GK444
GK444 is a selective HDAC1, HDAC2 and HDAC3 inhibitor with IC50 values of 100 nM, 116 nM and 361 nM, respectively. GK444 reduces TGF-β1-induced COL1A1 mRNA levels. GK444 exhibits anticancer activity against lung cancer, astrocytoma and colorectal cancer. GK444 exerts antifibrotic effects in Bleomycin (HY-108345)-induced pulmonary fibrosis mouse models.
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- CAS No.: 3032392-39-2
- Formule: C33H32N4O4
- Masse moléculaire:548.63
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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
- Protocole
- Pureté et documentation
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
HDAC1 100 nM (IC50) |
HDAC2 116 nM (IC50) |
HDAC3 361 nM (IC50) |
HDAC6 >100,000 nM (IC50) |
HDAC4 >100,000 nM (IC50) |
HDAC8 >10,000 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
6.8 μM
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Antiproliferative activity against human A549 epithelial lung cancer cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human A549 epithelial lung cancer cells assessed as viability reduction incubated 72 hrs by MTT assay.
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37795958 |
| SF-268 | IC50 |
4.8 μM
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Antiproliferative activity against human SF268 astrocytoma cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human SF268 astrocytoma cells assessed as viability reduction incubated 72 hrs by MTT assay.
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37795958 |
In Vitro
GK444 (up to 20 μM) does not reduce the viability of primary normal lung fibroblasts at concentrations up to 20 μM[1].
GK444 (5-10 μM; 1 h) reduces TGF-β1-induced COL1A1 mRNA levels in primary normal lung fibroblasts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 human epithelial lung cancer cells, SF268 astrocytoma cells, and Caco-2 cells
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Concentration:0.5, 1, 3, 5, 10, and 25 μM
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Incubation Time:72 h
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Result:Inhibited A549 cell proliferation with IC50 6.8 μM and SF268 cell proliferation with IC50 4.8 μM.
Similar antiproliferative activity against Caco-2 cells was observed (IC50 1.9 to 6.1 μM group range, Table S2).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (C57/Bl6; male and female; 8-10 weeks old)[1]
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Dosage:30 mg/kg
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Administration:i.p.; twice daily; from day -1 to day 14
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Result:Decreased total protein levels in BALF (pulmonary edema) compared with the BLM group.
Decreased soluble collagen levels in BALF.
Decreased Col1a1 mRNA expression in whole-lung tissue.
Decreased the numbers of fibrotic masses and collagen deposition in lungs by histopathological analysis.
Chemical Information
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CAS No. 3032392-39-2
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Masse moléculaire 548.63
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Formule C33H32N4O4
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SMILES
O=C([C@@H]1CCC(N1CC2=CC=CC=C2)=O)NCC3=CC=C(OCC4=CC=C(C(NC5=CC=CC=C5N)=O)C=C4)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)
GK444 Related Classifications
HY-155328 Related Classifications
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