HDAC6-IN-69
HDAC6-IN-69 is a brain-penetrant and highly selective HDAC6 inhibitor with an IC50 of 4.0 nM. HDAC6-IN-69 shows >176-fold against other HDAC isoforms. HDAC6-IN-69 engages the target in neuronal cells by dose-dependently upregulating acetylated α-tubulin in virto. HDAC6-IN-69 has neuroprotective effect and can be used for ischemic stroke research .
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- Formule: C17H17BrN2O4S
- Masse moléculaire:425.30
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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HDAC1 1135 nM (IC50) |
HDAC3 9.0 nM (IC50) |
HDAC4 1248 nM (IC50) |
HDAC6 4.0 nM (IC50) |
HDAC8 702.5 nM (IC50) |
HDAC11 1243.0 nM (IC50) |
HDAC6-IN-69 (compound 8k) demonstrates a favorable pharmacokinetic profile with moderate clearance and metabolic stability in both human and rat liver microsomes (T1/2 in HLM = 154.00 min, T1/2 in RLM = 29.49 min), along with a low risk of cardiotoxicity.[1].
HDAC6-IN-69 (1.0-10 μM, 24 h) selectively inhibit HDAC6 rather than HDAC1 in human neuroblastoma cells (SH-SY5Y cells)[1].
HDAC6-IN-69 (0.1-10 μM, 0.5 h) has potential neuroprotective activity in L-glutamate (HY-N0455B) induced-SH-SY5Y cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human neuroblastoma cells
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Concentration:0.1 μM,1 μM,10 μM
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Incubation Time:24 h
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Result:Efficiently transported to SH-SY5Y cells and upregulated the expression of acetylated α-tubulin in a dose-dependent manner, while the expression of acetylated histone H3 was only moderately affected
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Cell Line:L-glutamate induced-SH-SY5Y cells
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Concentration:0.1 μM,1 μM,10 μM
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Incubation Time:0.5 h
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Result:Increased the survival rate of damaged cells at low and medium doses
Exhibit more stable neuroprotective activity and a wide therapeutic range
Showed a downward trend at high concentrations
Showed a high cell survival rate at high concentrations
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ischemia induced (a nylon thread was gently inserted from the common carotid artery into the middle cerebral artery for 1.5 hours)-male Sprague-Dawley (SD) rats (240 g)[1].
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Dosage:6 or 12.5 mg/kg
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Administration:i.v., once
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Result:Reduced the cerebral infarction area (from 32.87% to 13.13%).
Chemical Information
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Masse moléculaire 425.30
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Formule C17H17BrN2O4S
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SMILES
O=C(NO)C1=CC=C(CN(CCC2)C3=CC=C(Br)C=C3S2(=O)=O)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC6-IN-69 Related Classifications
HY-180214 Related Classifications
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