HDAC-IN-76
HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C27H26N4O4
- 分子量:470.52
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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
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hHDAC1 7 nM (IC50) |
hHDAC6 9 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
136 μM
Compound: 6i
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Cytotoxicity against HEK293 cells incubated for 24 hrs by Neutral Red Uptake assay
Cytotoxicity against HEK293 cells incubated for 24 hrs by Neutral Red Uptake assay
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[PMID: 39208744] |
体外実験
HDAC-IN-76 has low toxicity to HEK293 cells[1].
HDAC-IN-76 (1 μM) effectively inhibits PfHDAC1 with an inhibition rate of 70.2%[1].
HDAC-IN-76 has low activity against liver-stage parasites (IC50 PbEEF (Extraerythrocytic liver stage of Plasmodium berghei)=0.25 μM), good microsomal stability (t1/2 > 60 min), and low toxicity in HEK293 cells (IC50=136 μM, selectivity index SI=544)[1].
HDAC-IN-76 can effectively enter HepG2 cells and inhibit HDAC activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK293
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Concentration:1%
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Incubation Time:24 h
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Result:Had low cytotoxicity to HEK293 cells.
化学情報
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分子量 470.52
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分子式 C27H26N4O4
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SMILES
O=C(CN(C(C1=CN(C)C2=C1C=CC=C2)=O)CC3=CC=C(C(NO)=O)C=C3)NCC4=CC=CC=C4
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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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)
HDAC-IN-76 関連分類
HY-161984 関連分類
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