verucopeptin
verucopeptin Basic information
- Product Name:
- verucopeptin
- Synonyms:
-
- Glycine, (3S)-3-hydroxy-N-[(2S)-2-hydroxy-1-oxo-2-[(5S,6R)-tetrahydro-2-hydroxy-5-methoxy-6-[(1E,3S,5S,7R)-1,3,5,7-tetramethyl-1-nonen-1-yl]-2H-pyran-2-yl]propyl]-L-leucyl-(3R)-hexahydro-3-pyridazinecarbonyl-N-hydroxyglycyl-N-methylglycylglycyl-N-methyl-, (6→13)-lactone
- CAS:
- 138067-14-8
- MF:
- C43H73N7O13
- MW:
- 896.086
- Mol File:
- 138067-14-8.mol
verucopeptin Chemical Properties
- Density
- 1.27±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- pka
- 8.61±0.60(Predicted)
- form
- Solid
- color
- White to light yellow
verucopeptin Usage And Synthesis
Uses
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
in vivo
Verucopeptin (intravenous?injection; 1 mg/kg; twice daily; 7 days) substantially represses tumor growth without significant body weight loss or gross signs of toxicity. HE staining indicated that Verucopeptin potently induces cell death and abrogates mTORC1 signaling by dephosphorylation of S6K and 4EBP1[3].
| Animal Model: | BALB/c nude mice by subcutaneous injection of SGC7901/VCR cells[3] |
| Dosage: | 1 mg/kg |
| Administration: | Intravenous?injection; 1 mg/kg; twice daily; 7 days |
| Result: | Exhibited profound antitumor efficacy in vivo against MDR tumors. |
References
[1] Aya Yoshimura, et al.Structure Elucidation of Verucopeptin, a HIF-1 Inhibitory Polyketide-Hexapeptide Hybrid Metabolite from an Actinomycete. Org Lett. 2015 Nov 6;17(21):5364-7. DOI:10.1021/acs.orglett.5b02718
[2] Nobuaki Takahashi, et al. Total synthesis of verucopeptin, an inhibitor of hypoxia-inducible factor 1 (HIF-1). Chem Commun (Camb). 2019 Oct 1;55(79):11956-11959. DOI:10.1039/c9cc06169j
[3] Yuezhou Wang, et al. Pharmacological Targeting of Vacuolar H +-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Jun 30;S2451-9456(20)30234-8. DOI:10.1016/j.chembiol.2020.06.011
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