HDAC-IN-9
HDAC-IN-9 is a potent and selective tubulin and HDAC dual inhibitor. HDAC-IN-9 inhibits the invasion and migration of A549 cells. HDAC-IN-9 shows potent antitumor and antiangiogenic effect in vitro and in vivo.
For research use only. We do not sell to patients.
- Formula: C33H38N2O4
- Molecular Weight:526.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
HDAC1 6.8 μM (IC50) |
HDAC2 0.06 μM (IC50) |
HDAC6 0.12 μM (IC50) |
HDAC8 8.5 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.78 μM
Compound: 17
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Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
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[PMID: 38823265] |
| U-937 | IC50 |
0.371 μM
Compound: 17
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Cytotoxicity against human U-937 cells
Cytotoxicity against human U-937 cells
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[PMID: 38823265] |
In Vitro
HDAC-IN-9 (compound 4s) shows anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 µM for MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells, respectively)[1].
HDAC-IN-9 displays 6.1, 3.2 and 4.6-fold selectivity ratios for 293 T, macrophages, and L02 cells respectively (IC50s of 10.89, 5.63, 8.14 µM for 293 T, macrophages, and L02 cells, respectively)[1].
HDAC-IN-9 shows inhibition activities against HDAC isoforms (IC50s of 6.8, 0.06, 0.12, 8.5 µM for HDAC 1, HDAC 2, HDAC 6, HDAC 10, respectively)[1].
HDAC-IN-9 (1, 2, 4 µM; 72 h; A459 cells) induces cell cycle arrest at the G2/M phase in a concentration-dependent manner[1].
HDAC-IN-9 (1, 2, 4 µM; 72 h) induces apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells[1].
HDAC-IN-9 (0, 0.5, 1, 2 µM; 48 h) shows anti-proliferative activity by the inhibition of angiogenesis and the reduction of endothelial cell metastasis in A549 cells[1].
HDAC-IN-9 (0, 1, 2, 4 µM, 48 h) inhibits the invasion and migration of A549 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:MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells
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Concentration:
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Incubation Time:72 h
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Result:Showed anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 µM for MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells, respectively).
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Cell Line:A459 cells
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Concentration:0, 1, 2, 4 µM
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Incubation Time:72 h
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Result:Cells were arrested at the G2/M phase with a dose-dependent manner.
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Cell Line:A459 cells
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Concentration:0, 1, 2, 4 µM
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Incubation Time:72 h
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Result:Induced apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells.
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Cell Line:A459 cells
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Concentration:0, 1, 2, 4 µM
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Incubation Time:72 h
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Result:Showed down regulation of Cyclin B1 and Pcdc2 levels.
In Vivo
HDAC-IN-9 (0, 2.5, 5, 10 µM; 3 days) inhibits the proliferation and metastasis of A549 cells in zebrafish xenograft models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:embryos of Tg(flk:EGFP) transgenic zebrafish (transgenic zebrafish model Tg(flk1:EGFP))[1]
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Dosage:0, 10, 20, 40 µM
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Administration:
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Result:Suppressed the formation of ISVs in zebrafish embryos.
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Animal Model:zebrafish xenograft models[1]
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Dosage:0, 2.5, 5, 10 µM
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Administration:3 days
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Result:Inhibited the proliferation and metastasis of A549 cells in zebrafish xenograft models.
Chemical Information
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Molecular Weight 526.67
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Formula C33H38N2O4
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SMILES
[H][C@]12CC[C@@]3([C@H](CC[C@]3([C@@]1(CCC4=CC(OCC5=CC=C(C=C5)C(NC6=C(C=CC=C6)N)=O)=C(C=C42)OC)[H])[H])O)C
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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 migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)