HDAC-IN-99
HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer.
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- Formule: C23H25BN4O3S
- Masse moléculaire:448.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
HDAC1 48.09 nM (IC50) |
HDAC2 300.28 nM (IC50) |
HDAC6 9.16 nM (IC50) |
In Vitro
HDAC-IN-99 (Z16) potently inhibits the activities of HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). It exhibits over 15-fold higher selectivity for HDAC6 than class I HDACs, while showing extremely low activity against HDAC8 (IC50 = 37.77 μM)[1].
HDAC-IN-99 inhibits the growth of various cancer cell lines, with IC50 values of 0.05 μM (HeLa), 0.07 μM (HCT116), 0.1 μM (SKOV3), 0.04 μM (MDA-MB-231) and 0.02 μM (Jurkat) against different cell lines[1].
HDAC-IN-99 (0-250 nM, 48 h) induces concentration-dependent S-phase cell cycle arrest and apoptosis in HCT116 cells, accompanied by increased acetylation levels of histone H3, histone H4 and α-tubulin, upregulated p21 expression, and cleavage of caspase-3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:0, 40, 100, 250
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Incubation Time:48 h
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Result:Induced concentration-dependent S-phase cell cycle arrest and apoptosis in HCT116 cells, accompanied by increased acetylation of histone H3, histone H4, and α-tubulin, upregulation of p21, and cleavage of caspase-3.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | CL | Vz | AUC0-t | AUC0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 2880.00 ng/mL | 0.08 h | 1.28 h | 1.45 L/h/kg | 2.63 L/kg | 1667.93 ng·h/mL | 1750.26 ng·h/mL | / |
| Rat[1] | 20 mg/kg | i.p. | 2040.83 ng/mL | 2.00 h | 5.48 h | 0.96 L/h/kg | 7.24 L/kg | 16130.71 ng·h/mL | 17274.30 ng·h/mL | 98.70 % |
| Mice[1] | 2 mg/kg | i.v. | 1245.26 ng/mL | 0.08 h | 0.66 h | 6.25 L/h/kg | 5.77 L/kg | 405.27 ng·h/mL | 425.22 ng·h/mL | / |
| Mice[1] | 20 mg/kg | i.p. | 1248.09 ng/mL | 1.40 h | 1.25 h | 4.83 L/h/kg | 8.53 L/kg | 4226.64 ng·h/mL | 4092.64 ng·h/mL | 96.25 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 4-6 weeks old, SPF grade)[1]
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Dosage:30 mg/kg; 40 mg/kg
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Administration:i.p.; q.d.
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Result:Achieved a tumor growth inhibition (TGI) rate of 26.32%.
Achieved a tumor growth inhibition (TGI) rate of 45.80%.
Caused no significant changes in body weight during the study.
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Masse moléculaire 448.35
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Formule C23H25BN4O3S
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SMILES
O=C(N[C@H](C1=NC=C(C2=CC3=C(C=C2)C=CC=C3)N1)CCCCCB(O)O)C4=CN=CS4
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-99 Related Classifications
HY-181843 Related Classifications
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