1-NAPHTHOHYDROXAMIC ACID
1-NAPHTHOHYDROXAMIC ACID Basic information
- Product Name:
- 1-NAPHTHOHYDROXAMIC ACID
- Synonyms:
-
- HDAC Inhibitor XIX, Compound 2 - CAS 6953-61-3 - Calbiochem
- Naphthalene-1-carbohydroximic acid
- N-Hydroxy-1-naphthalenecarboxamide
- a-Naphthohydroxamic acid
- NSC 57457
- HDAC Inhibitor XIX, Compound 2
- N-HYDROXYNAPHTHALENE-1-CARBOXAMIDE
- alpha-naphthohydroxamicacid
- CAS:
- 6953-61-3
- MF:
- C11H9NO2
- MW:
- 187.19
- Product Categories:
-
- Hydroxylamines
- Hydroxylamines (N-Substituted)
- Mol File:
- 6953-61-3.mol
1-NAPHTHOHYDROXAMIC ACID Chemical Properties
- Melting point:
- 176-178 °C
- Density
- 1.291±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥5mg/mL
- pka
- 8.91±0.30(Predicted)
- form
- White solid
- color
- white to tan
Safety Information
- Risk Statements
- 52
- WGK Germany
- 3
- RTECS
- QJ1894500
- HS Code
- 2928009090
1-NAPHTHOHYDROXAMIC ACID Usage And Synthesis
Uses
1-Naphthohydroxamic Acid is a potent HDAC inhibitor with efficacy against HDAC8, HDAC1 and HDAC6.
Biochem/physiol Actions
1-Naphthohydroxamic Acid is a cell-permeable, potent, and selective histone deacetylase 8 (HDAC8) inhibitor. 1-Naphthohydroxamic acid selectively inhibits HDAC8 (IC50 = 14 μM) over class I HDAC1 and class II HDAC6 (IC50 >100 μM). Treatment of cells with 1-Naphthohydroxamic acid does not increase neither global histone H4 nor tubulin acetylation . Also in contrast to the pan-HDAC inhibitors the compound is not reducing total intracellular HDAC activity.
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].
| 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. |
IC 50
HDAC8: 14 μM (IC50); HDAC1: >100 μM (IC50); HDAC6: >100 μM (IC50)
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