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 番号: 3032392-39-2
- 分子式: C33H32N4O4
- 分子量:548.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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 |
|---|---|---|---|---|
| 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 |
体外実験
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).
体内実験
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.
化学情報
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CAS 番号 3032392-39-2
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分子量 548.63
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
GK444 関連分類
HY-155328 関連分類
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