Identification | Back Directory | [Name]
1-NAPHTHOHYDROXAMIC ACID | [CAS]
6953-61-3 | [Synonyms]
NSC 57457 Naphthohydroxamicacid 1-NAPHTHOHYDROXAMIC ACID a-Naphthohydroxamic acid alpha-naphthohydroxamicacid 1-NAPHTHOHYDROXAMIC ACID 98+% HDAC Inhibitor XIX, Compound 2 1-Naphthalenecarbohydroximic acid n-hydroxy-1-naphthalenecarboxamid N-HYDROXYNAPHTHALENE-1-CARBOXAMIDE Naphthalene-1-carbohydroximic acid N-Hydroxy-1-naphthalenecarboxamide | [Molecular Formula]
C11H9NO2 | [MDL Number]
MFCD00059546 | [MOL File]
6953-61-3.mol | [Molecular Weight]
187.19 |
Chemical Properties | Back Directory | [Melting point ]
176-178 °C | [density ]
1.291±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥5mg/mL | [form ]
White solid | [pka]
8.91±0.30(Predicted) | [color ]
white to tan |
Hazard Information | Back Directory | [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.
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| [IC 50]
HDAC8: 14 μM (IC50); HDAC1: >100 μM (IC50); HDAC6: >100 μM (IC50) | [storage]
Store at -20°C |
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Company Name: |
Energy Chemical
|
Tel: |
021-021-58432009 400-005-6266 |
Website: |
http://www.energy-chemical.com |
Company Name: |
Maya High Purity Chemicals
|
Tel: |
+86 (573) 82222445 (0)18006601000 452520369 |
Website: |
m.is0513.com/ShowSupplierProductsList15221/0.htm |
Company Name: |
TCI Europe
|
Tel: |
320-37350700 |
Website: |
https://www.tcichemicals.com/de/de/index.html |
Company Name: |
TCI AMERICA
|
Tel: |
800-4238616 |
Website: |
https://www.tcichemicals.com/en/us/index.html |
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