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17

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8081 LC3-mHTT-IN-AN1

Others; Autophagy; ATTECs Autophagy; Others; PROTAC
LC3-mHTT-IN-AN1 是一种 mHTT-LC3 接头化合物,可与突变亨廷顿蛋白 (mHTT) 和 LC3B 相互作用。 它将 mHTT 靶向自噬体以等位基因选择性方式降低培养的亨廷顿病小鼠神经元中的 mHTT 水平。
T8903 Retro-2

Retro 2,2-{[(5-methyl-2-thienyl)methylene]amino}

Others; Virus Protease; Parasite; Autophagy Autophagy; Microbiology/Virology; Others
Retro-2 (2-{[(5-methyl-2-thienyl)methylene]amino}) 是一种植物毒素蓖麻毒素抑制剂,它保护 HeLa 细胞免受蓖麻毒素、Stx1 和 Stx2 的侵害,选择性地阻断早期内体蛋白质-高尔基体界面处的逆行毒素运输。
T116970 TLC3407-3786

MMV665916 是一种喹唑啉二酮衍生物,是一种抗疟药。MMV665916 对恶性疟原虫 FcB1 菌株具有显著的抗疟原虫生长抑制活性,EC50值为 0.4 μM,并呈现出高选择性指数 (SI>250)。
T36279 VH 032 amide-alkylC3-amine

VH 032 amide-alkylC3-amine

Functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development; incorporates an E3 ligase ligand plus an alkyl C3 linker and terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.
T36278 VH 032 amide-alkylC3-acid

VH 032 amide-alkylC3-acid

Functionalized von-Hippel-Lindau protein ligand (VHL) for research and development; incorporates an E3 ligase ligand plus alkylC3 linker with terminal carboxylic acid ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules.
T61871 DC-LC3in-D5

DC-LC3in-D5 is a chemical compound that functions as an autophagy inhibitor by diminishing the process of LC3B lipidation. It forms a binding association with LC3B, disrupting the LC3B-LBP2 interaction with an IC50 of 200 nM. This compound, DC-LC3in-D5, exhibits potential for application in anti-HCV or combination cancer treatments by effectively inhibiting autophagy [1].
T36250 Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine

Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine

Functionalized cereblon ligand for PROTAC research and development; incorporates an E3 ligase ligand plus an alkylC1-PEG3-alkylC3 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.
T23716 AMDE-1

AMDE 1

Autophagy Autophagy
AMDE-1 是一种自噬调节剂,以 Atg5 依赖性方式触发自噬。 AMDE-1 将 Atg16 募集到自噬体前位点并导致 LC3 脂化。
T19188 ALLO-1

Autophagy Autophagy
ALLO-1 is a crucial autophagy receptor responsible for facilitating the formation of autophagosomes around paternal organelles. It directly interacts with the worm LC3 homologue, LGG-1, through its LC3-interacting region (LIR) motif.
T83945 XIE62-1004

XIE62-1004 是一种促进p62与LC3相互作用的诱导剂。通过与p62的ZZ域结合,导致p62自我聚集并与自噬体膜上的LC3相互作用;促进货物蛋白被送往自噬体以便降解。在体外及体内以浓度依赖和时间依赖的方式活性,并特异性针对野生型p62。在体外诱导突变型huntingtin的降解。也可以用于AUTAC蛋白质降解系统,通过p62自我聚集及与LC3的相互作用来诱导自噬。
T27187 DK-1-49

DK-1-49 is an autophagonizer. It causes accumulation of autophagy-associated LC3-II and enhanced levels of autophagosomes and acidic vacuoles.
T71151 Z36

Z36 is a novel Bcl-xL inhibitor, upregulating the expression levels of FAM134B, LC3, and Atg9, inducing autophagy along with autophagic cell death, resulting in ER stress and the unfolded protein response (UPR).
T76599 Ac-Leu-Val-Lys-Aldehyde

Ac-Leu-Val-Lys-Aldehyde 是有效的组织蛋白酶 B (cathepsin B) 抑制剂,其 IC50 值为 4 nM。该化合物能显着降低喹啉酸引起的纹状体细胞死亡,并促使 LC3-II 积累。
T35747 Quinacrine analog 34

Quinacrine is a compound with multiple actions that is commonly used as an anti-protozoal agent. It has also been shown to be a highly potent autophagy inhibitor, although the dose required to achieve this effect is considerably cytotoxic (LD50 = 2.5 μM). Quinacrine analog 34 is a derivative of quinacrine that was designed with an improved cell viability profile (LD50 = 27 μM) to inhibit autophagy. At a minimum concentration of 0.5 μM, this compound has been shown to increase the protein levels ...
T83765 Dendrogenin A

​DDA

Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物,通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在,但在多种乳腺癌细胞或黑色素瘤细胞中未发现,且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM),但也是LXR的部分激动剂,在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ,而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外,DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平,并在2...
T60453 TrxR-IN-3

TrxR-IN-3 (Compound 2c) 是TrxR 的有效抑制剂。TrxR-IN-3 对五种人类癌细胞系表现出强大的抗增殖活性,特别是对乳腺肿瘤细胞。TrxR-IN-3 增加 ROS 水平并通过调节乳腺癌细胞中细胞凋亡相关蛋白的表达导致明显的细胞凋亡。TrxR-IN-3 还通过促进 LC3-II 和 Beclin-1 的表达并减少 LC3-I 和 p62 蛋白的表达,来触发自噬体和自溶酶体的形成。
T61580 Autophagy inducer 3

Autophagy Inducer 3 is a chemical compound that exhibits autophagy-induced activity, specifically inducing robust autophagic cell death in various cancer cells while sparing normal cells. This compound induces lethal autophagy through the formation of distinct autophagic vacuoles, LC3 puncta formation, and upregulation of signature autophagy markers such as Beclin and Atg family proteins [1].

化合物

LC3-mHTT-IN-AN1
Cat.No: T8081
Synonym:
Target: Others, Autophagy, ATTECs
Retro-2
Cat.No: T8903
Synonym: Retro 2,2-{[(5-methyl-2-thienyl)methylene]amino}
Target: Others, Virus Protease, Parasite, Autophagy
TLC3407-3786
Cat.No: T116970
Synonym:
Target:
VH 032 amide-alkylC3-amine
Cat.No: T36279
Synonym: VH 032 amide-alkylC3-amine
Target:
VH 032 amide-alkylC3-acid
Cat.No: T36278
Synonym: VH 032 amide-alkylC3-acid
Target:
DC-LC3in-D5
Cat.No: T61871
Synonym:
Target:
Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine
Cat.No: T36250
Synonym: Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine
Target:
AMDE-1
Cat.No: T23716
Synonym: AMDE 1
Target: Autophagy
ALLO-1
Cat.No: T19188
Synonym:
Target: Autophagy
XIE62-1004
Cat.No: T83945
Synonym:
Target:
DK-1-49
Cat.No: T27187
Synonym:
Target:
Z36
Cat.No: T71151
Synonym:
Target:
Ac-Leu-Val-Lys-Aldehyde
Cat.No: T76599
Synonym:
Target:
Quinacrine analog 34
Cat.No: T35747
Synonym:
Target:
Dendrogenin A
Cat.No: T83765
Synonym: ​DDA
Target:
TrxR-IN-3
Cat.No: T60453
Synonym:
Target:
Autophagy inducer 3
Cat.No: T61580
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5070 LC3-mHTT-IN-AN2

5,7-二羟基-4-苯基香豆素,5,7-Dihydroxy-4-phenylcoumarin

Antibacterial; Autophagy; ATTECs Autophagy; Microbiology/Virology; PROTAC
LC3-mHTT-IN-AN2 (5,7-Dihydroxy-4-phenylcoumarin) 是一种 mHTT-LC3 接头化合物,可与突变亨廷顿蛋白(mHTT) 和 LC3B 相互作用。 它将 mHTT 靶向自噬体以等位基因选择性方式降低培养的亨廷顿病小鼠神经元中的 mHTT 水平。它存在于西番莲植物中,具有抗菌活性。
T1152 Albendazole

SKF-62979,阿苯达唑

HIF/HIF Prolyl-Hydroxylase; Microtubule Associated; Antibiotic; Parasite Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism; Microbiology/Virology
Albendazole (SKF-62979) 是一种广谱抗寄生虫剂,具有高效,低宿主毒性的特点。 它用于研究人类和动物的胃肠道寄生虫。
T8166 Pennogenin 3-O-beta-chacotrioside

偏诺皂苷元-3-O-Α-L-吡喃鼠李糖-(1→4)[Α-L-吡喃鼠李糖基](1→2)-Β-D-葡萄糖苷

Autophagy Autophagy
Pennogenin 3-O-beta-chacotrioside 是从七叶一枝花中分离得到的一种天然产物,具有抗结肠癌活性。它可以调节自噬,增加自噬相关蛋白 LC3 和 Beclin-1 的表达。

天然产物

LC3-mHTT-IN-AN2
Cat.No: T5070
Synonym: 5,7-二羟基-4-苯基香豆素,5,7-Dihydroxy-4-phenylcoumarin
Target: Antibacterial, Autophagy, ATTECs
Albendazole
Cat.No: T1152
Synonym: SKF-62979,阿苯达唑
Target: HIF/HIF Prolyl-Hydroxylase, Microtubule Associated, Antibiotic, Parasite
Pennogenin 3-O-beta-chacotrioside
Cat.No: T8166
Synonym: 偏诺皂苷元-3-O-Α-L-吡喃鼠李糖-(1→4)[Α-L-吡喃鼠李糖基](1→2)-Β-D-葡萄糖苷
Target: Autophagy
TargetMol Loading
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