Rapamycin
| Code | Size | Price |
|---|
| TAR-T1537-25mg | 25mg | £103.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T1537-1mL | 1 mL * 10 mM (in DMSO) | £106.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T1537-50mg | 50mg | £109.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T1537-100mg | 100mg | £122.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T1537-200mg | 200mg | £159.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T1537-500mg | 500mg | £237.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells).
Biological Applications:
Bafilomycin A1 is a late-stage autophagy inhibitor. Autophagy, meaning "self-eating", is the cellular process of degrading its own cytoplasmic proteins and damaged organelles using lysosomes. Autophagy serves to prevent cellular damage, promote cell survival under nutrient-deficient conditions, and respond to cytotoxic stimuli. However, excessive autophagy can lead to metabolic stress, degradation of cellular components, and even cell death. Research indicates that autophagy plays a crucial role in various physiological and pathological processes such as cellular homeostasis, aging, immunity, inflammation, tumorigenesis, and neurodegenerative diseases.
CAS:
53123-88-9
Description:
Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells). Rapamycin shows potent immunosuppressive properties and induces autophagy.
Formula:
C51H79NO13
Mechanism of Action:
Bafilomycin A1 disrupts the fusion of autophagosomes with lysosomes and the acidification of lysosomes, exerting an inhibitory effect on autophagy. The fusion of autophagosomes with lysosomes and the acidification of lysosomes are late-stage steps in the autophagic process, essential for maintaining functional autophagic flux and cellular homeostasis. Lysosomes are cellular organelles containing hydrolytic enzymes capable of degrading substances such as proteins, nucleic acids, and lipids. Modulating the acidic environment within lysosomes controls the efficiency and speed of their degradation.
Bafilomycin A1 inhibits the function of the V-ATPase within lysosomes, thereby preventing the formation of an acidic environment in lysosomes. Additionally, Baf A1 can inhibit the endoplasmic reticulum calcium ATPase Ca-P60A/SERCA, disrupting the fusion of autophagosomes with lysosomes. By acting at two steps in the autophagy, Baf A1 collectively prevents protein degradation and functional autophagy.
Molecular Weight:
914.18
Pathway:
Microbiology/Virology; Metabolism; Autophagy; PI3K/Akt/mTOR signaling;
Purity:
0.9873
Research Area:
Cellular homeostasis; Aging; Immunity; Inflammation; Tumours; Neurodegenerative diseases
SMILES:
CO[C@@H]1C[C@H](C[C@@H](C)[C@@H]2CC(=O)[C@H](C)C=C(C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)C=CC=CC=C(C)[C@H](C[C@@H]3CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@H]3C(=O)O2)OC)CC[C@H]1O
Target:
Endogenous Metabolite; Antibiotic; mTOR; Autophagy; Antifungal
References
1. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem. 2007 May 4;282(18):13395-401.
10. Zhao, Ming, et al. GCG inhibits SARS-CoV-2 replication by disrupting the liquid phase condensation of its nucleocapsid protein. Nature Communications . 12.1 (2021): 1-14.
2. Guba M, et al. Rapamycin inhibits primary and metastatic tumor growth by antiangiogenesis: involvement of vascular endothelial growth factor. Nat Med. 2002 Feb;8(2):128-35.
3. Takeuchi H, et al. Synergistic augmentation of rapamycin-induced autophagy in malignant glioma cells by phosphatidylinositol 3-kinase/protein kinase B inhibitors. Cancer Res. 2005 Apr 15;65(8):3336-46.
4. Bodine SC, et al. Akt/mTOR pathway is a crucial regulator of skeletal muscle hypertrophy and can prevent muscle atrophy in vivo. Nat Cell Biol. 2001 Nov;3(11):1014-9.
5. Marin TM, et al. Rapamycin reverses hypertrophic cardiomyopathy in a mouse model of LEOPARD syndrome-associated PTPN11 mutation. J Clin Invest. 2011 Mar;121(3):1026-43.
6. Zhang JW, et al. Metformin synergizes with rapamycin to inhibit the growth of pancreatic cancer in vitro and in vivo. Oncol Lett. 2018 Feb;15(2):1811-1816.
7. Gao C, Wang H, Wang T, et al. Platelet CLEC?2 regulates neuroinflammation and restores blood brain barrier integrity in a mouse model of traumatic brain injury[J]. Journal of Neurochemistry. 2020: e14983.
8. Zhang T, Tian C, Wu J, et al.?. MicroRNA?182 exacerbates blood?brain barrier (BBB) disruption by downregulating the mTOR/FOXO1 pathway in cerebral ischemia[J]. ?The FASEB Journal. 2020, 34(10): 13762-13775.
9. Shang Z, Zhang T, Jiang M, et al. High-carbohydrate, High-fat Diet-induced Hyperlipidemia Hampers the Differentiation Balance of Bone Marrow Mesenchymal Stem Cells by Suppressing Autophagy via the AMPK/mTOR Pathway in Rat Models[J]. 2020.