HDAC3-IN-4
HDAC3-IN-4 is a selective and orally active HDAC3 inhibitor with an IC50 of 89 nM. HDAC3-IN-4 induces the degradation of PD-L1 by regulating cathepsin B (CTSB) in the lysosomes, with a DC50 of 5.7 μM. HDAC3-IN-4 shows better selectivity for HDAC3 over HDAC1, HDAC6, HDAC7, and HDAC8.
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- CAS No.: 2988762-46-3
- Formule: C22H25N5O2S
- Masse moléculaire:423.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
HDAC3 89 nM (IC50) |
HDAC1 730 nM (IC50) |
HDAC6 >10 μM (IC50) |
HDAC7 >10 μM (IC50) |
HDAC8 >10 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16-F10 | IC50 |
1.2 μM
Compound: HQ-30
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Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
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[PMID: 39031090] |
| HCT-116 | IC50 |
0.43 μM
Compound: HQ-30
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
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[PMID: 39031090] |
| HepG2 | IC50 |
0.24 μM
Compound: HQ-30
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Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
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[PMID: 39031090] |
| Jurkat | IC50 |
0.09 μM
Compound: HQ-30
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Antiproliferative activity against human Jurkat T cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay
Antiproliferative activity against human Jurkat T cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay
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[PMID: 39031090] |
| MCF7 | IC50 |
2.94 μM
Compound: HQ-30
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
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[PMID: 39031090] |
In Vitro
HDAC3-IN-4 (compound HQ-30) shows potent antiproliferative potency, with IC50 values of 0.09 μM, 0.43 μM, 1.20 μM, 2.94 μM, and 0.24 μM against Jurkat (T lymphoma), HCT-116 (colorectal carcinoma), B16-F10 (melanoma), MCF-7 (breast cancer), and HepG2 (hepatoma) cells, respectively[1].
HDAC3-IN-4 (0.5-8 μM; 48 h) induces apoptosis in B16-F10 cells in a concentration-dependent manner[1].
HDAC3-IN-4 (0.5-4 μM; 48 h) dose-dependently increases the percentage of cell cycle arrest in the G2/M phase and reduced the percentage G0/G1 phase in B16-F10 cells[1].
HDAC3-IN-4 (0.5-4 μM; 24 h) causes significant upregulation of acetylated-H3 (Ac-H3). HDAC3-IN-4 downregulates/degrades PD-L1 expression via the lysosomal pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:B16-F10 cells
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Concentration:0.5 μM, 1 μM, 2 μM, 4 μM, and 8 μM
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Incubation Time:48 h
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Result:Induced cancer cell apoptosis.
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Cell Line:B16-F10 cells
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Concentration:0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:48 h
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Result:Dose-dependently increased the percentage of cell cycle arrest.
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Cell Line:B16-F10 cells
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Concentration:0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:24 h
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Result:Caused significant upregulation of acetylated-H3.
In Vivo
Pharmacokinetic Parameters of HDAC3-IN-4 in Male Sprague-Dawley rats[1].
| PK parameters | i.v. administration (2 mg/kg, n = 6) | p.o. administration (20 mg/kg, n = 6) |
| AUC0-t (ng/mL·h) | 521.85 ± 93.78 | 2742.08 ± 768.82 |
| AUC0-∞ (ng/mL·h) | 529.16 ± 91.38 | 3032.62 ± 805.03 |
| MRT0-t (h) | 0.52 ± 0.09 | 3.19 ± 0.84 |
| MRT0-∞ (h) | 0.55 ± 0.10 | 4.48 ± 1.75 |
| t1/2 (h) | 0.4 ± 0.10 | 3.6 ± 1.6 |
| Tmax (h) | 0.14 ± 0.08 | 0.50 ± 0 |
| CL (L/h/kg) | 3.87 ± 0.65 | 7.27 ± 3.10 |
| Vz (L/kg) | 2.21 ± 0.64 | 34.45 ± 12.38 |
| Cmax (ng/mL) | 725.25 ± 169.59 | 1038.18 ± 514.59 |
| F (%) | - | 57 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six weeks old C57BL/6J male mice (6 weeks old) injected B16 cells[1]
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Dosage:25 mg/kg
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Administration:p.o.; per day; for 9 days
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Result:Decreased the tumor volume and tumor weight with tumor growth inhibitions.
Chemical Information
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CAS No. 2988762-46-3
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Masse moléculaire 423.53
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Formule C22H25N5O2S
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SMILES
O=C(C1=NC=C(CNC2=CC=CC=C2)S1)NCC3=CC=C(C(NNCCC)=O)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC3-IN-4 Related Classifications
HY-159172 Related Classifications
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