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Search Results for " autophagic "

37

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T18968	Dansylcadaverine Monodansyl cadaverine,丹酰尸胺	Others; Autophagy	Autophagy; Others
	Dansylcadaverine (Monodansyl cadaverine) 是谷氨酰胺转胺酶的高亲和力底物，能阻断受体介导的多种配体的内吞作用。它是一种用于标记自噬空泡的荧光探针。
T8322	BL-918	Autophagy	Autophagy
	BL-918 是一种 UNC-51 样激酶 1 的有效激活剂，EC50 为 24.14 nM。它通过靶向 ULK 复合物发挥其细胞保护性自噬作用。它有用于帕金森氏病的研究潜力。
T7882	Indomethacin farnesil 吲哚美辛法呢酯,Infree	Others; COX; Autophagy	Autophagy; Immunology/Inflammation; Neuroscience; Others
	Indomethacin farnesil (Infree) 是具有口服活性的 Indomethacin 前药，可通过干扰溶酶体的正常功能来破坏自噬流，有抗炎和抗风湿作用。它是一种可透过血脑屏障的，非选择性的 COX1和 COX2抑制剂，在 CHO 细胞中，对人 COX-1 和 COX-2 的IC50值分别为 18 nM 和 26 nM。
T41286	N6-Isopentenyladenosine	Endogenous Metabolite; Autophagy	Autophagy; Metabolism
	N6-Isopentenyladenosine 是甲羟戊酸途径的终产物，是一种具有抗黑色素瘤活性的自噬抑制剂。 N6-Isopentenyladenosine 是一种在细胞分裂素中发现的 RNA 修饰，可调节植物生长/分化，提高翻译的效率和准确性。
T9541	CTB Cholera Toxin B subunit	Epigenetic Reader Domain	Chromatin/Epigenetic
	CTB (Cholera Toxin B subunit) 是一种 p300 组蛋白乙酰转移酶的激活剂，可诱导 MCF-7 细胞凋亡。
T1434	Clarithromycin A-56268,克拉霉素	P450; ribosome; MRP; Antibacterial; Antibiotic; Autophagy	Autophagy; Immunology/Inflammation; Metabolism; Microbiology/Virology
	Clarithromycin (A-56268) 具有广谱的抗菌活性。它抑制 CYP3A4催化的三唑仑 α-羟基化，IC50(Ki) 值为 56 (43) μM。它抑制 HERG 钾电流。它可削弱连接 hERG1 和 PI3K 的信号通路影响自噬流。
T9207	GW406108X GW108X	Kinesin; Autophagy	Autophagy; Cytoskeletal Signaling
	GW406108X (GW108X) 是一种 Kif15 抑制剂，在 ATPase 测定中的 IC50 为 0.82 uM。它也是一种 ULK1 激酶抑制剂，pIC50 值为 6.37(427 nM)，可阻断自噬通量。
T60036	ML-SA5	Autophagy	Autophagy
	ML-SA5 是一种 MCOLN1 激动剂，通过扰乱自噬体和溶酶体之间的融合来阻止自噬通量。
T5211	NSC 185058 NSC185058	Cysteine Protease; Autophagy	Autophagy; Proteases/Proteasome
	NSC 185058 是一种半胱氨酸蛋白酶 ATG4B 抑制剂，可抑制自噬。
T11142	EACC	Autophagy	Autophagy
	EACC 是自噬的可逆抑制剂，可阻断自噬通量。它对自噬体特异性的 SNARE Stx17 易位具有选择性抑制作用，从而阻止自噬体与溶酶体的融合。
T9583	HJ-PI01 N-Acetylphenoxazine,10-acetylphenoxazine	Pim	Chromatin/Epigenetic; JAK/STAT signaling
	HJ-PI01 (HJ-PI01) 是一种 Pim-2 抑制剂。它在三阴性人乳腺癌中诱导细胞凋亡和自噬性细胞死亡。
T1908	MHY1485	mTOR; Autophagy	Autophagy; PI3K/Akt/mTOR signaling
	MHY1485 是一种 mTOR 激活剂。它通过抑制自噬体和溶酶体之间的融合来抑制自噬过程，导致 LC3II 蛋白的积累和自噬体增大。
T9169	MPP+ iodide	Mitochondrial Metabolism; Autophagy	Autophagy; Metabolism
	MPP+ iodide 是一种 5-羟色胺转运体的高亲和力底物，也是一种神经毒素 MPTP 的有毒代谢物，通过选择性破坏黑质多巴胺能神经元，在动物模型中引起帕金森病症状。它被多巴胺转运体吸收进入多巴胺能神经元，通过影响呼吸链复合体 I 对线粒体发挥神经毒性作用。
T69365	HMS607P03
	HMS607P03 is an activator of SIRT1 which induces autophagic cell death via the AMPK-mTOR-ULK complex and induces mitophagy by the SIRT1-PINK1-Parkin pathway. HMS607P03 downregulates 14-3-3γ, catalase, profilin-1, and HSP90α.
T31411	DHA-37 DHA 37
	DHA-37 is an inducer of autophagic cell death through upregulation of HMGB1 in A549 cells.
T26938	CAA0225 CAA 0225,CAA-0225
	CAA0225 is a selective inhibitor of cathepsin L. CAA0225 is a probe for autophagic proteolysis.
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].
T4569L	Lucanthone hydrochloride Lucanthone HCl
	Lucanthone hydrochloride is a novel acridine derivative which supresses autophagic degradation and triggers apoptosis in colon cancer cells.
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).
T38411	KRA-533
	KRA-533, a potent KRAS agonist, directly targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This inhibition leads to the buildup of constitutively active GTP-bound KRAS, which subsequently activates both apoptotic and autophagic cell death pathways specifically in cancer cells.
T80052	Cathepsin B
	Cathepsin B为一种半胱氨酸蛋白酶，涉及多种程序性细胞死亡（包括细胞凋亡、焦亡、铁亡、坏死亡及自噬性细胞死亡）。
T60749	Autophagy-IN-2
	Autophagy-IN-2 (Compound 7h) 是自噬通量的抑制剂，可诱导癌细胞凋亡，具有研究三阴性乳腺的潜力。
T79668	PIK5-12d	Autophagy	Autophagy
	PIK5-12d为一种高效的PROTAC PIKfyve降解剂，具有显著的DC50值为1.48 nM。该化合物在多种前列腺癌细胞系中有效诱导细胞质空泡化，同时阻碍自噬流的进行，有效抑制前列腺癌细胞的增殖，并展现出抗肿瘤活性。
T82368	FTO-IN-10	Autophagy	Autophagy
	FTO-IN-10（化合物7）是一种针对人类去甲基酶FTO（脂肪量和肥胖相关蛋白）的有效抑制剂，其IC50值为4.5 μM。该化合物通过疏水作用和氢键相互作用与FTO的结构域II的结合口袋相结合。在A549细胞中，FTO-IN-10能够诱导DNA损伤和自噬性细胞死亡。
T33766	OAB-14 OAB 14,OAB14
	OAB-14 是一种 Bexarotene 衍生物，通过清除 APP/PS1 转基因小鼠的 β-淀粉样蛋白，改善其阿尔茨海默病相关的病理学和认知障碍。OAB-14 可有效改善 APP/PS1 转基因小鼠内体自噬溶酶体（EAL）途径的功能障碍。
T72291	Mitochondria degrader-1
	Mitochondria degrader-1 (实施例 5) 是一种通过自噬机制诱导受损线粒体降解的有效线粒体降解剂。适用于神经退行性疾病、癌症、炎症性疾病、年龄相关性疾病、代谢性疾病、线粒体疾病及唐氏病的研究。
T69269	DMGF
	DMGF, also known as 7,7-dimethoxyagastisfavone, is a biflavonoid isolated from Taxus × media cv. Hicksii. DMGF induces apoptotic and autophagic cell death. DMGF could effectively attenuate the motility of B16F10 cells, and the results of real-time PCR revealed that DMGF also suppressed the expressions of matrix metalloproteinase-2 (MMP-2). MGF can inhibit the metastasis of highly invasive melanoma cancer cells through the down-regulation of F-actin polymerization DMGF may be further developed to...
T11896	LV-320	Cysteine Protease	Proteases/Proteasome
	LV-320 是一种有效且非竞争性的ATG4B 抑制剂，其IC50值为 24.5 μM，Kd 值为 16 μM。 LV-320 抑制ATG4B 的酶促活性，阻断细胞自噬，并且稳定无毒，在体内具有活性。
T73912	Maysin
	Maysin 是一种具有神经保护作用的 C-糖基黄酮，可以从玉米须中分离得到。Maysin 对 Syn 淀粉样蛋白聚集体-低聚物和原纤维引起的损伤具有保护作用。Maysin 可防止氧化应激和细胞内钙稳态失衡，激活自噬降解过程。Maysin 可用于帕金森病(PD) 的研究。
T72630	BRD4 Inhibitor-25
	BRD4Inhibitor-25 是一种BRD4抑制剂，对BRD4的BD1和BD2结构域的IC50为 0.82 μM，1.94 μM。BRD4Inhibitor-25 在卵巢癌细胞中诱导凋亡和自噬细胞死亡。BRD4Inhibitor-25 可用于癌症、心血管、神经肌肉和炎症性疾病的研究。
T62331	Autophagy-IN-1
	Autophagy-IN-1 是一种有效的细胞自噬 (autophagy) /线粒体自噬 (mitophagy) 抑制剂，能够阻断癌细胞内自噬体-溶酶体融合，并同时选择性地提高自噬通量发挥作用。Autophagy-IN-1 能够阻滞细胞周期，并诱导细胞凋亡 (apoptosis)。Autophagy-IN-1 在 HCT116 小鼠异种移植瘤模型中明显抑制肿瘤生长，且毒性低。Autophagy-IN-1 能够用于研究结直肠癌。
T35922	NAADP (sodium salt)
	Nicotinic acid adenine dinucleotide phosphate (NAADP) is a secondary messenger that induces calcium mobilization. It induces calcium release from endosomes and lysosomes via two-pore channel 2 (TPC2) and TPC1, which then stimulates large-scale calcium release from granules and the endoplasmic reticulum mediated by type 1 ryanodine receptors (RyR2s), RyR3s, and inositol-(1,4,5)-triphosphate receptors (IP3Rs). NAADP induces calcium mobilization in sea urchin and starfish eggs post fertilization to...
T78871	PLM-101
	PLM-101是一种口服抗癌剂，针对FLT3和RET具有选择性抑制作用，有效抑制急性髓系白血病（AML）细胞。通过抑制RET，PLM-101促使FLT3的自噬降解，并且通过抑制PI3K和Ras/ERK信号通路来发挥其抗白血病的活性。在小鼠MV4-11侧翼异种移植模型中，PLM-101以口服剂量3及10 mg/kg显示出抗肿瘤效果，并且在同种异种移植小鼠模型中，剂量为40 mg/kg（口服）亦展现出明显的抗肿瘤功效。
T36846	Chromomycin A2
	Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respective...
T36991	Monascuspiloin
	Monascuspiloin is a fungal metabolite that has been found inM. pilosusM93-fermented rice.1It induces endoplasmic reticulum stress and autophagy in PC3 prostate cancer cells. Monascuspiloin (15-45 μM) decreases viability of PC3 cells and has an additive effect on the reduction in viability of PC3 cells induced by irradiation when used at a concentration of 25 μM. It induces intratumor apoptosis and autophagy and reduces tumor growth in a PC3 mouse xenograft model when administered at doses of 40 ...
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...
T38381	CAY17c
	CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,...

化合物

Dansylcadaverine

Cat.No: T18968

Synonym: Monodansyl cadaverine,丹酰尸胺

Target: Others, Autophagy

Cat.No: T8322

Target: Autophagy

Indomethacin farnesil

Cat.No: T7882

Synonym: 吲哚美辛法呢酯,Infree

Target: Others, COX, Autophagy

N6-Isopentenyladenosine

Cat.No: T41286

Target: Endogenous Metabolite, Autophagy

Cat.No: T9541

Synonym: Cholera Toxin B subunit

Target: Epigenetic Reader Domain

Cat.No: T1434

Synonym: A-56268,克拉霉素

Target: P450, ribosome, MRP, Antibacterial, Antibiotic, Autophagy

Cat.No: T9207

Synonym: GW108X

Target: Kinesin, Autophagy

Cat.No: T60036

Target: Autophagy

Cat.No: T5211

Synonym: NSC185058

Target: Cysteine Protease, Autophagy

Cat.No: T11142

Target: Autophagy

Cat.No: T9583

Synonym: N-Acetylphenoxazine,10-acetylphenoxazine

Target: Pim

Cat.No: T1908

Target: mTOR, Autophagy

Cat.No: T9169

Target: Mitochondrial Metabolism, Autophagy

Cat.No: T69365

Cat.No: T31411

Synonym: DHA 37

Cat.No: T26938

Synonym: CAA 0225,CAA-0225

Autophagy inducer 3

Cat.No: T61580

Lucanthone hydrochloride

Cat.No: T4569L

Synonym: Lucanthone HCl

Cat.No: T71151

Cat.No: T38411

Cat.No: T80052

Cat.No: T60749

Cat.No: T79668

Target: Autophagy

Cat.No: T82368

Target: Autophagy

Cat.No: T33766

Synonym: OAB 14,OAB14

Mitochondria degrader-1

Cat.No: T72291

Cat.No: T69269

Cat.No: T11896

Target: Cysteine Protease

Cat.No: T73912

BRD4 Inhibitor-25

Cat.No: T72630

Cat.No: T62331

NAADP (sodium salt)

Cat.No: T35922

Cat.No: T78871

Cat.No: T36846

Cat.No: T36991

Cat.No: T83765

Synonym: DDA

Cat.No: T38381

Cat. No.	Product Name	Target	Signaling Pathways
T5S1099	Liensinine	Apoptosis; Mitophagy; Others; Autophagy	Apoptosis; Autophagy; Others
	Liensinine 是一种自噬/线粒体自噬抑制剂。Liensinine 是从芙蕖种子胚中提取的，一种主要的异喹啉生物碱，具抗心律不齐、抗高血压、抗肺纤维化、血管平滑肌松弛等广泛的生物活性。
T4519	Alisol A Alisol-A,泽泻醇 A	Autophagy	Autophagy
	Alisol A (Alisol-A) 是泽泻中的一种三萜类天然产物，可能是一种自噬诱导剂，具有抗癌活性。
T5S0890	Oleandrin Neriostene,Folinerin,Foliandrin,欧夹竹桃苷	Apoptosis; ATPase; Potassium Channel; Sodium Channel	Apoptosis; Membrane transporter/Ion channel
	Oleandrin (Folinerin) 是夹竹桃属中的一种类固醇，可抑制Na+/K+-ATPase 活性，IC50为 620 nM。
T5814	Aurantiamide TMC-58B,橙黄胡椒酰胺	p38 MAPK; NF-κB	MAPK; NF-κB
	Aurantiamide 是马齿苋的活性成分，具有多种生物活性（如抗氧化、抗血小板、抗炎、抗肿瘤活性等），具有口服活性。
TN1721	Gypenoside L	ERK; p38 MAPK; Calcium Channel; NF-κB; ROS	Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Metabolism; NF-κB
	Gypenoside L 是存在于绞股蓝中的一种皂苷，可增加 SA-β-半乳糖苷酶活性，促进衰老相关分泌细胞因子的产生。它还可以激活p38和ERK MAPK 通路和NF-κB 通路以诱导衰老，具有抗肿瘤和抗炎活性。
TN6591	Cannabisin B
	Cannabisin B possesses considerable antiproliferative activity and that it may be utilised as a promising chemopreventive agent against hepatoblastoma disease. It induces autophagic cell death by inhibiting the AKT/mTOR pathway and S phase cell cycle arre
TN6069	Thalidezine
	Thalidezine, a novel AMPK activator, eliminates apoptosis-resistant cancer cells through energy-mediated autophagic cell death, it can inhibit the growth of mouse L1210 cells in vitro. Thalidezine possesses antimicrobial activity against Mycobacterium sme
TN2118	Lup-20(29)-en-28-oic acid Pulsatilla saponin D,白头翁皂苷D	ERK; mTOR; Autophagy	Autophagy; MAPK; PI3K/Akt/mTOR signaling
	Lup-20(29)-en-28-oic acid exhibits anticancer activities in various cancer types, it Inhibits autophagic flux and synergistically enhances the anticancer activity of chemotherapeutic agents against HeLa cells.Pulsatilla saponin D has strong haemolytic act

天然产物

Cat.No: T5S1099

Target: Apoptosis, Mitophagy, Others, Autophagy

Cat.No: T4519

Synonym: Alisol-A,泽泻醇 A

Target: Autophagy

Cat.No: T5S0890

Synonym: Neriostene,Folinerin,Foliandrin,欧夹竹桃苷

Target: Apoptosis, ATPase, Potassium Channel, Sodium Channel

Cat.No: T5814

Synonym: TMC-58B,橙黄胡椒酰胺

Target: p38 MAPK, NF-κB

Cat.No: TN1721

Target: ERK, p38 MAPK, Calcium Channel, NF-κB, ROS

Cat.No: TN6591

Cat.No: TN6069

Lup-20(29)-en-28-oic acid

Cat.No: TN2118

Synonym: Pulsatilla saponin D,白头翁皂苷D

Target: ERK, mTOR, Autophagy

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