C1A
C1A is a class I/II HDACs and sirtuin inhibitor with an IC50 of 479 nM for HDAC6. C1A induces sustained acetylation of HDAC6 substrates, α-tubulin and HSP90. C1A shows srtong anticancer effcts, and induces apoptosis in cancer cells.
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- No. CAS: 1021463-02-4
- Fòrmula: C22H25Cl2N3O4S
- Peso molecular:498.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC6 0.48 μM (IC50) |
HDAC8 0.61 μM (IC50) |
HDAC3 5.5 μM (IC50) |
HDAC10 9.8 μM (IC50) |
HDAC2 11 μM (IC50) |
HDAC1 14 μM (IC50) |
HDAC5 15 μM (IC50) |
HDAC4 16 μM (IC50) |
HDAC7 49 μM (IC50) |
HDAC9 56 μM (IC50) |
SIRT3 55 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| KMS-11 | GI50 |
0.48 μM
Compound: 22
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Antiproliferative activity against human KMS-11 cells incubated for 72 hrs by sulphorhodamine B assay
Antiproliferative activity against human KMS-11 cells incubated for 72 hrs by sulphorhodamine B assay
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[PMID: 29133060] |
| SH-SY5Y | IC50 |
0.28 μM
Compound: 22
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Antiproliferative activity against human SH-SY5Y cells incubated for 72 hrs by sulphorhodamine B assay
Antiproliferative activity against human SH-SY5Y cells incubated for 72 hrs by sulphorhodamine B assay
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[PMID: 29133060] |
In Vitro
C1A (2.5-10 μM; 24 h) increases the sub-G1 population in a drug concentration-related manner. And C1A induces apoptosis and inhibits proliferation of a panel of human tumour cell lines from different origins in the low micromolar range[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells
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Concentration:2.5 μM, 5 μM, 7.5 μM, 10 μM
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Incubation Time:24 h
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Result:Increased the sub-G1 population in a drug concentration-related manner.
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Cell Line:HCT-116 cells
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Concentration:0.5 μM, 1 μM, 2.5 μM, 5 μM, 7.5 μM, 10 μM
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Incubation Time:4 h and 24 h
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Result:Induced sustained acetylation of HDAC6 substrates, α-tubulin and HSP90.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nu/nu-BALB/c mice injected with HCT-116 cells[1]
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Dosage:20 mg/kg, 40 mg/kg
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Administration:ip; once a day, twice a day, once every two days; for 14 days
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Result:Inhibited the growth of colon tumours in vivo.
Chemical Information
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No. CAS 1021463-02-4
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Peso molecular 498.42
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Fòrmula C22H25Cl2N3O4S
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SMILES
ClCCN(C1=CC=C(C=C1)S(NC2=CC=C(C=C2)/C=C(C)/C=C/C(NO)=O)(=O)=O)CCCl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
C1A Related Classifications
HY-124946 Related Classifications
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