Dac590
Based on 1 Customer Validation
Dac590 is an orally active and selective obesity-associated protein (FTO) inhibitor with an IC50 of 6.06 nM. Dac590 shows highly selective over ALKBH5 and ALKBH3. Dac590 suppresses oncogenic FTO signaling, induces myeloid differentiation, G1-phase cell cycle arrest, and apoptosis in acute myeloid leukemia (AML) cells. Dac590 inhibits xenograft tumor growth and prolongs survival in acute myeloid leukemia mouse models with no observed toxicity. Dac590 can be used for the research of AML.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 96.15%
- CAS No.: 3084407-00-8
- Formule: C19H16ClFN2O4
- Masse moléculaire:390.79
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
HY-L061
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Anti-Blood Cancer Compound Library
HY-L079
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Anti-Hematopathy Compound Library
HY-L171
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
Activité biologique
Dac590 (20 μM) completely inhibits recombinant FTO demethylase activity at a concentration of 20 μM[1].
Dac590 (0-1 μM; 0-48 h) increases global m6A RNA methylation levels in a time- and dose-dependent manner in NB4 and MOLM-13 AML cells[1].
Dac590 (0.2-5 μM) modulates FTO downstream oncogenic pathways in NB4 and MOLM-13 AML cells, upregulating ASB2 and RARA expression while downregulating c-MYC and CEBPA[1].
Dac590 (0.5-1 μM; 48 h) induces myeloid differentiation in NB4 and MOLM-13 AML cells, as measured by increased CD11b expression[1].
Dac590 (1 μM; 48 h) induces G1-phase cell cycle arrest in NB4 and MOLM-13 AML cells[1].
Dac590 (0.2-2 μM; 48 h) induces dose-dependent apoptosis in NB4 and MOLM-13 AML cells[1].
Dac590 (0-1 μM; 48 h) reduces DNMT1 protein levels in NB4 and MOLM-13 AML cells[1].
Dac590 (72 h) inhibits the proliferation of NB4, MOLM-13, NOMO-1, MV-4-11, HEL, U937, K562, and MONO-MAC-6 cells with IC50s of 327.7, 358.3, 1405, 506.1, 507.6, 845.1, 1191, 596.5 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NB4 and MOLM-13 AML cells
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Concentration:0.5, 1 μM
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Incubation Time:48 h
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Result:Increased CD11b mean fluorescence intensity in both cell lines, indicating induction of myeloid differentiation.
Induced myeloid differentiation in NB4 and MOLM-13 AML cells.
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Cell Line:NB4 and MOLM-13 AML cells
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Concentration:1 μM
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Incubation Time:48 h
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Result:Caused G1-phase cell cycle arrest in both cell lines, increasing the percentage of cells in G0/G1 phase and decreasing the percentage in S and G2/M phases.
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Cell Line:NB4 and MOLM-13 AML cells
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Concentration:0.2, 0.5, 1, 2 μM
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Incubation Time:48 h
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Result:Induced apoptosis in a dose-dependent manner in both cell lines, increasing the percentage of Annexin V+/PI- and Annexin V+/PI+ cells.
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Cell Line:NB4 and MOLM-13 AML cells
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Concentration:0, 0.2, 0.5, 1 μM
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Incubation Time:48 h
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Result:Reduced DNMT1 protein levels in both cell lines, with a particularly strong effect in MOLM-13 cells.
Increased ASB2 and RARA levels.
Downregulated c-MYC and CEBPA levels.
Dac590 (40 mg/kg; i.g.; daily; 28 days) shows no observable toxicity in female BALB/c mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NSG mice (6 weeks old) intravenously injected wiht MOLM-13 cells, followed 20 mg/kg Busulfan (HY-B0245) pretreatment 24 hours prior[1]
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Dosage:25, 40 mg/kg
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Administration:i.g.; daily; 20 days
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Result:Significantly prolonged survival compared to vehicle control.
Showed no adverse effects on body weight.
Enhanced survival benefit when combined with Decitabine (DAC) (HY-A0004) .
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Animal Model:Female BALB/c mice (6-8 weeks old)[1]
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Dosage:40 mg/kg
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Administration:i.g.; daily; 28 days
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Result:Showed no significant body weight changes compared to vehicle controls.
Detected no pathological changes in heart, liver, spleen, lungs, or kidneys via H&E staining.
Chemical Information
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CAS No. 3084407-00-8
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Appearance Solid
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Masse moléculaire 390.79
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Formule C19H16ClFN2O4
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Color Yellow to brown
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SMILES
OC(C1=CC(OC)=CC=C1NC2=C(C=C(C=C2Cl)C3=C(ON=C3C)C)F)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 12.5 mg/mL (31.99 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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)
Pureté et documentation
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Fiche technique (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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. 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 | 2.5589 mL | 12.7946 mL | 25.5892 mL | 63.9730 mL |
| 5 mM | 0.5118 mL | 2.5589 mL | 5.1178 mL | 12.7946 mL | |
| 10 mM | 0.2559 mL | 1.2795 mL | 2.5589 mL | 6.3973 mL | |
| 15 mM | 0.1706 mL | 0.8530 mL | 1.7059 mL | 4.2649 mL | |
| 20 mM | 0.1279 mL | 0.6397 mL | 1.2795 mL | 3.1986 mL | |
| 25 mM | 0.1024 mL | 0.5118 mL | 1.0236 mL | 2.5589 mL | |
| 30 mM | 0.0853 mL | 0.4265 mL | 0.8530 mL | 2.1324 mL |
Dac590 Related Classifications
HY-174979 Related Classifications
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