HDAC6-IN-84
HDAC6-IN-84 is a potent and selective HDAC6 inhibitor with an IC50 of 25.56 nM and shows 478-fold selectivity over HDAC1. HDAC6-IN-84 increases α-tubulin acetylation and upregulates BDNF (exons I and IV) and other neurogenesis-related genes. HDAC6-IN-84 can be used for the study of Alzheimer’s disease (AD) and other neurodegenerative diseases.
For research use only. We do not sell to patients.
- CAS No.: 3053402-10-8
- Formula: C17H16N2O3S
- Molecular Weight:328.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
HDAC6 25.56 nM (IC50) |
Cellular Effect
In Vitro
HDAC6-IN-84 (5h) inhibits HDAC6 with an IC50 of 25.56 nM and shows 478-fold selectivity over HDAC1[1].
HDAC6-IN-84 eliminates activity against HDAC2 and class IIa HDACs and further reduces activity against class I HDACs (HDAC1 and HDAC3)[1].
HDAC6-IN-84 (0.3-3 μM; 24 h) promotes α-tubulin acetylation in SH-SY5Y and HeLa cells, while negligibly affecting histone H3 acetylation[1].
HDAC6-IN-84 (0.1-10 μM; 24 h) shows low cytotoxicity in SH-SY5Y cells and HeLa cells.
HDAC6-IN-84 (1 μM) promotes neuronal gene activation and may enhance synaptic plasticity and development in human iPSC-derived NPCs[1].
HDAC6-IN-84 (1 μM; 24-48 h) upregulates BDNF exons I, II, and IV in human iPSC-derived neural progenitor cells (NPCs)[1].
HDAC6-IN-84 shows low inhibitory activities against CYP2C9, CYP2C19, CYP2D6, and CYP3A4 and exhibits low binding affinity to the hERG membrane channel, with an IC50 of 159.1 μM[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:SH-SY5Y cells, HeLa cells
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Concentration:0.3 μM, 1 μM, 3 μM
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Incubation Time:24 h
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Result:Promoted α-tubulin acetylation in a concentration-dependent manner while negligibly affecting histone H3 acetylation.
Selectively inhibited HDAC6 in the tested cells.
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Cell Line:SH-SY5Y cells, HeLa cells
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Concentration:0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
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Incubation Time:24 h
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Result:Showed low cytotoxicity in SH-SY5Y cells and HeLa cells.
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Cell Line:human iPSC-derived NPCs
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Concentration:1 μM
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Incubation Time:24 h
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Result:Upregulated BDNF exons I, II, and IV.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male 4-week-old ICR mice were treated with Scopolamine (HY-N0296) ( administered 30 min after compound treatment)[1].
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Dosage:0.015 mg/kg, 0.05 mg/kg, 0.15 mg/kg
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Administration:Intraperitoneal injection (i.p.); single administration
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Result:For the 24 h-training session, no group differences in step-through latency were observed.
Markedly recovered the scopolamine-induced impairment and restored step-through latency.
Chemical Information
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CAS No. 3053402-10-8
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Molecular Weight 328.39
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Formula C17H16N2O3S
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SMILES
O=C(NO)CCC1=CSC(C2=CC=C3C=C(OC)C=CC3=C2)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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-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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)