2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. 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 .

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

HDAC6-IN-69

HDAC6-IN-69 Chemical Structure

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HDAC6-IN-69 Related Antibodies

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

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Description

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 [1].

IC50 & Target[1]

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)

In Vitro

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.

HDAC6-IN-69 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human neuroblastoma cells
Concentration: 0.1 μM,1 μM,10 μM
Incubation Time: 24 h
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

Cell Cytotoxicity Assay[1]

Cell Line: L-glutamate induced-SH-SY5Y cells
Concentration: 0.1 μM,1 μM,10 μM
Incubation Time: 0.5 h
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
In Vivo

HDAC6-IN-69 (compound 8k) (6 or 12.5 mg/kg, i.v., once) shows a great potential for alleviating stroke-induced brain infarction in MCAO rat model[1].

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

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].
Dosage: 6 or 12.5 mg/kg
Administration: i.v., once
Result: Reduced the cerebral infarction area (from 32.87% to 13.13%).
Molecular Weight

425.30

Formula

C17H17BrN2O4S
SMILES

O=C(NO)C1=CC=C(CN(CCC2)C3=CC=C(Br)C=C3S2(=O)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HDAC6-IN-69 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC6-IN-69HDACHistone deacetylasesHDAC6Neuroprotective Agentα-tubulinischemic strokeInhibitorinhibitorinhibit

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