ACY-738

Catalog No.S8648 Batch:S864801

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Technical Data

Formula

C14H14N4O2
Molecular Weight 270.29 CAS No. 1375465-91-0
Solubility (25°C)* In vitro DMSO 54 mg/mL (199.78 mM)
Ethanol 1 mg/mL (3.69 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.
Targets
HDAC6 [1]
(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 min and concentration below 10 ng/ml after 2 h. ACY-738 rapidly distributes to the brain leading to a total drug exposure in CNS comparable to that of peripheral tissues[1]. 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[2].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Undifferentiated RN46A-B14 cells

  • Concentrations

    2.5 μM

  • Incubation Time

    4 h

  • Method

    Undifferentiated RN46A-B14 cells, a line of immortalized rat raphe neuronal precursors, are grown. They are treated with 2.5 μM ACY-738, ACY-775, tubastatin A, or 0.6 μM TSA, or vehicle (0.1% DMSO) for 4 h. Samples are processed using Epigentek histone extraction kit and quantified using protein assay.
Animal Study:

[1]
  • Animal Models

    Male NIH Swiss mice

  • Dosages

    5 mg/kg

  • Administration

    i.p.

Selleck's ACY-738 has been cited by 4 publications

Aggresome assembly at the centrosome is driven by CP110-CEP97-CEP290 and centriolar satellites [ Nat Cell Biol, 2022, 24(4):483-496] PubMed: 35411088
Histone deacetylase 6 plays an important role in TGF-β-induced murine Treg cell differentiation by regulating cell proliferation [ Sci Rep, 2022, 12(1):22550] PubMed: 36581745
The CP110-CEP97-CEP290 module orchestrates a centriolar satellite dependent response to proteotoxic stress [ bioRxiv, 2020, 10.1101/2020.12.20.423672] PubMed: None
HDAC6 dysfunction contributes to impaired maturation of adult neurogenesis in vivo: vital role on functional recovery after ischemic stroke [ J Biomed Sci, 2019, 26(1):27] PubMed: 30999900

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.