HDAC6-IN-77
HDAC6-IN-77 is a highly selective HDAC6 inhibitor with an IC50 of 7.0 nM.HDAC6-IN-77 induces neurite outgrowth.HDAC6-IN-77 exerts neuroprotective activity.HDAC6-IN-77 shows no significant toxicity on dopaminergic cells.HDAC6-IN-77 can be used for the research of Alzheimer's disease.
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- CAS No.: 3126891-54-8
- 화학식: C17H16ClFN2O2
- 분자량:334.77
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
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HDAC6 7.0 nM (IC50) |
In Vitro
HDAC6-IN-77 (compound 8g) potently and selectively inhibits purified HDAC6 with an IC50 of 7.0 nM, and exhibits negligible activity against HDAC1, HDAC2, HDAC3, HDAC5 and HDAC8[1].
HDAC6-IN-77 (1-9 μM; 6 h) selectively increases the level of acetylated α-tubulin (a marker of HDAC6 inhibition) in a dose-dependent manner in PC-12 cells in vitro, without affecting the level of acetylated histone H3 (a marker of class I HDAC inhibition)[1].
HDAC6-IN-77 (20 μM) shows no significant cytotoxicity in PC-12 cells[1].
HDAC6-IN-77 (0.5-2 μM; 48 h) promotes axonal growth in PC-12 cells, with an axonal growth rate of 80.2%, and exhibits a dose-dependent effect within the concentration range of 0.5, 1 and 2 μM[1].
HDAC6-IN-77 (10 μM; 24 h) exerts neuroprotective activity against H2O2-induced oxidative damage in PC-12 cells[1].
HDAC6-IN-77 (10 μM; 24 h) exerts neuroprotective activity against 6-OHDA-induced oxidative damage in PC-12 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Rat dopaminergic pheochromocytoma PC-12 cells
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Concentration:1 μM (6 h incubation); 1-9 μM (no specified incubation time)
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Incubation Time:6 h (1 μM); unspecified (1, 3, 9 μM)
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Result:Increased acetylated α-tubulin levels relative to vehicle control, with no notable increase in acetylated histone H3 levels at 1 μM for 6 h.
Showed a dose-dependent increase in acetylated α-tubulin levels at concentrations of 1, 3, and 9 μM, with no corresponding increase in acetylated histone H3 levels.
Chemical Information
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CAS No. 3126891-54-8
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분자량 334.77
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화학식 C17H16ClFN2O2
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SMILES
ClC1=CC=C(CCN(CC2=CC=C(C(NO)=O)C=C2F)C3)C3=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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PC12 NGF-Induced Neuronal Differentiation Culture
PC12 cells are a rat adrenal pheochromocytoma clonal line that responds to NGF by stopping proliferation and extending branching neurite-like processes; after longer NGF exposure, cells develop long processes and neuronal-like ultrastructural and functional features. NGF-induced differentiation is read out mainly by neurite outgrowth, reduced proliferation, microtubule assembly, and neuronal differentiation-associated proteins such as MAPs, tau, GAP-43, and synapsin-1.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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SH-SY5Y Neuronal Differentiation Culture
SH-SY5Y neuronal differentiation culture uses sequential exposure to retinoic acid and neurotrophic factors to reduce proliferative neuroblastoma-like behavior and induce neuron-like morphology, including neurite extension, neuronal marker expression, and, in RA/BDNF protocols, greater synaptic-marker expression than undifferentiated culture. Retinoic acid is commonly used as the initiating differentiation cue, while BDNF in serum-reduced or serum-free medium supports later maturation and neurotrophic-factor-dependent neuron-like survival.
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SH-SY5Y neuronal-like differentiation
SH-SY5Y neuronal-like differentiation uses defined culture conditions to shift proliferative human neuroblastoma cells toward a neuron-like state, mainly assessed by reduced proliferation, neurite extension, neuronal-marker expression, and, in some protocols, increased dependence on neurotrophic support. Retinoic acid (RA) is commonly used for the first differentiation phase, and sequential RA followed by brain-derived neurotrophic factor (BDNF) in serum-free medium is a well-characterized approach for generating neuron-like SH-SY5Y cultures with extensive neurite outgrowth. The primary readouts are morphology-based neurite outgrowth and marker-based confirmation using proteins such as βIII-tubulin, MAP2, GAP43, synaptophysin, NeuN, NSE, TH, or related neuronal/synaptic markers, depending on the study endpoint.
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Cell differentiation
Cell differentiation refers to the process in which cells of the same origin gradually produce cell groups with different morphological structure and functional characteristics.
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PC12 NGF-induced neuronal-like differentiation
PC12 cells are a rat adrenal pheochromocytoma-derived clonal cell line that responds to nerve growth factor by stopping proliferation and extending neurites, producing a sympathetic neuron-like phenotype used to study neuronal differentiation and neurite outgrowth. NGF acts through TrkA-dependent signaling, and neurite outgrowth is associated with ERK/Akt signaling, microtubule organization, neuronal-marker expression, and increased electrophysiological neuronal features such as sodium-channel density. The main assay readout is morphological differentiation, usually measured as the percentage of neurite-bearing cells, neurite length, neurite number, or total neurite length per cell. Additional readouts include GAP-43, tyrosine hydroxylase, βIII-tubulin, neurofilament, synapsin I, synaptophysin, ERK phosphorylation, Akt phosphorylation, and sodium-channel current density.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)