ACY-738 - 99%, high purity , CAS No.1375465-91-0, Inhibitor of histone deacetylase 1;Inhibitor of histone deacetylase 2;Inhibitor of histone deacetylase 3;Inhibitor of histone deacetylase 6
ACY-738 - 99%, high purity , CAS No.1375465-91-0, Inhibitor of histone deacetylase 1;Inhibitor of histone deacetylase 2;Inhibitor of histone deacetylase 3;Inhibitor of histone deacetylase 6
ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of histone deacetylase 1;Inhibitor of histone deacetylase 2;Inhibitor of histone deacetylase 3;Inhibitor of histone deacetylase 6
Product Description
Information
ACY-738 inhibitsHDAC6with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.
Targets
HDAC6 (Cell-free) 1.7 nM
In vivo
ACY-738 induces dramatic increases in α-tubulin acetylation in brain and stimulate mouse exploratory behaviors in novel, but not familiar environments. ACY-738 has the antidepressant-like properties. Elimination of ACY-738 from plasma is rapid, with plasmatic half-life of 12\u2009min and concentration below 10\u2009ng/ml after 2\u2009h. ACY-738 rapidly distributes to the brain leading to a total drug exposure in CNS comparable to that of peripheral tissues. ACY-738 decreases several characteristics of SLE (Systemic lupus erythematosus) in NZB/W mice by dictating B cell development in the bone marrow. ACY-738 treatment increases the percentage of B cells in early developmental stages, while decreasing the percentage of cells in late pre-B cell fraction F. ACY-738 regulation of BM B cell development could be due to regulation developmental checkpoints known to be dysfunctional during SLE.
1.LoPresti P. (2019) The Selective HDAC6 Inhibitor ACY-738 Impacts Memory and Disease Regulation in an Animal Model of Multiple Sclerosis.. Front Neurol, 10 (13):(519). [PMID:31316445][10.1021/op500134e]
2.Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton O. (2014) Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability.. Neuropsychopharmacology, 39 (2):(389-400). [PMID:23954848][10.1021/op500134e]
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I2206157