histone deacetylase (hdac)

Droxinostat (NS 41080) is a selective HDAC inhibitor, primarily targeting HDACs 6 and 8 with IC50 values of 2.47 μM and 1.46 μM, respectively. It is over 8-fold more selective against HDAC3 and shows no inhibition for HDAC1, 2, 4, 5, 7, 9, and 10.

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.

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

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.

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.

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.

Rac-Belinostat (PX-105684) is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase.

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.

4-Phenylbutyric acid (Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and an endoplasmic reticulum stress (ERS) inhibitor. 4-Phenylbutyric acid can be used to treat urea cycle disorders.

Belinostat (PXD101) is an inhibitor of hydroxamic acid-type histone deacetylase (HDAC, IC50 of 27 nM in HeLa cell extracts),and with antineoplastic activity.

Manganese chloride tetrahydrate is a high-purity manganese salt that can serve as a cofactor for enzyme reactions and provide essential trace elements in cell culture, and is commonly used in biochemical experiments.

TMP195 (TFMO 2) is a selective class IIa histone deacetylase (HDAC) inhibitor.

HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor [inducing apoptosis, with potential antineoplastic (antitumor) and chemopreventive activities], inhibiting cell proliferation and regulating cell differentiation (IC50=0.0056 µM, 72 h) in murine erythroleukemia cells.

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.

CHDI-390576 is a CNS-permeable, selective and potent dibenzoyl isohydroxamic acid class IIa histone deacetylase (HDAC) inhibitor that inhibits class IIa HDAC 4, HDAC 5, HDAC 7, HDAC 9, and can be used in cancer research.

Nanatinostat (CHR-3996) is an HDAC inhibitor with selectivity and oral bioavailability, with IC50 values of 3-7 nM for HDAC1 2 3 and >200 nM for other subtypes. Nanatinostat also inhibits tumour cell proliferation and induces apoptosis, for studying neurodegenerative diseases and cancer.

Oxamflatin (Metacept-3) is a selective histone deacetylase (HDAC) inhibitor characterized by high potency (IC50 = 15.7 nM) and the presence of an alkyne group capable of undergoing azide-alkyne cycloaddition reactions (CuAAc).

SW-100 is a selective histone deacetylase 6 inhibitor (IC50: 2.3 nM). It also shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays an obviously improved ability to cross the blood-brain-barrier.

Tefinostat (CHR-2845) is a potent monocyte macrophage-targeted histone deacetylase (HDAC) inhibitor that is cleaved to the active acid CHR-2847 by intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat exhibits antitumor activity and can be used in the study of leukemia and advanced hematologic malignancies.

HDAC-IN-76 (compound 6i), a histone deacetylase (HDAC) inhibitor, demonstrates robust antimalarial activity, particularly against the asexual blood stages of Plasmodium. The compound exhibits potent efficacy with IC 50 values of 30 nM and 98 nM against Pf3D7 (chloroquine drug-susceptible strain) and PfDd2 (chloroquine drug-resistant strain), respectively. Moreover, HDAC-IN-76 shows selective inhibition towards parasites, displaying IC 50 values of 7 nM and 9 nM against human HDAC1 and HDAC6, respectively, and effectively inhibits PfHDAC1.

CDK HDAC-IN-4 is a highly selective dual inhibitor of cyclin-dependent kinase (CDK) and histone deacetylase (HDAC), with IC50 values of 88.4 nM and 168.9 nM, respectively. This compound exhibits antiproliferative effects in both hematologic and solid tumor cells. Additionally, CDK HDAC-IN-4 induces apoptosis and S-phase cell cycle arrest in MV-4-11 cells. It has also demonstrated significant antitumor efficacy in an MV-4-11 xenograft model.

HDAC-IN-82 (Compound 18b) is a histone deacetylase (HDAC) inhibitor that demonstrates selective antimalarial and anticancer activities. It shows significant antiproliferative and caspase3 7 activity in tumor cells. Additionally, HDAC-IN-82 induces hyperacetylation of histone H3 and α-tubulin.

HDAC-IN-83 (compound 9D) is an inhibitor of histone deacetylase (HDAC), demonstrating an IC50 of 0.01 μM for HDAC1 and 0.44 μM for HDAC6. It exhibits anticancer and antiproliferative activities and promotes caspase-3 7 activation. The compound inhibits Cal27, HepG2, and MRC-5 cells with IC50 values of 0.693 μM, 0.427 μM, and 3.19 μM, respectively.