1-Naphthohydroxamic acid

Name: 1-Naphthohydroxamic acid
Brand: MedChemExpress
SKU: HY-130538
Rating: 4.5 (1 reviews)

Cat. No.: HY-130538 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC₅₀ of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC₅₀ >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity.1-Naphthohydroxamic acid can induce tubulin acetylation.

For research use only. We do not sell to patients.

1-Naphthohydroxamic acid Chemical Structure

CAS No. : 6953-61-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 72	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 72	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 65	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All HDAC Isoform Specific Products:

View All Isoforms

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Purity & Documentation
References
Customer Review

Description

1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC₅₀ of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC₅₀ >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity^[1]^[2].1-Naphthohydroxamic acid can induce tubulin acetylation^[3].

IC₅₀ & Target^[1]

HDAC8

14 μM (IC₅₀)

HDAC1

>100 μM (IC₅₀)

HDAC6

>100 μM (IC₅₀)

In Vitro

1-Naphthohydroxamic acid (compound 2; 20-40 μM; 0-144 ?hours; BE(2)-C, SK-N-BE(2) and SH-SY5Y cells) treatment reduces cell numbers in a concentration-dependent manner^[2].
1-Naphthohydroxamic acid (compound 2) at concentrations in the range of its in vitro IC₅₀ against HDAC8 results in reduced cell density and outgrowth of neurite-like structures that stained positive for neurofilament.1-Naphthohydroxamic acid reduces the formation of clones in soft-agar concentration dependently^[2].
When either cell type (HeLa and HEK293 cells) is treated with 1-Naphthohydroxamic acid (compound 2; 0.8 μM, 4 μM, 20 μM or 100 μM), only tubulin becomes hyperacetylated^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	BE(2)-C, SK-N-BE(2) and SH-SY5Y cells
Concentration:	20 µM, 40 µM
Incubation Time:	0 hours, 24 hours, 48 hours, 72 hours, 96 hours, and 144 hours
Result:	Reduced cell numbers in a concentration-dependent manner.

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. 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^[3].
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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NMRI Foxn1 nude mice^[3]
Dosage:	0 mg/kg, 50 mg/kg, 100mg/kg, 200 mg/kg, 300 mg/kg 400 mg/kg
Administration:	Intraperitoneal injection; daily; for 10 days
Result:	Dose-limiting toxicities (DLTs) included weight loss and signs of liver toxicity, as evidenced by elevated plasma liver enzymes and detection of necrotic areas on histological liver examination.

Molecular Weight

187.19

Formula

C₁₁H₉NO₂

CAS No.

6953-61-3

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2C=CC=CC2=CC=C1)NO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (667.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.3422 mL	26.7108 mL	53.4217 mL
5 mM	1.0684 mL	5.3422 mL	10.6843 mL
10 mM	0.5342 mL	2.6711 mL	5.3422 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.72%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (255 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Krennhrubec K, et al. Design and evaluation of 'Linkerless' hydroxamic acids as selective HDAC8 inhibitors. Bioorg Med Chem Lett. 2007 May 15;17(10):2874-8. [Content Brief]

[2]. Oehme I, et al. Histone deacetylase 8 in neuroblastoma tumorigenesis. Clin Cancer Res. 2009 Jan 1;15(1):91-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	5.3422 mL	26.7108 mL	53.4217 mL	133.5541 mL
	5 mM	1.0684 mL	5.3422 mL	10.6843 mL	26.7108 mL
	10 mM	0.5342 mL	2.6711 mL	5.3422 mL	13.3554 mL
	15 mM	0.3561 mL	1.7807 mL	3.5614 mL	8.9036 mL
	20 mM	0.2671 mL	1.3355 mL	2.6711 mL	6.6777 mL
	25 mM	0.2137 mL	1.0684 mL	2.1369 mL	5.3422 mL
	30 mM	0.1781 mL	0.8904 mL	1.7807 mL	4.4518 mL
	40 mM	0.1336 mL	0.6678 mL	1.3355 mL	3.3389 mL
	50 mM	0.1068 mL	0.5342 mL	1.0684 mL	2.6711 mL
	60 mM	0.0890 mL	0.4452 mL	0.8904 mL	2.2259 mL
	80 mM	0.0668 mL	0.3339 mL	0.6678 mL	1.6694 mL
	100 mM	0.0534 mL	0.2671 mL	0.5342 mL	1.3355 mL