HDAC6-IN-90
HDAC6-IN-90 is a selective HDAC6 inhibitor with an IC50 of 3.4 nM for hHDAC6 and an IC50 of 0.55 μM for zebrafish HDAC6. HDAC6-IN-90 induces Autophagy and modulates liquid-liquid phase separation by altering stress granule dynamics. HDAC6-IN-90 increases acetylated α-Tubulin. HDAC6-IN-90 exhibits anticancer activity against lung cancer.
For research use only. We do not sell to patients.
- Formula: C36H44FN5O6
- Molecular Weight:661.76
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
hHDAC6 3.4 nM (IC50) |
Zebrafish HDAC6 0.55 μM (IC50) |
hHDAC1 4626.3 nM (IC50) |
hHDAC10 32.8 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
20 μM
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Cytotoxicity against human A549 lung adenocarcinoma cells assessed as viability reduction incubated 24 hrs by MTT assay.
Cytotoxicity against human A549 lung adenocarcinoma cells assessed as viability reduction incubated 24 hrs by MTT assay.
|
42911756 |
| A549 | IC50 |
10 μM
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Cytotoxicity against human A549 lung adenocarcinoma cells assessed as viability reduction incubated 48 hrs by MTT assay.
Cytotoxicity against human A549 lung adenocarcinoma cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911756 |
In Vitro
HDAC6-IN-90 (20-0.0457 μM; 30 min) inhibits zHDAC6 CD2 with an IC50 of 0.55 μM[1].
HDAC6-IN-90 (50 μM-86.7 pM or 100 μM-8.67 nM; 90 min) inhibits HDAC10 with an IC50 of 32.8 nM in the TR-FRET assay[1].
HDAC6-IN-90 (5-80 nM; 16 h) engages HDAC6 in HeLa cells, increasing acetylated α-tubulin without substantial histone H3 hyperacetylation[1].
HDAC6-IN-90 (5 μM; 6 h) modulates LLPS in A549 cells by increasing stress-granule size after arsenite stimulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:5, 20, and 80 nM
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Incubation Time:16 h
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Result:Induced a dose-dependent increase in acetylated α-tubulin, while histone H3 acetylation remained limited.
The acetyl-α-tubulin/acetyl-H3 ratio increased with concentration.
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Cell Line:A549 human lung adenocarcinoma cells
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Concentration:10 and 30 μM for 48 h; 1, 3, 10, and 30 μM for 24 and 48 h
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Incubation Time:48 h; 24 and 48 h
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Result:Was among the most cytotoxic compounds at 10 and 30 μM.
IC50 was 20 μM at 24 h and IC50 was 10 μM at 48 h.
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Cell Line:A549 cells
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Concentration:10 μM
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Incubation Time:6 and 24 h
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Result:Markedly upregulated mRNA levels of ATG13, ATG5, ATG7, VSP34, UVRAG, LAMP1, ULK1, and BECN1.
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Cell Line:A549 3D multicellular tumor spheroid model
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Concentration:3 μM
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Incubation Time:7 days of exposure; days 0, 3, 5, and 7 (brightfield imaging); day 7 (Live/Dead staining)
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Result:Spheroids showed progressive structural alterations and peripheral disintegration by day 7.
Live/Dead staining showed reduced green fluorescence, strong diffuse red fluorescence, and a halo of detached cells and cellular fragments.
Spheroid viability was reduced relative to control.
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Cell Line:A549 cells
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Concentration:5 μM
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Incubation Time:6 h (pretreatment); 30 min (sodium arsenite); 6 h (Poly(I/C))
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Result:Increased G3BP1-positive stress-granule size after arsenite stimulation, consistent with the effect observed for all tested HDAC6 inhibitors.
Strong suppression of SG number was not attributed.
Chemical Information
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Molecular Weight 661.76
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Formula C36H44FN5O6
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SMILES
O=C(N(CC1=C(F)C=C(C(NO)=O)C=C1)CN2C3=CC=CC=C3)C42CCN(C[C@@H](O)[C@H](CC5=CC=CC=C5)NC(OC(C)(C)C)=O)CC4
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC6-IN-90 Related Classifications
HY-190947 Related Classifications
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