Garcinol

HAT inhibitor



BML-GR343-0010	10 mg	127.00 USD

BML-GR343-0050	50 mg	486.00 USD
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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 Details

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).

Shipping:	Blue Ice

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

Regulatory Status:	RUO - Research Use Only

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Product Literature References

Vascular hyperacetylation is associated with vascular smooth muscle dysfunction in a rat model of non-obese type 2 diabetes: M.A.C. Sepulveda, et al.; Mol. Med. 28, s10020 (2022), Abstract;

Phosphorylation of Eukaryotic Initiation factor-2α (eIF2α) in Autophagy: J. Humeau, et al.; Cell Death Dis. 11, 433 (2020), Abstract; Full Text

Targeting MHC Regulation Using Polycyclic Polyprenylated Acylphloroglucinols Isolated from Garcinia bancana: C. Coste, et al.; Biomolecules 10, 1266 (2020), Abstract; Full Text

Regulation of Histone Acetylation by Autophagy in Parkinson Disease: G. Park, et al. ; J. Biol. Chem. 291, 3531 (2016), Application(s): Cell culture, Abstract; Full Text

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;