hdac4

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.

SantacruzaMate A (CAY-10683) is a potent and selective HDAC inhibitor.

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

TMP269 is an effective, specific class IIa HDAC inhibitor for HDAC4 (IC50: 157 nM), HDAC5 (IC50: 97 nM), HDAC7 (IC50: 43 nM), and HDAC9 (IC50: 23 nM), respectively.

Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors.

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4 nM, 2.4 nM, and 15.7 nM, respectively.

Quisinostat (JNJ-26481585) (JNJ-26481585) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7.

LMK-235 is a potent HDAC inhibitor, and is used in cancer research.

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

Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.

HDAC4 CHDI Degrader 11 is a potent, selective degrader of HDAC4 (PROTAC) with DC_50 values of 4 nM and 6 nM in Jurkat E6-1 and Jurkat cells, respectively. This compound integrates the class IIa HDAC inhibitor trifluoromethyloxadiazole with a ligand for the Von Hippel-Lindau (VHL) protein through a linker. Demonstrating significant efficacy, HDAC4 CHDI Degrader 11 achieves a DC_50 value of 1 nM in a mouse cell model of Huntington's disease. For enhanced degradation in neuroblastoma cell lines, it can be administered alongside the P-glycoprotein inhibitor, Elacridar.

HDAC4-IN-1 (compound 1a), a class IIa HDACI inhibitor with an IC 50 of 0.077 μM, exhibits anticancer activity by enhancing Caspase-induced apoptosis. It is also utilized in cancer drug combination research [1].

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.

ACY-1083 is a selective, brain-penetrating HDAC6 inhibitor (IC50: 3 nM) that effectively reverses chemotherapy-induced peripheral neuropathy.

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.

BRD 9757 (N-Hydroxy-1-cyclopentene-1-carboxamide) is a selective inhibitor of HDAC6 (IC50 = 30 nM).

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.

3-Hydroxybutyric acid (Butanoic acid) (or beta-hydroxybutyrate) is a ketone body. Like the other ketone bodies (acetoacetate and acetone), levels of 3-hydroxybutyrate in blood and urine are raised in ketosis. In humans, 3-hydroxybutyrate is synthesized in the liver from acetyl-CoA and can be used as an energy source by the brain when blood glucose is low. Blood levels of 3-hydroxybutyric acid levels may be monitored in diabetic patients to look for diabetic ketoacidosis. Persistent mild hyperketonemia is a common finding in newborns. Ketone bodies serve as an indispensable source of energy for extrahepatic tissues, especially the brain and lung of developing mammals. Another important function of ketone bodies is to provide acetoacetyl-CoA and acetyl-CoA for the synthesis of cholesterol, fatty acids, and complex lipids. During the early postnatal period, acetoacetate (AcAc) and beta-hydroxybutyrate are preferred over glucose as substrates for synthesis of phospholipids and sphingolipids in accord with requirements for brain growth and myelination. Thus, during the first 2 weeks of postnatal development, when the accumulation of cholesterol and phospholipids accelerates, the proportion of ketone bodies incorporated into these lipids increases. On the other hand, an increased proportion of ketone bodies is utilized for cerebroside synthesis during the period of active myelination. In the lung, AcAc serves better than glucose as a precursor for the synthesis of lung phospholipids. The synthesized lipids, particularly dipalmitoylphosphatidylcholine, are incorporated into surfactant, and thus have a potential role in supplying adequate surfactant lipids to maintain lung function during the early days of life (PMID: 3884391 ). 3-Hydroxybutyric acid is found to be associated with fumarase deficiency and medium-chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism.

CHDI 00484077 is a highly selective, central nervous system (CNS) permeable Class IIa HDAC inhibitor with inhibitory effects on HDAC4, HDAC5, HDAC7, and HDAC9, which improves neuronal function, and can be used to study Huntington's disease.

Ricolinostat (Rocilinostat) is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity.

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

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.

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.