Other HDAC Inhibitors

No data suggesting HDAC class selectivity.

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A2478 APHA Compound 8 ≥98% (HPLC), solid One of a class of aroyl pyrrole hydroxy amide (APHA) compounds showing histone deacetylase (HDAC) inhibition, Compound 8 is the most potent and HDAC class I-selective.
 
B4061 BATCP ≥98% (HPLC), solid HDAC 6 selective substrate (over HDAC 1, Class II over Class I).
 
C0494 Cambinol ≥97% (HPLC), white powder Cambinol is a Sirtuin (Human Silent Information Regulator) Type 1/2 Inhibitor. Sirtuins are structurally and mechanistically unrelated to HDACs Class 1 & 2 deacetylases but share many protein targets. HDAC is a large complex enzyme family involved in epigenetic-control of gene expression. Sirt2 has an IC50 equal to 59 μM.
 
EPS003   CUDC 101 A potent inhibitor of HDACs and receptor tyrosine kinases    
EPI008   Histone Deacetylase (HDAC) Inhibitor Set I Set includes 6 inhibitors • Apicidin - A potent, cell permeable inhibitor of histone deacetylase (IC50 = 700 pM for parasitic histone deacetylase). Inhibits HeLa cell proliferation (IC50 = 50-100 nM) and induces the transcriptional activation of p21 (WAF1) in a reversible manner. Also prevents H-ras-induced invasive phenotype of MCF-10A cells possibly by down regulating MMP-2 in a reversible manner.
• M344 - An amide analog of Trichostatin A that potently Inhibits histone deacetylases (IC50 = 40 nM for rat liver HDAC and IC50 = 100 nM for maize HDAC). Induces differentiation and inhibits proliferation (~2 μM) of murine erythroleukemia cells.
• Sodium 4-phenylbutuyrate - Inhibitor of histone deacetylase (HDAC). Anti-neoplastic agent and transcriptional regulator. Also acts as an inducer of tumor cytostasis and differentiation.
• Splitomycin - Potent inhibitor of yeast NAD+ dependent histone deacetylase Sir2p (IC50= 60 μM). Sensitizes mammalian cells to a variety of DNA-damaging agents by abrogating Sir2p activity on p53. Acts by either altering or blocking access to the acetylated histone binding pocket.
• Trichostatin A - Potent, reversible inhibitor of histone deacetylase. Mediates the activation of O6- methylguanine-DNA methyltransferase (MGMT). May be involved in cell cycle progression of several cell types, induces cell growth arrest at both G1 and G2/M phases. In some cases induces apoptosis.
• Valproic acid sodium salt - A cell-permeable histone deacetylase 1 (HDAC1) inhibitor (IC50 = 400 μM) that exhibits anticancer, anti-inflammatory and neuroprotective properties. Recently it has been reported that Valproic acid enables reprogramming of primary human fibroblasts with only two factors, Oct4 and Sox2, without the need for the oncogenes c-Myc or Klf4.

 
EPI009   Histone Deacetylase (HDAC) Inhibitor Set II Set includes 7 inhibitors • CI-994 - Cell-permeable. A histone deacetylase (HDAC) inhibitor: Ki values are 0.41, 0.75, >100 and >100 μM for HDAC1, HDAC3, HDAC6 and HDAC8, respectively. Displays significant antitumor activity in vitro and in vivo against a broad spectrum of murine and human tumor models.
• Panobinostat (LBH589) - Highly potent inhibitor of both histone deacetylase 1 (HDAC1) activity and tumour cell proliferation in vitro. The IC50 values of HDAC isozymes HDAC1-IP Ac-H4, HDAC8, MALunselective, B61HDAC1 and B12HDAC6 are 0.23±0.06, 283±29, 75±4, 47±5 and 89±12 nM, respectively. And to A2780 proliferation, IC50 value is 4.6±1.8 nM.
• SAHA - Potent, reversible inhibitor of histone deacetylase 1 (HDAC1) and 3 (HDAC3). Induces cell growth arrest at both G1 and G2 phases. Induces apoptosis.
• SBHA - Competitive histone deacetylase (HDAC) inhibitor that has been shown to inhibit HDAC1 (IC50 = 0.25 μM) and HDAC3 (IC50 = 0.30 μM). SBHA causes cell differentiation, cell cycle arrest, or apoptosis. SBHA also enhances cytotoxicity induced by Oxaliplatin in the colorectal cancer cell lines.
• Scriptaid - A relatively non-toxic Inhibitor of histone deacetylase (HDAC). Facilitates transcriptional activation (TGF-ß/Smad4) in both stable and transient receptor assays in a concentration-dependent manner. At ~2 μg/ml (6-8 μM) concentrations, results in a greater than 100-fold increase in histone acetylation in PANC-1 cells.
• Trichostatin A - Potent, reversible inhibitor of histone deacetylase. Mediates the activation of O6-methylguanine-DNA methyltransferase (MGMT). May be involved in cell cycle progression of several cell types, induces cell growth arrest at both G1 and G2/M phases. In some cases induces apoptosis.
• Tubacin - Tubacin (Tubulin acetylation inducer) is a highly potent, selective, reversible, and cell-permeable inhibitor of histone deacetylase 6 (HDAC6, IC50 = 4 nM). Displays 1000-fold more selectivity for HDAC6 over other HDACs. It inhibits α-tubulin deacetylation in mammalian cells. Unlike trichostatin A (TSA), which is a broad spectrum HDAC inhibitor, tubacin is specific for the tubulin deacetylase activity of HDAC6. Tubacin causes increased acetylation of α-tubulin, accumulation of polyubiquitinated proteins, and apoptosis. It does not affect global histone deacetylation, gene-expression profiling, or cell cycle progression mediated α-tubulin deacetylation in mammalian cells.

 
M5820 M344 ≥98% (HPLC), powder M344 is a HDAC inhibitor; subtype selective for HDAC6 over HDAC1. M344 inhibits HDAC (IC50 = 100 nM) and also inhibits hyperacetylation of histone H4, terminal cell differentiation, transcription (γ-globin), and tumor cell death.
 
M2195 MOCPAC ≥95% (HPLC), solid Selective HDAC1 substrate (over HDAC6, class I over class II).
 
EPS002 MS-275 A HDAC1 and HDAC3 inhibitor HDAC inhibitor; antiproliferative.
 
P5874 PTACH ≥98% (HPLC), solid HDAC inhibitor; more potent than the majority of HDAC inhibitors except for SAHA (gold standard).
 
R5010 Resveratrol ≥99% (HPLC) Resveratrol is a phenolic phytoalexin found in grape skin and other plants. It has intracellular antioxidant activity and activates SIRT1, a NAD+-dependent histone deacetylase involved in mitochondrial biogenesis and the enhancement of peroxisome proliferator-γ-activated receptor coactivator-1α (PGC-1α) and FOXO activity. The anti-diabetic, neuroprotective and anti-adipogenic actions of resveratrol may be mediated via SIRT1 activation.
human ... AR(367), CYP1A2(1544), ESR1(2099), SIRT1(23411)
mouse ... Nos2(18126)
rat ... Esr1(24890)
S4068 Splitomicin ≥98% (HPLC), powder Sir2p (silent information regulator) and HDAC inhibitor.
Splitomicin, a derivative of β-naphthol is an inhibitor of Silent Information Regulator 2 (SIR2). It inhibits the NAD+-dependent deacetylase activity of Sir2 in vitro. It increases the levels of cyclic AMP by inhibiting the activity of cyclic AMP phosphodiesterase, interferes with mobilization of intracellular Ca+2 and ATP release. This results in inhibition of platelet aggregation that is effective in cardiovascular and cerebrovascular diseases.