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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- 화학식: C27H26N4O4
- 분자량:470.52
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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] |
In Vitro
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.
Chemical Information
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분자량 470.52
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-76 Related Classifications
HY-161984 Related Classifications
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