hdac

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.

PARP-1/HDAC-IN-1 is an effective dual inhibitor of PARP-1 and HDAC6, with IC50 values of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 exhibits anti-cancer, anti-migration, and anti-angiogenesis activities.

HDAC-IN-51 is an 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.

MDK-7933 (HDAC8-IN-1) is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines. MDK-7933 shows antiproliferative effects toward several human lung cancer cell lines (A549, H1299, and CL1-5). HDAC8-IN-1 exhibits cytotoxicity against human lung CL1-5 cells without significant cytotoxicity for normal IMR-90 cells[1].

HDAC-IN-3 (GSK3117391A) is a potent histone deacetylase (HDAC) inhibitor, and treatment chronic inflammatory disorders.

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.

HDAC-IN-7, an analogue of Tucidinostat (Chidamide), is a HDAC inhibitor. HDAC-IN-7 inhibits acetylation of histone protein H3 and induces apoptosis in human colon cancer cell lines[1].

BRD-6929 is a selective, brain-penetrant HDAC1 and HDAC2 inhibitor (IC50:  1 and 8 nM). BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 (Kis: 0.2 and 1.5 nM) [2]. BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV

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 a small molecule inhibitor and a highly selective HDAC6 inhibitor (IC50=36 nM). The IC50 value for MPI_5a inhibition of intracellular acetylated tubulin accumulation is 210 nM, used for HDAC6 function research.

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 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.

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.

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.

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 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.