1-Naphthohydroxamic acid

SKU: orb1308735

Description

1-Naphthohydroxamic acid is a selective HDAC8 inhibitor (IC50 = 14 μM) with minimal activity against HDAC1 and HDAC6 (IC50 >100 μM). It induces tubulin acetylation without affecting global histone H4 acetylation or total intracellular HDAC activity, making it a useful tool for studying HDAC8-specific roles in cellular processes.

Research Area

Epigenetics & Chromatin, Molecular Biology

Images & Validation

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Key Properties

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CAS Number	6953-61-3
MW	187.19
Purity	>99.99% (May vary between batches)
Formula	C₁₁H₉NO₂
SMILES	ONC(=O)c1cccc2ccccc12
Target	HDAC
Solubility	DMSO:125 mg/mL (667.77 mM)

Bioactivity

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Target IC50	HDAC6:>100 μM\|HDAC8:14 μM\|HDAC1:>100 μM
In Vivo	1-Naphthohydroxamic acid has the maximum tolerable doses at 50 mg/kg per day. At these concentrations, neither body weight nor blood parameters are critically changed. 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. Pharmacokinetic studies after intraperitoneal administration of the inhibitors identified the half-life of 1-Naphthohydroxamic acid to be ~15 min, with a plasma peak concentration of ~30 μM. Read more...
In Vitro	1-Naphthohydroxamic acid (compound 2; 20-40 μM; 0-144 hours; BE(2)-C, SK-N-BE(2), and SH-SY5Y cells) reduces cell numbers in a concentration-dependent manner . It decreases clone formation in soft agar in a similar manner . In HeLa and HEK293 cells treated with 1-Naphthohydroxamic acid (compound 2; 0.8 μM, 4 μM, 20 μM, or 100 μM), only tubulin becomes hyperacetylated . At concentrations within its in vitro IC50 against HDAC8, 1-Naphthohydroxamic acid (compound 2) reduces cell density and induces outgrowth of neurofilament-positive neurite-like structures. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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deacetylate, hyperacetylated, Histone deacetylases, HDAC6, HDAC, HDAC1, HDAC8, Inhibitor, inhibit, clone, 1Naphthohydroxamic acid, 1-Naphthohydroxamic acid, 1 Naphthohydroxamic acid, acetylation, anti-proliferation, tubulin

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Compound Identifiers

PubChem CID

23382 ↗

Key Properties

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No computed properties available.

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