Garcinol

BML-GR343

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HAT inhibitor

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.

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Product Details

Appearance	Yellow solid.
CAS	78824-30-3
Couple Target	HAT
Couple Type	Inhibitor
Formula	C₃₈H₅₀O₆
Identity	Determined by NMR.
MW	602.8
Purity	≥95% (TLC)
Solubility	Soluble in DMSO (25mg/ml) or 100% ethanol (25mg/ml) or dimethylformamide (25mg/ml).
Source	Synthetic.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. 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
Short Term Storage	-20°C
Shipping	Blue Ice

Regulatory Status	RUO – Research Use Only

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
Nuclear mechanosensing drives chromatin remodelling in persistently activated fibroblasts: Walker, C. J., Crocini, C., et al.; Nat. Biomed. Eng. 5, 1485 (2021), 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
Inhibition of Pseudomonas aeruginosa and Mycobacterium tuberculosis disulfide bond forming enzymes: Landeta, C., McPartland, L., et al.; Mol. Microbiol. 111, 918 (2019), Abstract
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
Epigenetic Modulation of Collagen 1A1: Therapeutic Implications in Fibrosis and Endometriosis: Zheng, Y., Khan, Z., et al.; Biol. Reprod. 94, 87 (2016), Abstract
Garcinol Inhibits GCN5-Mediated Lysine Acetyltransferase Activity and Prevents Replication of the Parasite Toxoplasma gondii: Jeffers, V., Gao, H., et al.; Antimicrob. Agents Chemother. 60, 2164 (2016), Abstract
A novel functional site in the PB2 subunit of influenza A virus essential for acetyl-CoA interaction, RNA polymerase activity, and viral replication: Hatakeyama, D., Shoji, M., et al.; J. Biol. Chem. 289, 24980 (2014), Abstract
A cell-free fluorometric high-throughput screen for inhibitors of Rtt109-catalyzed histone acetylation: Dahlin, J. L., Sinville, R., et al.; PLoS One 8, e78877 (2013), Abstract

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Garcinol

BML-GR343

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