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
- 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
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hHDAC1 7 nM (IC50) |
hHDAC6 9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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] |
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.
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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.
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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