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 (921):

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,免疫抑制剂。
  • 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 99.86%
    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 Activator 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。LY294002 是一种竞争性 DNA-PK 抑制剂,可逆结合 DNA-PK 的激酶结构域,IC50 为 1.4 μM。
  • HY-115453
    UBCS039 98.55%
    UBCS039 是首个合成的,SIRT6 的特异性激活剂,可在人癌细胞中诱导自噬,其EC50 值为38 μM。
  • HY-111772
    CFTR corrector 1 99.70%
    CFTR corrector 1 (compound 1) 是一种囊性纤维化跨膜电导调节剂 (CFTR) 的调节剂。CFTR corrector 1 (compound 1) 促进CFTR的加工和转运,增加细胞表面CFTR的数量。
  • HY-B1479A
    Emetine dihydrochloride Inhibitor >99.0%
    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-17559
    Actinomycin D Activator 99.58%
    Actinomycin D 抑制 DNA 修复,IC50 为 0.42 μM。
  • 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。Doxorubicin hydrochloride 下调 AMPK 的基础磷酸化以及下游 acetyl-CoA 羧化酶。
  • HY-11109
    Resatorvid Inhibitor 99.95%
    Resatorvid (TAK-242) 是一种选择性的 TLR4 信号传导抑制剂,在各种炎症性疾病中起关键作用。Resatorvid 抑制 NO,TNF-R 和 IL-6 的产生,其 IC50 值分别为 1.8 nM,1.9 nM,1.3 nM。Resatorvid 下调 TLR4 下游信号分子 MyD88 和 TRIF 的表达。
  • HY-13030
    (+)-JQ-1 Activator 99.90%
    (+)-JQ-1 是一种有效特异性的可逆 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-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-10256
    SB 203580 Activator 99.92%
    SB 203580 (RWJ 64809) 是一种选择性的,ATP竞争性的 p38 MAPK 抑制剂。SB 203580 (RWJ 64809) 抑制 SAPK2a/p38SAPK2b/p38β2IC50 分别为 50 nM 和 500 nM。而 SB 203580 (RWJ 64809) 抑制 LCK, GSK3β 和 PKBα 的 IC50 比 SAPK2a/p38 高 100-500 倍。
  • 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 diphosphate 是 autophagytoll-like receptors (TLRs) 的抑制剂。
  • HY-12041
    SP600125 Inhibitor 98.82%
    SP600125是一种细胞渗透性的,可逆的,ATP竞争性的 JNK 抑制剂,抑制 JNK1JNK2JNK3IC50 分别为 40, 40, 90 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-100558
    Bafilomycin A1 Inhibitor >99.0%
    Bafilomycin A1,一种从链霉菌属物种中分离的大环内酯类抗生素,是特异的 vacuolar-type H+ ATPase (V-ATPase) 抑制剂。Bafilomycin A1 抑制自噬。
  • 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。
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