HDAC inhibitor

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1 2 3 6 7 11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

MPI_5a is an effective and selective inhibitor of HDAC6 (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms and it also inhibits acyl-tubulin accumulation in cells (IC50: 210 nM).

ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but shows no activity towards other HDAC inhibitors.

Tucidinostat (Chidamide) is an effective and orally bioavailable HDAC enzymes class I (HDAC1 2 3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 11 (IC50: 733 432 nM), and shows no effect on HDAC4 5 6 7 9.

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1 2 4 6 (IC50=36 47 510 1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

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.

Tasquinimod (ABR-215050) is an oral antiangiogenic agent with potential antitumor activity. It is also an S100A9 inhibitor and binds to the HDAC4Zn2+ binding structural domain with Kd values between 10 and 30 nM.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

ACY-957 (HDAC Inhibitor C001) is an orally active and selective inhibitor of HDAC1 and HDAC2 (IC50s: 7 nM, 18 nM, and 1300 nM against HDAC1 2 3) and shows no inhibition on HDAC4 5 6 7 8 9.

CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor. CRA-026440 hydrochloride exhibits Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM, respectively. CRA-026440 hydrochloride exhibits antitumor and antiangiogenic activities.

SS-208 is a selective inhibitor of HDAC6 (IC50 = 12 nM) with anti-tumor activity. SS-208 shows selectivity over other HDAC subtypes.

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.

HDAC8-IN-20a (HDAC8 inhibitor-20a) is a potent and selective HDAC8 inhibitor with an IC50 of 27 nM. HDAC8-IN-20a blocks activation of growth receptor survival signals.

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.

Patamostat mesylate (E-3123) is a potent protease inhibitor with IC50 values of 39 nM for trypsin, 950 nM for plasmin, and 1.9 μM for thrombin. This compound demonstrates promising potential in suppressing the pathogenesis and development of acute pancreatitis.

MPT0G211 is a highly selective and orally active HDAC6 inhibitor (IC50=0.291 nM) that has neuroprotective effects and has shown anti-metastatic activity in human breast cancer cells. MPT0G211 has 1,000 times more affinity for HDAC6 than other HDAC subtypes. MPT0G211 can cross the blood-brain barrier and could be used to improve tau phosphorylation and cognitive deficits in Alzheimer's disease models.

mTOR HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].

mTOR HDAC-IN-1 HCl is a potent dual inhibitor of mTOR and HDAC with potential anti-inflammatory, anti-proliferative, autophagy and apoptosis-inducing effects for cancer research.

ST7612AA1 is a novel potent and oral HDCA inhibitor that acts as an HIV-1 latency reactivator. ST7612AA1 showed significant antitumor activity at low concentrations in vitro and in vivo. ST7612AA1 has potential anticancer activity and can be used to study malaria.

MC2590 is a potent and selective histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.

Bufexamac (Bufexamic acid) is a COX inhibitor for IFN-α release with anti-inflammatory, analgesic, and antipyretic action.

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

Sodium butanoate (Sodium Butyrate) is the sodium salt of butyrate with potential antineoplastic activity. Butyrate, a short chain fatty acid, competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).

Sodium 4-phenylbutyrate (TriButyrate), a transcriptional regulator, reversibly inhibits class I and II histone deacetylases (HDACs )resulting in a global increase in gene expression, decreased cellular proliferation, increased cell differentiation, and the induction of apoptosis in susceptible tumor cell populations.