HDAC-IN-36
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research.
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- No. CAS: 2482992-54-9
- Fòrmula: C29H39N5O5
- Peso molecular:537.65
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
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HDAC6 11.68 nM (IC50) |
HDAC10 13.24 nM (IC50) |
HDAC3 79.17 nM (IC50) |
HDAC1 86.93 nM (IC50) |
HDAC2 97.32 nM (IC50) |
HDAC8 378.2 nM (IC50) |
HDAC4 >1000 nM (IC50) |
HDAC5 >1000 nM (IC50) |
HDAC7 >1000 nM (IC50) |
HDAC9 >1000 nM (IC50) |
HDAC11 >1000 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
0.732 μM
Compound: 23g
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Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
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[PMID: 32791401] |
| MDA-MB-231 | IC50 |
1.155 μM
Compound: 23g
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Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by MTT assay
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[PMID: 32791401] |
| MDA-MB-231 | IC50 |
1.167 μM
Compound: 23g
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Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
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[PMID: 32791401] |
| MDA-MB-231 | IC50 |
1.323 μM
Compound: 23g
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Antiproliferative activity against human MDA-MB-231 cells measured after 24 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 24 hrs by MTT assay
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[PMID: 32791401] |
In Vitro
HDAC-IN-36 (compound 23 g) (0-10, 24 h) exhibits good antiproliferative activity in MDA-MB-231 cells, promotes the acetylation of α-Tubulin and HSP90[1].
HDAC-IN-36 (0-10, 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, and mainly induces mitochondrial-dependent apoptosis[1].
HDAC-IN-36 (0-10, 24 h) inhibits MDA-MB-231 cells migration in a dose-dependent manner, increases the expression of E-cadherin and decreases the expression of MMP-2 obviously[1].
HDAC-IN-36 (0-10, 24 h) induces noteworthy autophagy, increases the expression of Beclin1, LC3II and decreases the expression of SQSTM1/p62[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells[1]
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Concentration:0, 2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Exhibited good anti-proliferative activity in MDA-MB-231 cells, with IC50 of 1.32 ± 0.13 μM, increased the acetylation level of intracellular proteins, and promoted the acetylation of α-Tubulin and HSP90.
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Cell Line:MDA-MB-231 cells[1]
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Concentration:0, 2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Induced apoptosis in MDA-MB-231 cells in a dose-dependent manner.
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Cell Line:MDA-MB-231 cells[1]
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Concentration:0, 2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Induced noteworthy autophagy with increased aggregation of LC3 puncta.
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Cell Line:MDA-MB-231 cells[1]
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Concentration:0, 2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Mainly induced mitochondrial-dependent apoptosis, up-regulated the expression of Bax and downregulated the expression of Bcl-2, and increased the cleavage of caspase3, caspase8 and caspase9; increased the expression of E-cadherin and decreased the expression of MMP-2 obviously; increased the expression of Beclin1, LC3II and decreased the expression of SQSTM1/p62.
In Vivo
HDAC-IN-36 (Beagles, 20 mg/kg, Orally, once) shows a significant improvement in pharmacokinetic parameters[1].
Pharmacokinetic Parameters of HDAC-IN-36 in male Beagles[1].
| Parameters | 23g (20 mg/kg) |
| T1/2 (h) | 1.24 ± 0.21 |
| Tmax (h) | 0.79 ± 0.33 |
| Cmax (μg/L) | 120.36 ± 15.53 |
| AUC0-t (μg/L∗h) | 1275.35 ± 70.17 |
| AUC0-∞ (μg/L∗h) | 1289.40 ± 88.91 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zebrafish (MDA-MB-231-derived xenograft model, Wild-type AB strain)[1]
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Dosage:0, 2.5, 5 μg/mL
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Administration:3 days
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Result:Inhibited tumor formation and migration in a dose-dependent manner, and improved in vivo anti-tumor efficacy.
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Animal Model:Beagles (female, 8-10 kg, n = 4)[1]
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Dosage:20 mg/kg (dissolved 0.5% sodium carboxyl methyl cellulose (CMC-Na) aqueous solution)
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Administration:Orally, once (Pharmacokinetic Analysis)
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Result:Showed a significant improvement in pharmacokinetic parameters with T1/2 value of 1.24 h.
Chemical Information
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No. CAS 2482992-54-9
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Peso molecular 537.65
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Fòrmula C29H39N5O5
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SMILES
COC1=CC(OC)=C2C(N=C(N=C2N3CCN(CC3)C)C4=CC(C)=C(C(C)=C4)OCCCCCC(NO)=O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-36 Related Classifications
HY-146684 Related Classifications
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