histone

Daminozide (Succinic Acid) is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.

Trichostatin A (TSA), a natural derivative of diene isohydroxamic acids, is a specific and reversible histone deacetylase inhibitor (IC50=1.8 nM) that induces hyperacetylation of core histones to regulate chromatin structure.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

Acetaminophen (APAP) is a COX inhibitor that inhibits COX-1 and COX-2 (IC50=113.7/25.8 μM). Acetaminophen has antipyretic and analgesic activity as well as weak anti-inflammatory activity.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

Sinapinic Acid (Synapoic acid) protects the rat liver from CCl4-induced inflammation, most likely by acting as a free radical scavenger and modulator of NF-κB p65 activation and proinflammatory cytokine expression. Sinapic acid with antioxidant role protects cardiac cells and its functions from I/R induced oxidative stress. Sinapic acid is a potentially useful agent for the protection against liver fibrosis and cirrhosis. Sinapic acid prevents the alterations in the levels of lipids and lipoproteins by virtue of its anti-lipidaemic effect in isoproterenol induced myocardial infarcted rats. Sinapic acid ameliorates hyperglycemia through PLC-PKC signals to enhance the glucose utilization in diabetic rats.

Butanoic acid is an endogenous human metabolite, an endogenous histone deacetylase (HDAC) inhibitor. The IC50 of HDAC3, HDAC4 and HDAC1 were 2.4 mM, 4.5 mM and 5.3 mM, respectively. 3-Hydroxybutyric acid has the effects of energy metabolism, neuroprotection, anti-inflammatory, and improvement of insulin resistance.

Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

4-tert-Octylphenol, an endocrine-disrupting chemical with estrogenic properties, notably induces apoptosis in offspring mouse brain neuronal progenitor cells. This compound decreases levels of bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), thereby diminishing the proliferation of neuronal progenitors. Consequently, 4-tert-Octylphenol adversely affects brain development and behavior in mice.

Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively.

(15:3)-Anacardic acid is a benzoic acid derivative with antibacterial activity and inhibits histone acetyltransferase (HAT) at the μM level.

L-2-Hydroxyglutaric acid (L-2-HG) is a compartmentalized metabolite and a substrate for L-2-hydroxyglutarate dehydrogenase (L2HGDH). It inhibits histone demethylases and increases the expression of ATF4 and its target genes by activating the mTOR pathway. L-2-Hydroxyglutaric acid mediates the mTOR-ATF4 signaling pathway and can be used in biosensor research.

Apicidin (OSI 2040) is a histone deacetylase (HDAC) inhibitor with antiparasitic and antiproliferative activity. It attenuates memory deficits, inhibits cell growth and proliferation, and induces apoptosis and autophagy by decreasing Abeta load in APP/PS1 mice, making it a valuable tool for leukemia research.

SantacruzaMate A (CAY-10683) is a potent and selective HDAC inhibitor.

1-Alaninechalmydocin is a fungal metabolite originally isolated from a Great Lakes-derived Tolypocladium sp. and an inhibitor of histone deacetylases (HDACs). It reduces total HDAC activity in HeLa cell lysates in a concentration-dependent manner. 1-Alaninechlamydocin reduces proliferation of MIA PaCa-2, PANC-1, and hTERT-HPNE cells (GI50s = 5.3, 14, and 2.0 nM, respectively).

9-hydroxy Stearic Acid is a hydroxy fatty acid that is the active metabolite of 9-PAHSA. 9-hydroxy Stearic Acid is formed from 9-PAHSA through carboxyl ester lipase in the liver and pancreas. The 9-hydroxy Stearic Acid (5 μM) was stearic acid, which inhibited the expression of histone deacetylase 1 (HDAC1) in the lysate of HT-29 colon cancer cells. 3. When the concentration was 100 μM.1, the proliferation of HT-29 cells was inhibited and cell cycle arrest was induced in G0/ g1 phase.

cis-Resveratrol ((Z)-Resveratrol) has antiviral activity, inhibits enteroviruses, increases TyrRS, promotes histone serine-ADP ribosylation-dependent DNA repair, and provides neuroprotection in a TyrRS-dependent manner.

Raddeanin A is a natural triterpenoid saponin from Cyperus japonicus that inhibits histone deacetylase and is also a potent immunogenic cell death inducer with strong anti-angiogenic and anti-tumor activities.

Nε,Nε,Nε-Trimethyllysine chloride (Lys(Me)3-OH Chloride) is a methylated derivative of lysine, found in histone proteins and serves as a coenzyme in fatty acid oxidation. It is a precursor for carnitine, generated by S-adenosyl-L-methionine on lysine residues. Upon proteolysis, it is converted to 3-hydroxy-6-N-trimethyllysine by mitochondrial 6-N-trimethyllysine dioxygenase, initiating carnitine biosynthesis.

Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.

1. Crotonoside (Isoguanosine) has much more active than adenosine in reducing the blood pressure in rabbits and cats, in decreasing the tone of isolated intestinal strips of the rabbit, guinea pig and hamster and in stimulating the isolated uterus of guinea pigs and hamsters. 2. Crotonoside inhibits the growth of S-18 and Ehrlich solid tumor in mice at the optimal doses of 96 mg/kg/day x 12 and 48 mg/kg/day x 12, with 1-T/C values of 65% and 6%, respectively.

Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of a

Depudecin is a polyketide obtained from the fungus Alternaria brassicicola and having a highly unusual structure of an 11-carbon chain containing two epoxides and six stereogenic centres. It is an inhibitor of histone deacetylase (HDAC) both in vivo and in vitro and also exhibits anti-angiogenic activity.