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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——Autophagy(1002)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM5271 (+)-JQ-1

(+)-JQ-1 (JQ1) 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)。

1268524-70-4 99%
KM11022 (+)-Talarozole

(+)-Talarozole 是视黄酸代谢的有效抑制剂,来自专利 WO 1997049704 A1。

201410-66-4 99%
KE2834 (+)-Taxifolin 17654-26-1 ≥95%
KM12160 (-)-Epicatechin gallate

(-)-Epicatechin gallate (Epicatechin gallate) 抑制环加氧酶-1 (COX-1) , IC50 为 7.5 μM。

1257-08-5 98%
KM15701 (-)-Epigallocatechin

(-)-Epigallocatechin (Epigallocatechin) 是绿茶中最丰富的类黄酮,能结合未折叠多肽和防止转化为淀粉样纤维。

970-74-1 98%
KM5155 (-)-Epigallocatechin Gallate

(-)-Epigallocatechin Gallate是一种茶类黄酮,具有强大的抗氧化,抗炎和抗癌作用。报道显示(-)-Epigallocatechin Gallate可抑制 EGFR 信号传导,从而发挥抗癌作用。(-)-Epigallocatechin Gallate (EGCG) 是谷氨酸脱氢酶 1/2 (GDH1/2GLUD1/2) 抑制剂。(-)-Epigallocatechin Gallate 通过激活细胞色素c氧化酶来诱导氧化磷酸化 (OXPHOS)。

989-51-5 99%
KM9789 (-)-PX20606 trans isomer

(-)-PX20606 trans isomer 是一种 FXR 激动剂,在 FRET 和 M1H 测定中对于 FXR 的 EC50 值分别为 18 和 29 nM。

1268244-88-7
KM4725 (-)-Talarozole

(-)-Talarozole 是视黄酸代谢的有效抑制剂,来自专利 WO 1997049704 A1。

201410-67-5 98%
KM7580 (3S,5R)-Fluvastatin D6

(3S,5R)-Fluvastatin D6 是 (3S,5R)-Fluvastatin sodium 的氘代物。Fluvastatin 是第一个完全合成的,竞争性的 HMG-CoA reductase 还原酶抑制剂,IC50 为 8 nM。Fluvastatin 通过依赖 Nrf2 的抗氧化通路保护血管平滑肌细胞免受氧化应激。

2249799-34-4
KM17068 (E)-Daporinad

(E)-Daporinad (FK866) 是烟酰胺磷酸核糖转移酶 (NMPRTase; Nampt) 的有效抑制剂, IC50 为 0.09 nM。

658084-64-1 99%
KM6618 (R)-(-)-Gossypol acetic acid

(R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) 是天然产物 Gossypol 的左旋异构体。AT-101 结合到 Bcl-2Mcl-1Bcl-xL 蛋白,Ki 值分别为 260±30 nM,170±10 nM 和 480±40 nM。

866541-93-7 98%
KM11787 (R)-BPO-27

(R)-BPO-27 是 BPO-27 的 R 型对映体,是一种有效的、具有口服活性的、ATP 竞争性的 CFTR 抑制剂,具有 IC50 的 4 nM。

1415390-47-4 99%
KM17358 (Rac)-AZD 6482

(Rac)-AZD 6482 ((Rac)-KIN-193) 是 AZD 6482 的消旋体,AZD 6482 是一种有效的选择性 p110β 抑制剂,IC50 为 0.69 nM。

663620-70-0
KM5568 (Rac)-BL-918

(Rac)-BL-918 是BL-918 的消旋体。BL-918 是 ULK1 的有效激活剂,可诱导细胞保护性自噬,用于帕金森病的研究。

2435589-07-2 98%
KM6792 (Rac)-Efavirenz-d4

(Rac)-Efavirenz-d4 ((Rac)-DMP 266-d4) 是 Efavirenz 氘代消旋体。Efavirenz (DMP 266) 是一种有效的野生型 HIV-1 RT 抑制剂,Ki 为 2.93 nM,抑制 HIV-1 复制,IC95 为 1.5 nM。

1246812-58-7
KM16208 (Rac)-Hesperetin

(Rac)-Hesperetin 是Hesperetin 的外消旋体。 Hesperetin 是一种天然黄烷酮类物质,为有效的,广谱的人 UGT 抑制剂。Hesperetin 可通过激活 p38 MAPK 来诱导凋亡。

69097-99-0 98%
KM7645 (Rac)-Sitagliptin-d4 hydrochloride

(Rac)-Sitagliptin-d4 hydrochloride 是 Sitagliptin 氘代消旋体。Sitagliptin 是一种有效的 DPP4 抑制剂,在 Caco-2 细胞中,IC50 值为 19 nM。

1620233-77-3
KM9133 (S)-(-)-Felodipine-d5

(S)-(-)-Felodipine-d5 是 (S)-(-)-Felodipine 的氘代物。(S)-(-)-Felodipine 是 Felodipine 的异构体。Felodipine 是一种二氢吡啶,是一种有效的血管选择性钙通道 (b>calcium channel) 拮抗剂。Felodipine 通过选择性作用于血管平滑肌,尤其是阻力血管来降低血压。Felodipine 是具有抗高血压活性,可诱导自噬。Felodipine 可以跨越血脑屏障。

1217744-87-0
KM19176 (±)-Taxifolin

(±)-Taxifolin ((±)-Dihydroquercetin) 是 Taxifolin 的消旋体。Taxifolin 具有重要的抗酪氨酸酶活性。Taxifolin 有效抑制胶原酶 (collagenase),IC50 为 193.3 μM。Taxifolin是一种重要的天然化合物,具有抗纤维化作用。Taxifolin 是一种自由基清除剂具有抗氧化能力。

24198-97-8
KM13941 1-Monomyristin

1-Monomyristin 提取自 Serenoa repens,抑制 2-油酰甘油的水解 (IC50=32 μM) 和脂肪酸酰胺水解酶 (FAAH) 活性 (IC50=18 μM)。1-Monomyristin 对金黄色葡萄球菌和聚集性放线菌有抗菌活性,对白色念珠菌也有抗真菌活性。

589-68-4 ≥98%
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