HDAC6-IN-12
HDAC6-IN-12 (compound GZ) is a potent HDAC6 inhibitor. HDAC6-IN-12 has anticancer activity through merges into DNA strands causing DNA damage. HDAC6-IN-12 can be used for cancer research.
For research use only. We do not sell to patients.
- CAS No.: 2803866-44-4
- Formula: C24H39F2N3O5
- Molecular Weight:487.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
0.66 μM
Compound: GZ
|
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
| A549 | IC50 |
0.14 μM
Compound: GZ
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
| HCT-116 | IC50 |
0.3 μM
Compound: GZ
|
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
| HeLa | IC50 |
0.43 μM
Compound: GZ
|
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
| Huh-7 | IC50 |
0.12 μM
Compound: GZ
|
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
| MDA-MB-231 | IC50 |
0.072 μM
Compound: GZ
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated in presence of 10 uM imatinib
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated in presence of 10 uM imatinib
|
[PMID: 35810950] |
| MDA-MB-231 | IC50 |
0.14 μM
Compound: GZ
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
| MDA-MB-231 | IC50 |
0.17 μM
Compound: GZ
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth pretreated with hENT1 inhibitor, dipyridamole at 10 uM followed by compound addition
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth pretreated with hENT1 inhibitor, dipyridamole at 10 uM followed by compound addition
|
[PMID: 35810950] |
| PANC-1 | IC50 |
1.08 μM
Compound: GZ
|
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
| SGC-7901 | IC50 |
3.7 μM
Compound: GZ
|
Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth
Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
| SK-OV-3 | IC50 |
0.62 μM
Compound: GZ
|
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth
|
[PMID: 35810950] |
HDAC6-IN-12 (compound GZ) (72 h) has anti-proliferative activity on tumor cells against HuH-7, HeLa, MDA-MB-231, SKOV3, A549, PANC-1, HCT-116, SGC7901 and 4T1 cells with IC50 values of 0.12 μM, 0.43 μM, 0.14 μM, 0.62 μM, 0.14 μM, 1.08 μM, 0.30 μM, 3.70 μM and 0.66 μM, respectively[1].
HDAC6-IN-12 (compound GZ) (0-3 μM; 24 h; MBA-MB-231 cells) merges into DNA strands causing DNA damage and increases the level of phospho-γ-H2A.X, which is the marker of DNA strand break[1].
HDAC6-IN-12 (compound GZ) (0-100 μM; 30 min) has major metabolic enzymes including CYP3A2, CYP1A1/2 isoforms[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MBA-MB-231 cells
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Concentration:0, 0.1, 0.3, 1 and 3 μM
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Incubation Time:24 hours
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Result:Increased the level of phospho-γ-H2A.X in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Bablc female mice[1]
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Dosage:5 and 10 mg/kg
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Administration:Intraperitoneal injection; once every three days, for 15 days
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Result:Inhibited tumor growth with TGI of 73.2% at 5 mg/kg and 83.8% at 10 mg/kg, respectively.
Chemical Information
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CAS No. 2803866-44-4
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Molecular Weight 487.58
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Formula C24H39F2N3O5
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SMILES
CCCCCCCCCCCCCCC(NC(C=CN1[C@@H]2O[C@H](CO)[C@H](C2(F)F)O)=NC1=O)=O
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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)