HDAC-IN-89
HDAC-IN-89 is an inhibitor of HDAC1 (IC50: 0.95 nM), HDAC2 (IC50: 0.86 nM), HDAC3 (IC50: 1.06 nM) and HDAC8 (IC50: 4.24 nM). HDAC-IN-89 blocks the cell cycle and induces apoptosis. HDAC-IN-89 has anti-tumor activity.
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- 화학식: C24H35F2N5O5S2
- 분자량:575.69
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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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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HDAC1 0.95 nM (IC50) |
HDAC2 0.86 nM (IC50) |
HDAC3 1.06 nM (IC50) |
HDAC8 4.24 nM (IC50) |
HDAC6 >1000 nM (IC50) |
HDAC-IN-89 (Compound 12) (0-10000 nM, 72 h) shows cytotoxicity against both NCI-H1975 (IC50: 0.57 μM) and HT-29 (IC50: 0.17 μM) cancer cells, but shows significantly reduced cytotoxicity against both WRL-68 (IC50: 2.6 μM) and HEK293 (IC50: 1.0 μM) normal cells[1].
HDAC-IN-89 (250 nM-1 μM, 48 h) induces cell cycle arrest in the G0/G1 phase of HT-29 cells and significantly promotes apoptosis of early and late cells at the corresponding concentrations[1].
HDAC-IN-89 (0-40 μM) has a small inhibitory effect on the hERG potassium channel (21%), indicating a low risk of cardiotoxicity[1].
HDAC-IN-89 (0.1 μM, 7-60 min) shows moderate metabolic stability (MF%: 30%-70%) and rapid clearance (Clint: 21.7-43.7 mL/min/g) in mouse, rat and human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Tumor cells (NCI-H1975 cells, HT-29 cells) and normal cells (WRL-68 cells, HEK293 cells)
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Concentration:0-10000 nM
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Incubation Time:72 h
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Result:Inhibited the activity of two cancer cells, NCI-H1975 (IC50: 0.57 μM) and HT-29 (IC50: 0.17 μM).
Reduced the toxicity to two normal cells, WRL-68 (IC50: 2.6 μM) and HEK293 (IC50: 1.0 μM).
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Cell Line:HT-29 cells
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Concentration:250 nM, 500 nM and 1μM
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Incubation Time:48 h
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Result:Induced cell cycle arrest in HT-29 cells at the G0/G1 phase (%G0/G1: 55.0%/57.2%/74.0%).
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Cell Line:HT-29 cells
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Concentration:250 nM and 500 nM
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Incubation Time:48 h
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Result:Promoted apoptosis of early cells (14.3%/19.7%) and late cells (7.57%/11.1%) at the corresponding concentrations (250 nM/500 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCI-H1975 xenograft model[1]
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Dosage:2.2 mg/kg and 11 mg/kg
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Administration:Intraperitoneal injection (i.p.), once every 3 days for 21 days
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Result:Inhibited tumor growth (63.5% and 87.9%).
Had no significant changes in body weight compared to the same dose of Romidepsin (2.2 mg/kg).
Chemical Information
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분자량 575.69
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화학식 C24H35F2N5O5S2
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SMILES
CC(C)[C@@H](C(N[C@H](/C=C/CCSSC[C@@H](C1=O)NC2=O)C(F)(F)C(N[C@@H]2C(C)C)=O)=O)NC(/C(N1)=C/C)=O
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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.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-89 Related Classifications
HY-173330 Related Classifications
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