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14

抑制剂 & 化合物

4

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Cat. No. Product Name Target Signaling Pathways
T11752 Keap1-Nrf2-IN-1

Keap1Nrf2-IN-1

Src Angiogenesis; Tyrosine Kinase/Adaptors
Keap1Nrf2 IN-1 activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models. Keap1Nrf2 IN-1 is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (
T12253 Nrf2-IN-1

Others; Nrf2 Immunology/Inflammation; Others
Nrf2-IN-1Nrf2抑制剂,可用于研究急性髓性白血病药物。
T39514 Keap1-Nrf2-IN-3

Keap1-Nrf2-IN-3

Keap1-Nrf2-IN-3 is a KEAP1:NRF2 protein protein interaction inhibitor, and with a K d value of 2.5 nM for KEAP1 protein.
T64218 Keap1-Nrf2-IN-1 TFA

Keap1-Nrf2-IN-1 TFA (compound35) 是一种 Keap1-Nrf2 蛋白-蛋白相互作用抑制剂 (IC50: 43 nM),可以激活 Nrf2 调节的细胞保护反应。在细胞和体内模型中。Keap1-Nrf2-IN-1 TFA 能够拮抗对乙酰氨基酚诱导的肝损伤。
T78841 Nrf2-IN-3

Nrf2-IN-3 (Compound R16) 为Nrf2抑制剂,与KEAP1突变体 (G333C mKEAP1) 结合,能够恢复受损的KEAP1/NRF2相互作用。该化合物通过修复mKEAP1/NRF2复合物,增加KEAP1突变癌细胞对Cisplatin和Gefitinib的敏感性。
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。
T79698 S217879

S217879是一种选择性高效的NRF2激活剂,能够破坏KEAP1-NRF2之间的相互作用,从而强有力地激活NRF2通路。它可应用于非酒精性脂肪性肝炎(NASH)的研究领域。
T74600 Keap1-Nrf2-IN-9

Keap1-Nrf2-IN-9(compound 11)是一种有效Keap1-Nrf2PPI抑制剂,IC50为0.575 µM。该化合物能够提升Nrf2靶基因表达,涉及血红素加氧酶1 (Hmox1)、谷胱甘肽S转移酶P (GstP) 以及谷氨酸-半胱氨酸连接酶的催化(Gclc)与调节(Gclm)亚基。在ARPE19细胞中,Keap1-Nrf2-IN-9展现出无细胞毒活性。
TP2109 TAT 14

Nrf2 Immunology/Inflammation
TAT-14 是 由14 个氨基酸组成的多肽,是 Nrf2激活因子,表现出抗炎活性。它通过靶向 Nrf2Keap1 的结合位点而非 Nrf2 mRNA 表达来提高 Nrf2 蛋白水平。
T78697 Keap1-Nrf2-IN-15

Keap1-Nrf2-IN-15 (Compound 24a) 作为Keap1-Nrf2蛋白-蛋白相互作用抑制剂,其FP试验与TR-FRET试验的IC50值分别为77 nM和2.5 nM,显示出高效的抑制活性。
T72687 Keap1-Nrf2-IN-11

Keap1-Nrf2-IN-11Keap1-Nrf2抑制剂,KD2值达0.21 nM。该化合物可有效抑制ROS及NO的生成,并降低TNF-α的表达。通过促进Nrf2的核内转移,Keap1-Nrf2-IN-11对炎症具有调节作用,适用于抗炎研究。
T61688 Nrf2 activator-2

Nrf2 activator-2 (referred to as compound O15), an Osthole derivative, is a highly potent Nrf2 agonist exhibiting an EC 50 of 2.9 μM in 293 T cells. By effectively disrupting the binding between Keap1 and Nrf2, Nrf2 activator-2 activates the Nrf2 pathway. Furthermore, this compound significantly reduces the ubiquitination of Nrf2 in cells, indicating its potential in regulating Nrf2 activity [1].
T61773 Keap1-Nrf2-IN-4

Keap1-Nrf2-IN-4, a powerful neddylation inhibitor, demonstrates significant anti-proliferation activity against MGC-803 cells (IC50 = 2.55 μM), effectively impeding their migration and inducing apoptosis. Additionally, it effectively inhibits tumor growth while exhibiting minimal toxicity [1].
T64214 NXPZ-2

NXPZ-2 是一种口服具有活力的 Keap1-Nrf2protein–protein interaction(PPI) 抑制剂 (Ki: 95 nM, EC50: 120 and 170 nM)。NXPZ-2 能够上调Nrf2含量,并促进其从细胞质向细胞核的易位,表现出对氧化应激的抑制作用。NXPZ-2 能够剂量依赖性地缓解 Aβ[1-42]诱导的认知紊乱,能够提高神经元数量和功能,增强阿尔茨海默病 (AD) 小鼠脑组织的病理改变情况。NXPZ-2 具有潜力进行 Keap1-Nrf2 PPI 抑制剂和 AD 相关的疾病的研究。

化合物

Keap1-Nrf2-IN-1
Cat.No: T11752
Synonym: Keap1Nrf2-IN-1
Target: Src
Nrf2-IN-1
Cat.No: T12253
Synonym:
Target: Others, Nrf2
Keap1-Nrf2-IN-3
Cat.No: T39514
Synonym: Keap1-Nrf2-IN-3
Target:
Keap1-Nrf2-IN-1 TFA
Cat.No: T64218
Synonym:
Target:
Nrf2-IN-3
Cat.No: T78841
Synonym:
Target:
Keap1-Nrf2-IN-10
Cat.No: T81984
Synonym:
Target:
S217879
Cat.No: T79698
Synonym:
Target:
Keap1-Nrf2-IN-9
Cat.No: T74600
Synonym:
Target:
TAT 14
Cat.No: TP2109
Synonym:
Target: Nrf2
Keap1-Nrf2-IN-15
Cat.No: T78697
Synonym:
Target:
Keap1-Nrf2-IN-11
Cat.No: T72687
Synonym:
Target:
Nrf2 activator-2
Cat.No: T61688
Synonym:
Target:
Keap1-Nrf2-IN-4
Cat.No: T61773
Synonym:
Target:
NXPZ-2
Cat.No: T64214
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN5171 Tricetin

Apoptosis; Others; Nrf2 Apoptosis; Immunology/Inflammation; Others
Tricetin 是一种从石榴中分离出的类黄酮。TricetinKeap1-Nrf2 蛋白相互作用(PPI)的强效竞争性抑制剂,通过激活 Nrf2/HO-1 信号通路和阻止线粒体依赖性细胞凋亡通路,保护帕金森病患免受 6-OHDA 诱导的神经毒性的影响。Tricetin 通过 Akt/GSK-1β途径抑制鼻咽癌的迁移和指示性蛋白酶早老素-1(PS-1)表达。Tricetin 抑制由Egr-1介导的氧化LDL 诱导的内皮炎症,保护大鼠软骨细胞免受IL-1β诱导的炎症和细胞凋亡。
T6S0525 Farrerol

ERK; p38 MAPK; Akt Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling
Farrerol 是一种杜鹃花的生物活性成分,具有抗氧化、抗肿瘤、抗炎、神经保护和肝保护等多种功能。
T75485 Dehydrobruceine B

Dehydrobruceine B 是一种苦木素,可从鸦胆子 (Brucea javanica) 中分离得到。Dehydrobruceine B 与 Cisplatin 通过线粒体途径,协同诱导细胞凋亡 (apoptosis)。Dehydrobruceine B 还增加凋亡诱导因子 (AIF) 和 Bax 表达,抑制 Keap1-Nrf2
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

天然产物

Tricetin
Cat.No: TN5171
Synonym:
Target: Apoptosis, Others, Nrf2
Farrerol
Cat.No: T6S0525
Synonym:
Target: ERK, p38 MAPK, Akt
Dehydrobruceine B
Cat.No: T75485
Synonym:
Target:
Dehydroglyasperin C
Cat.No: TN3806
Synonym:
Target: ERK, IκB/IKK, p38 MAPK, TNF, NF-κB, Akt, COX, PI3K, NADPH, DNA/RNA Synthesis, Nrf2, JNK, Autophagy
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