1-Naphthohydroxamic acid

Catalog No.E6577

Technical Data

Formula	C11H9NO2
Molecular Weight	187.19	CAS No.	6953-61-3
Solubility (25°C)*	In vitro


* <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.)

Biological Activity

Description	1-Naphthohydroxamic acid (Compound 2) demonstrates potent and selective inhibition of HDAC8 (IC50 = 14 μM), exhibiting significantly greater selectivity for HDAC8 compared to class I HDAC1 and class II HDAC6 (IC50 >100 μM). This compound does not elevate global histone H4 acetylation levels nor decrease total intracellular HDAC activity. Additionally, 1-naphthohydroxamic acid has been shown to promote tubulin acetylation.
In vivo	Dose-limiting toxicities (DLTs) of 1-Naphthohydroxamic acid (compound 2; 0-40 mg/kg; intraperitoneal injection; daily; for 10 day; NMRI Foxn1 nude mice) include weight loss and signs of liver toxicity, as evidenced by elevated plasma liver enzymes and detection of necrotic areas on histological liver examination. This compound has the maximum tolerable doses at 50?mg/kg per day. At these concentrations, neither body weight nor blood parameters are critically changed. Pharmacokinetic studies after intraperitoneal administration of the inhibitors identified the half-life of this chemical to be ~15?min, with a plasma peak concentration of ~30?μM.

Description

1-Naphthohydroxamic acid (Compound 2) demonstrates potent and selective inhibition of HDAC8 (IC50 = 14 μM), exhibiting significantly greater selectivity for HDAC8 compared to class I HDAC1 and class II HDAC6 (IC50 >100 μM). This compound does not elevate global histone H4 acetylation levels nor decrease total intracellular HDAC activity. Additionally, 1-naphthohydroxamic acid has been shown to promote tubulin acetylation.

In vivo

Dose-limiting toxicities (DLTs) of 1-Naphthohydroxamic acid (compound 2; 0-40 mg/kg; intraperitoneal injection; daily; for 10 day; NMRI Foxn1 nude mice) include weight loss and signs of liver toxicity, as evidenced by elevated plasma liver enzymes and detection of necrotic areas on histological liver examination. This compound has the maximum tolerable doses at 50?mg/kg per day. At these concentrations, neither body weight nor blood parameters are critically changed. Pharmacokinetic studies after intraperitoneal administration of the inhibitors identified the half-life of this chemical to be ~15?min, with a plasma peak concentration of ~30?μM.

Protocol (from reference)

References

https://www.ncbi.nlm.nih.gov/17346959
https://www.ncbi.nlm.nih.gov/19118036

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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.

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