acetylation

Histone Acetyltransferase Inhibitor II is a selective and cell permeable inhibitor of p300 histone acetyltransferase(IC50 : 5 μM).with anti-acetylase activity in mammalian cells.

L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.

1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM, demonstrating greater selectivity for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). It does not increase global histone H4 acetylation or reduce total intracellular HDAC activity but can induce tubulin acetylation[1][2].

CMS-121, a quinolone derivative, is an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage (EC50: 7 nM and 200 nM). CMS-121 shows strong neuroprotective, antioxidative, anti-inflammatory, and renoprotective activities.

Tenovin-6 is a p53 transcriptional activity agonist.

Tenovin-1 inhibits protein-deacetylating activities of SirT1 and SirT2 and protects against MDM2-mediated p53 degradation, which involves ubiquitination.

OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor, and for SIRT6(IC50=89 μM), SIRT1(IC50=1578 μM) and SIRT2(IC50=751 μM).

CXD101 is a novel class I-selective HDACi (HDAC1 (IC50 : 63nM), HDAC2 (IC50 :570nM), HDAC3 (IC50 :550nM)). CXD101(CXD-101) has no activity against HDAC class II

Tenovin-6 Hydrochloride is an SIRT1, SIRT2 and HDAC8 inhibitor(IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively), and is also a potent p53 activator .

BRD32048 is the ETV1 transcription factor oncoprotein inhibitor.

BRD73954, an effective and specific HDAC inhibitor, which is with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

Tri-GalNAc-COOH acetylation represents the acetylated derivative of tri-galactosamine (tri-GalNAc-COOH), utilized in the synthesis of lysosome targeting chimeras (LYTAC).

EGCG Octaacetate, a prodrug of EGCG, is utilized to enhance the stability and bioavailability of EGCG in vivo. It has high efficacy, bioavailability, anti-oxidation, and anti-angiogenesis capacities.

Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea.

DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione)  as a bona fide is a potent p300/CBP inhibitor

YK-3-237 (B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid) reduces acetylation of mtp53 and exhibits anti-proliferative effects toward triple-negative breast cancer (TNBC) cells carrying mtp53.

PTACH (Cpd 51) (NCH-51) is a SAHA-based inhibitor of human HDAC. It can potently inhibit the growth of various human Y cells (EC50: 1 to 10 μM).

4-Hydroxyestrone, an endogenous estrogen metabolite, can strongly protect neuronal cells against oxidative damage.

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

R306465 (JNJ-16241199) is an orally active and selective class I histone deacetylase (HDAC 1) inhibitor with an IC50 of 3.3 nM. R306465 has a broad spectrum of antitumor activity, can induce histone 3 acetylation, and induce apoptosis, and can be used to study solid tumors and hematological malignancies.

CGP 3466B maleate (Omigapil maleate) is an orally bioavailable GAPDH nitrosylation inhibitor. Omigapil maleate abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease. Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD).

SIRT6-IN-5(SIRT6 inhibitor 5) is a potent and selective SIRT6 inhibitor with an IC50 value of 34 μM.SIRT6-IN-5 is immunosuppressive and chemo-sensitizing, increases H3K9 acetylation and glucose uptake in cultured cells, and reduces T-cell proliferation.

Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.

RK-9123016 is a SIRT2 inhibitor. RK-9123016 increases the acetylation level of eukaryotic translation initiation factor 5A (eIF5A), a physiological substrate of SIRT2, and reduces cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression.