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Gossypol

Cat. No. M4385
Gossypol Structure
Synonym:

BL 193

Size Price Availability Quantity
20mg USD 60  USD60 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Gossypol has been known to exert a potential for anti-cancer, anti-inflammatory and other important therapeutic activities, gossypol binds and antagonizes anti-apoptotic effect of Bcl-2 family proteins. IC50 value: Target: Bcl-2; anticancer agent The substance, a yellow pigment similar to flavonoids, is present in cottonseed oil. In the plant, it acts as a natural defensive agent against predators, provoking infertility in insects. In most animals, gossypol provokes infertility, and in man it causes spermatogenesis arrest at relatively low doses. in vitro: The natural product and putative BH3 mimetic gossypol enhanced the cytotoxicity of BRD4770 in a synergistic manner in p53-mutant PANC-1 cells but not in immortalized non-tumorigenic pancreatic cells. The combination of gossypol and BRD4770 increased LC3-II levels and the autophagosome number in PANC-1 cells, and the compound combination appears to act in a BNIP3 (B-cell lymphoma 2 19-kDa interacting protein)-dependent manner. Gossypol treatment resulted in cell death through oxidative stress. Metabolite analysis showed that gossypol induces a decrease of the cellular levels of GSH, aspartic acid, and FAD in ovarian cancer cell line, SKOV3. gossypol blocked the phosphorylation of IκBα protein, p65, p38, c-Junterminal kinase (JNK) and extracellular signal-regulated kinase (ERK) in LPS stimulated RAW 264.7 cells. gossypol could down-regulate activation of ConA-induced NF-κB, NFAT and AP-1 signal transduction pathways in mouse T lymphocyte [4]. in vivo: gossypol significantly inhibited the production of LPS-induced TNF-α, IL-6 and IL-1β both in vitro and vivo.gossypol attenuated lung histopathologic changes in mouse models. Preliminary studies in vivo showed that a growth inhibition (T/C) of 30.9% (gossypol acetate 40 mg/kg) was obtained in Balb/C mice bearing Wus1 cells. In addition, there was no body weight loss for the treated group in comparison with the vehicle mice.

Protocol
Cell Experiment
Cell lines bovine granulosa cells
Preparation method In bovine granulosa cells, treatment with gossypol dose-dependently decreased hCG-induced cAMP formation.
Concentrations 12.5 μg/ml
Incubation time 24 h
Animal Experiment
Animal models BALB/c mice
Formulation
Dosages 25 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 518.55
Formula C30H30O8
CAS Number 303-45-7
Purity >98%
Solubility 25 mM in DMSO
Storage at -20°C
References

[1] Yang D, et al. Cancer Chemother Pharmacol. Gossypol sensitizes the antitumor activity of 5-FU through down-regulation of thymidylate synthase in human colon carcinoma cells.

[2] Liu H, et al. Xenobiotica. Identification of glucuronidation and biliary excretion as the main mechanisms for gossypol clearance: in vivo and in vitro evidence.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Gossypol, BL 193 supplier, Bcl-2, inhibitors

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