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Garcinol

HAT inhibitor
 
BML-GR343-0010 10 mg 90.00 USD
 
BML-GR343-0050 50 mg 342.00 USD
 
Garcinol is a polyisoprenylated benzophenone derivative isolated from Garcinia indica. It is a potent inhibitor of histone acetyltransferases (HATs) p300 (IC50=7µM) and PCAF (IC50=5µM) both in vitro and in vivo. HAT activity-dependent chromatin transcription was inhibited by garcinol, but it had no effect on naked DNA transcription. It induces apoptosis in HeLa cells (100µM) where it down regulates global gene expression. Acetylation of histone H4 by p300 was more sensitive to inhibition by garcinol compared with that of H3. Histone H4 acetylation was completely inhibited at 1 µM while acetylation of H3 was not abolished at 20 µM.

Product Specification

Formula:C38H50O6
 
MW:602.8
 
Source:Synthetic.
 
CAS:78824-30-3
 
Purity:≥95% (TLC)
 
Identity:Determined by NMR.
 
Appearance:Yellow solid.
 
Solubility:Soluble in DMSO (25mg/ml) or 100% ethanol (25mg/ml) or dimethylformamide (25mg/ml).
 
Short Term Storage:-20°C
 
Use/Stability:Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
 
Handling:Protect from exposure to air
 
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Product Literature References

Garcinol potentiates TRAIL-induced apoptosis through modulation of death receptors and antiapoptotic proteins: S. Prasad, et al.; Mol. Cancer Ther. 9, 856 (2010), Abstract;
Mechanism of p300 specific histone acetyltransferase inhibition by small molecules: M. Arif, et al.; J. Med. Chem. 52, 267 (2009), Abstract;
Specific inhibition of p300-HAT alters global gene expression and represses HIV replication: K. Mantelingu, et al.; Chem. & Biol. 14, 645 (2007), Abstract;
Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression: K. Balasubramanyam, et al.; J. Biol. Chem. 279, 33716 (2004), Abstract; Full Text
Cytotoxic benzophenone derivatives from Garcinia species display a strong apoptosis-inducing effect against human leukemia cell lines: K. Matsumoto, et al.; Biol. Pharm. Bull. 26, 569 (2003), Abstract;
On the structures of garcinol, isogarcinol and camboginol: N. Krishnamurthy, et al.; Tetrahed. Lett. 22, 793 (1981), Abstract;

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