HDAC11-IN-5
Based on 1 Customer Validation
HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC50 of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.25%
- Fòrmula: C24H25Cl2F3N4O2
- Peso molecular:529.38
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC11 0.021 μM (IC50) |
SHMT2 |
In Vitro
HDAC11-IN-5 (Compound 25) potently inhibits purified HDAC11 protein with an IC50 of 0.021 ± 0.005 μM, and shows no significant inhibition of HDAC1, HDAC6, HDAC7, or HDAC8 at concentrations up to 10 μM[1].
HDAC11-IN-5 (96 h) potently inhibits proliferation of U937, OCI-AML2, THP-1, and MOLM13 AML cell lines with IC50 values of 6.3 μM, 5.7 μM, 5.4 μM, and 6.7 μM, respectively[1].
HDAC11-IN-5 (10-20 μM; 6 h) selectively inhibits intracellular HDAC11 in U937 AML cells, as shown by increased SHMT2 fatty acylation at 10 μM for 6 h and no significant changes in histone H3 or α-tubulin acetylation at 20 μM for 6 h[1].
HDAC11-IN-5 (8 μM; 48 h) strongly induces apoptosis in U937 and OCI-AML2 AML cells[1].
HDAC11-IN-5 (8 μM; 48 h) induces G1-phase cell cycle arrest in U937 AML cells[1].
HDAC11-IN-5 (8 μM; 48 h) promotes myeloid differentiation of U937 AML cells, as shown by increased CD14 and CD11b expression[1].
HDAC11-IN-5 (8 μM; 48 h) induces ferroptosis in U937 AML cells, as shown by increased lipid peroxidation, cellular ROS, and intracellular Fe2+ levels[1].
HDAC11-IN-5 (5-20 μM; 96 h) exhibits strong synergistic antiproliferative activity with ivosidenib in U937, OCI-AML2, and MLL-AF9 mouse AML cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U937 AML cells
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Concentration:10 μM (SHMT2 fatty acylation analysis); 20 μM (histone H3 and α-tubulin acetylation analysis)
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Incubation Time:6 h
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Result:Significantly increased fatty acylation levels of SHMT2 (a specific HDAC11 substrate) at 10 μM for 6 h.
Had negligible effects on acetylation levels of histone H3 (a class I HDAC substrate) and α-tubulin (an HDAC6 substrate) at 20 μM for 6 h.
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Cell Line:U937, OCI-AML2 AML cell lines
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Concentration:8 μM
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Incubation Time:48 h
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Result:Significantly induced apoptosis in both U937 and OCI-AML2 cells.
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Cell Line:U937 AML cells
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Concentration:8 μM
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Incubation Time:48 h
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Result:Significantly increased expression of the myeloid differentiation markers CD14 and CD11b in U937 cells, with a stronger effect than FT895.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (6-week-old female, 20-22 g, tail vein injection of 1×105 MLL-AF9-GFP+ leukemic cells)[1]
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Dosage:50 mg/kg
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Administration:I.g.,; once daily; 14 days
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Result:Reduced the percentage of GFP+ leukemic cells in peripheral blood.
Significantly extended the survival of AML mice compared to vehicle control.
Reduced the percentage of GFP+ leukemic cells when combined with ivosidenib, with greater survival extension than either agent alone.
Caused no significant body weight loss prior to the moribund stage.
- HL-60 granulocytic/neutrophil-like differentiation
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- Apoptosis Solutions
- Protocol for Cell Cycle
- Ferroptosis Solutions
Chemical Information
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Appearance Solid
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Peso molecular 529.38
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Fòrmula C24H25Cl2F3N4O2
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Color Light brown to yellow
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SMILES
O=C(C1=CC=CC2=C1C=C(C#CC3=CC=CC(C(F)(F)F)=C3)N2CCN4CCNCC4)NO.Cl.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (188.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8890 mL | 9.4450 mL | 18.8900 mL | 47.2251 mL |
| 5 mM | 0.3778 mL | 1.8890 mL | 3.7780 mL | 9.4450 mL | |
| 10 mM | 0.1889 mL | 0.9445 mL | 1.8890 mL | 4.7225 mL | |
| 15 mM | 0.1259 mL | 0.6297 mL | 1.2593 mL | 3.1483 mL | |
| 20 mM | 0.0945 mL | 0.4723 mL | 0.9445 mL | 2.3613 mL | |
| 25 mM | 0.0756 mL | 0.3778 mL | 0.7556 mL | 1.8890 mL | |
| 30 mM | 0.0630 mL | 0.3148 mL | 0.6297 mL | 1.5742 mL | |
| 40 mM | 0.0472 mL | 0.2361 mL | 0.4723 mL | 1.1806 mL | |
| 50 mM | 0.0378 mL | 0.1889 mL | 0.3778 mL | 0.9445 mL | |
| 60 mM | 0.0315 mL | 0.1574 mL | 0.3148 mL | 0.7871 mL | |
| 80 mM | 0.0236 mL | 0.1181 mL | 0.2361 mL | 0.5903 mL | |
| 100 mM | 0.0189 mL | 0.0945 mL | 0.1889 mL | 0.4723 mL |
HDAC11-IN-5 Related Classifications
HY-182019 Related Classifications
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