HDAC1-IN-5
Based on 1 publication(s) in Google Scholar
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice.
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- Formule: C20H21N3O2S
- Masse moléculaire:367.46
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) HDAC1-IN-5
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Activité biologique
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HDAC1 15 nM (IC50) |
HDAC6 20 nM (IC50) |
HDAC1-IN-5 (compound 4j) (0-50 μM; 48 h) exhibits strong inhibitory effects on HCT116, HeLa, HepG2, MC38, K562 and HEL[1].
HDAC1-IN-5 (0.16-1.5 μM; 48 h) induces apoptosis in a dose-dependent manner[1].
HDAC1-IN-5 (0.17-1.5 μM; 24 h or 48 h) induces downregulation of SPT16 and SSRP-1, induces the cleavage of caspase-3, and increases the expression of Acetyl-Histone H3 and Acetyl-α-tubulin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, HeLa, HepG2, MC38, K562 and HEL
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Concentration:0-50 μM
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Incubation Time:48 h
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Result:Showed strong inhibitory effects on HCT116, HeLa, HepG2, MC38, K562 and HEL with IC50s of 0.47 μM, 0.78 μM, 1.4 μM, 0.43 μM, 0.91 μM and 0.28 μM, respectively.
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Cell Line:HCT116
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Concentration:0.16 μM, 0.5 μM and 1.5 μM
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Incubation Time:48 h
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Result:Induced apoptosis in a dose-dependent manner, and induced 38.5% at the concentration of 1.5 μM (both early and late apoptotic cells).
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Cell Line:HCT116 and MC38
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Concentration:0.17 μM, 0.5 μM and 1.5 μM
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Incubation Time:24 h or 48 h
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Result:Induced downregulation of SPT16 and SSRP-1 in HCT116.
Induced the cleavage of caspase-3 in HCT116 and MC38.
Increased the expression of HDAC1, 2, 6 substrate Acetyl-Histone H3 and Acetyl-α-tubulin with a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (6-10 weeks; 2×106 MC38 cells were injected subcutaneously into the right flank regions)[1]
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Dosage:50 and 100 mg/kg
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Administration:IP; every two days; for 16 days
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Result:Significantly decreased the tumor volume and weight with tumor growth inhibition (TGI) of 66% at 50 mg/kg.
Chemical Information
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Masse moléculaire 367.46
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Formule C20H21N3O2S
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SMILES
ONC(CCCCCC1=CC=CC(C2=NN=C(C3=CC=CC=C3)S2)=C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Metab Eng
Metabolic engineering of commensal bacteria for gut butyrate delivery and dissection of host-microbe interaction. [Abstract]2023 Nov:80:94-106. PMID: 37717646
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC1-IN-5 Related Classifications
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