2. Metabolic Enzyme/Protease Apoptosis
  3. Fat Mass and Obesity-associated Protein (FTO) Apoptosis
  4. Dac590

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.

For research use only. We do not sell to patients.

Dac590

Dac590 Chemical Structure

CAS No. : 3084407-00-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Dac590 Related Antibodies

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Description

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[1].

In Vitro

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.

Dac590 Related Antibodies

Cell Differentiation Assay[1]

Cell Line: NB4 and MOLM-13 AML cells
Concentration: 0.5, 1 μM
Incubation Time: 48 h
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.

Cell Cycle Analysis[1]

Cell Line: NB4 and MOLM-13 AML cells
Concentration: 1 μM
Incubation Time: 48 h
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.

Apoptosis Analysis[1]

Cell Line: NB4 and MOLM-13 AML cells
Concentration: 0.2, 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner in both cell lines, increasing the percentage of Annexin V+/PI- and Annexin V+/PI+ cells.

Western Blot Analysis[1]

Cell Line: NB4 and MOLM-13 AML cells
Concentration: 0, 0.2, 0.5, 1 μM
Incubation Time: 48 h
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.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t Bioavailability
Mice[1] 1 mg/kg i.v. 3.77 h 0.08 h 4340 ng/mL 6079 ng·h/mL /
Mice[1] 2 mg/kg i.g. 5.81 h 0.08 h 3970 ng/mL 7276 ng·h/mL 61.1 %
In Vivo

Dac590 (25 and 40 mg/kg; i.g.; daily; 20 days) significantly prolongs survival and inhibits tumor growth in mouse MOLM-13 AML models[1].
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.

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]
Dosage: 25, 40 mg/kg
Administration: i.g.; daily; 20 days
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) .
Animal Model: Female BALB/c mice (6-8 weeks old)[1]
Dosage: 40 mg/kg
Administration: i.g.; daily; 28 days
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.
Molecular Weight

390.79

Formula

C19H16ClFN2O4
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

OC(C1=CC(OC)=CC=C1NC2=C(C=C(C=C2Cl)C3=C(ON=C3C)C)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5589 mL 12.7946 mL 25.5892 mL
5 mM 0.5118 mL 2.5589 mL 5.1178 mL
View the 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.

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Purity & Documentation
References

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
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Dac590 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dac5903084407-00-8Dac 590Dac-590Fat Mass and Obesity-associated Protein (FTO)ApoptosisALKBH3xenograft tumordecitabineNB4ALKBH5N6-methyladenosineNSG micefat mass and obesity-associated proteinMOLM-13acute myeloid leukemia cellsInhibitorinhibitorinhibit

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