1. Signaling Pathways
  2. Autophagy
  3. Autophagy

Autophagy

Autophagy is a conserved cellular degradation and recycling process in the lysosome. In mammalian cells, there are three primary types of autophagy: microautophagy, macroautophagy, and chaperone-mediated autophagy (CMA). Microphagy captures cargoes by means of invaginations or protrusions of the lysosomal membrane directly, CMA uses chaperones to identify cargo proteins and then unfolds and transfers them into the lysosomal, while macroautophagy sequesters cargo by autophagosomes-de novo synthesized of double-membrane vesicles-and subsequently transport it to the lysosome.

Macroautophagy is the best studied and it occurs at a low level constitutively and can also be further induced under stress conditions, such as nutrient or energy starvation with a salient feature of autophagy protein degradation. Stress-induced macrophagy plays an important role in protein catabolism with another key protein degradation pathway, the ubiquitin–proteasome system (UPS).

As the study progressed, autophagy gains its importance under basal, nutrient-rich conditions, and is now recognized as a critical housekeeping pathway in catabolism of diverse cellular constituents, such as protein aggregates (aggrephagy), lipid droplets (lipophagy), iron complex (Ferritinophagy) and carbohydrate. Except for macromolecules, autophagy can also target several organelles and structures, such as mitochondria (mitophagy), peroxisome (pexophagy), endoplasmic reticulum (reticulophagy or ER-phagy), ribosome (ribophagy), spermatozoon-inherited organelles following fertilization (allophagy), secretory granules within pancreatic cells (zymophagy) and intracellular pathogens (xenophagy).

Autophagy and its dysfunction are associated with a variety of human pathologies, including ageing, cancer, neurodegenerative disease, heart disease and metabolic diseases, such as diabetes. Plenty of drugs and natural products are involved in autophagy modulation through multiple signaling pathways. Small molecules that can regulate autophagy seem to have great potential to intervene such diseases in animal models or clinical courses.

Autophagy 相关产品 (676):

Cat. No. Product Name Effect Purity
  • HY-10219
    Rapamycin Activator 99.93%
    Rapamycin (Sirolimus; AY 22989) 是一种有效且特异性的 mTOR 抑制剂,作用于 HEK293 细胞,抑制 mTORIC50 为 0.1 nM。Rapamycin 与 FKBP12 结合且抑制 mTORC1。Rapamycin 还是一种自噬 (autophagy) 激活剂。
  • HY-13259
    MG-132 Activator >98.0%
    MG-132 是一种多肽醛,也是有效的,可逆的,可透过细胞的蛋白酶体抑制剂,IC50 值为 100 nM,有效地阻断了 26S 蛋白酶体复合物的蛋白水解活性。
  • HY-12320
    Cycloheximide Inhibitor 99.45%
    Cycloheximide (Naramycin A) 是真核生物蛋白质合成的抑制剂,抑制体内蛋白质合成和RNA合成的 IC50 值分别为532.5 nM 和 2880 nM。
  • HY-19312
    3-Methyladenine Inhibitor 99.84%
    3-Methyladenine是 PI3K 的抑制剂。它通过抑制class III PI3K广泛作为自噬 (autophagy) 的抑制剂使用。
  • HY-10108
    LY294002 Inhibitor 99.95%
    LY294002 是一种广谱 PI3K 抑制剂,抑制 PI3Kα, PI3KδPI3KβIC50 分别为 0.5, 0.57, 0.97 μM。LY294002 也可抑制 CK2 的活性,IC50 为 98 nM。
  • HY-N2329
    Piperlongumine Activator 99.19%
    Piperlongumine 是从荜茇中得到的生物碱,具有抗炎、抗菌、抗血管生成、抗氧化、抗肿瘤和抗糖尿病等活性。在肿瘤细胞中,Piperlongumine 能够诱导 ROS 和凋亡。Piperlongumine 具有抗心肌纤维化的作用,通过抑制 ERK1/2 信号通路抑制肌成纤维细胞的转化。
  • HY-N0281
    Daphnetin Activator 99.55%
    Daphnetin (7,8-dihydroxycoumarin) 是从 Genus Daphne 中分离得到的一种香豆素衍生物,是一种蛋白酶 (protein kinase) 抑制剂,对 EGFR、PKA 和 PKC 的 IC50 值分别为 7.67 μM、9.33 μM 和 25.01 μM。Daphnetin (7,8-dihydroxycoumarin) 是用于抗炎、抗过敏疾病的植物次生代谢产物药物,也已被临床用于治疗凝血功能障碍、类风湿性关节炎等疾病,具有抗疟疾、解热等特性。
  • HY-B1479A
    Emetine dihydrochloride Inhibitor
    Emetine (dihydrochloride) 是一种抗原虫药,早期用于治疗肠道和组织的阿米巴病。
  • HY-10162
    Olaparib Activator 99.98%
    Olaparib (AZD2281; KU0059436) 是一种有效的 PARP 抑制剂,抑制 PARP-1PARP-2IC50 分别为 5 和 1 nM。
  • HY-11109
    Resatorvid Inhibitor 99.95%
    Resatorvid (TAK-242) 是一种有效的 TLR4 信号传导抑制剂,可选择性地抑制TLR-介导的细胞因子和一氧化氮的产生。
  • HY-15142
    Doxorubicin hydrochloride Activator 99.47%
    Doxorubicin hydrochloride是一种有细胞毒性的蒽环类抗生素,用于治疗多种癌症。 Doxorubicin 在癌细胞中起作用的可能机制是嵌入 DNA 和破坏 topoisomerase-II 介导的DNA修复。
  • HY-17559
    Actinomycin D Activator 99.89%
    Actinomycin D 抑制 DNA 修复,IC50 为 0.42 μM。
  • HY-13030
    (+)-JQ-1 Activator 99.90%
    (+)-JQ-1 是一种 BET bromodomain 抑制剂,抑制 BRD4(1/2)IC50 分别为 77 nM 和 33 nM。(+)-JQ-1 激活自噬 (autophagy)。
  • HY-10256
    SB 203580 Activator 99.92%
    SB 203580 (RWJ 64809) 是一种广泛使用的 p38 MAPK 抑制剂, IC50 介于 0.3-0.5 μM 之间。 对 p38 MAPK 的选择性比 Akt (PKB), LCK, 和 GSK-3β 高 100 倍。
  • HY-13316
    Mitomycin C Activator 99.45%
    Mitomycin C是一种抗肿瘤药物和抗生素,可有效的抑制DNA合成 (DNA synthesis)。Mitomycin C 是一种 DNA 交联剂,诱导 DNA 损伤。
  • HY-12041
    SP600125 Inhibitor 98.82%
    SP600125是一种可逆,ATP竞争性的 JNK 抑制剂,抑制 JNK1JNK2JNK3IC50 分别为 40, 40, 90 nM。
  • HY-17589
    Chloroquine diphosphate Inhibitor 99.94%
    Chloroquine diphosphate是一种广泛用于治疗疟疾和类风湿性关节炎的抗疟疾和抗炎药。 Chloroquine 是 autophagytoll-like receptors (TLRs) 的抑制剂。
  • HY-12031
    U0126 Inhibitor 98.06%
    U0126是一种有效,非ATP竞争性的 MEK1MEK2 抑制剂,IC50 分别为70 nM和60 nM。
  • HY-15531
    Venetoclax Activator 99.95%
    Venetoclax (ABT-199; GDC-0199) 是一种高效,有选择性和口服活性的 Bcl-2 抑制剂,Ki 小于0.01 nM。
  • HY-B0015
    Paclitaxel Inhibitor 99.97%
    Paclitaxel (Taxol) 是一种天然的抗癌药物,能稳定微管蛋白聚合,并导致细胞周期的 G2/M 期停滞和凋亡细胞死亡。
Isoform Specific Products

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