝癌细胞 Hepa1c1c7 中醌还原酶活性。Tigloylgomisin H 是单功能诱导剂，通过 Nrf2-ARE 途径特异性上调 II 期解毒酶 NQO1。Tigloylgomisin H 是潜在的肝癌预防剂。
T6S2099	Geraniin	Antioxidant; TNF	Apoptosis; oxidation-reduction
	Geraniin 是一种肿瘤坏死因子α释放抑制剂，其IC50值为 43 μM，具有抗肿瘤、抗炎和抗高血糖活性。
T0809	Dicoumarol Dicumarol,双羟香豆素,双香豆素	Dehydrogenase; NADPH; PDK	Metabolism; PI3K/Akt/mTOR signaling
	Dicoumarol (Dicumarol) 是一种 NAD(P)H: 醌氧化还原酶 1 和PDK1的抑制剂，它们的IC50值分别为 0.37 和 19.42 μM。
T82305	Glucoarabin
	Glucoarabin是一种硫代葡萄糖苷，具备生物活性。在Hepa1c1c7细胞内，Glucoarabin的水解产物能够上调NQO1，而对细胞色素P450 (CYP) 1A1的活性无显著作用。
TN3806	Dehydroglyasperin C	ERK; IκB/IKK; p38 MAPK; TNF; NF-κB; Akt; COX; PI3K; NADPH; DNA/RNA Synthesis; Nrf2; JNK; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint; Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Metabolism; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling
	Dehydroglyasperin C is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C possesses potent antioxidant, cancer chemopreventive, and neuroprotective activities, it has protective effects against chronic diseases
TN1543	Cynaropicrin	IL Receptor; Others; TNF	Apoptosis; Immunology/Inflammation; Others
	Cynaropicrin is a potent activator of the AhR-Nrf2-Nqo1 pathway, and could therefore be applied to prevention of UVB-induced photo aging; it may be a potential anticancer agent against some leukocyte cancer cells such as lymphoma or leukemia, through pro-

天然产物

5,7-Dihydroxychromone

Cat.No: T5S1805

Synonym: 5,7-Dihydroxy-4H-Chromen-4-One,5,7-二羟基色酮,5,7-二羟基色原酮

Target: Others, Virus Protease, PARP, Caspase, Nrf2

Tigloylgomisin H

Cat.No: TN2272

Target: Nrf2

Cat.No: T6S2099

Target: Antioxidant, TNF

Cat.No: T0809

Synonym: Dicumarol,双羟香豆素,双香豆素

Target: Dehydrogenase, NADPH, PDK

Cat.No: T82305

Dehydroglyasperin C

Cat.No: TN3806

Target: ERK, IκB/IKK, p38 MAPK, TNF, NF-κB, Akt, COX, PI3K, NADPH, DNA/RNA Synthesis, Nrf2, JNK, Autophagy

Cat.No: TN1543

Target: IL Receptor, Others, TNF

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