DDO-2728
Based on 3 publication(s) in Google Scholar
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N6 methyladenosine (m6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4 11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research.
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- Pureza: 98.64%
- No. CAS: 3029515-97-4
- Fòrmula: C28H17F3N4O7
- Peso molecular:578.45
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) DDO-2728
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Actividad biológica
AlkB homologue 5 (ALKBH5) IC50: 2.97 μM[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
97.4 μM
Compound: 19; DDO-2728
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Antiproliferative activity against HEK293 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer Luminescence assay
Antiproliferative activity against HEK293 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer Luminescence assay
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[PMID: 37983486] |
| HUVEC | IC50 |
165.1 μM
Compound: 19; DDO-2728
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Antiproliferative activity against HUVEC cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer Luminescence assay
Antiproliferative activity against HUVEC cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer Luminescence assay
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[PMID: 37983486] |
| MOLM-13 | IC50 |
0.45 μM
Compound: 19; DDO-2728
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Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer Luminescence assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer Luminescence assay
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[PMID: 37983486] |
| MV4-11 | IC50 |
1.2 μM
Compound: 19; DDO-2728
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer Luminescence assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer Luminescence assay
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[PMID: 37983486] |
DDO-2728 (0-40 μM, 48 h) increases m6A methylation levels in the MOLM-13, HEK293and MV4 11 cells over a concentration gradient[1].
DDO-2728 (0.01-100 μM, 72 h) inhibits the proliferation of MOLM-13 and MV4 11 cells with IC50s of 0.45 and 1.2 μM respectively, and showes a relatively weak toxicity in HEK293 and HUVECs[1].
DDO-2728 (20 μM, 48 h) significantly arrests the cell cycle of MOLM-13 and MV4 11 cells at the G1/M phase[1].
DDO-2728 (5, 10 μM, 48 h) concentration-dependently induces cell apoptosis of MV4 11 and MOLM-13 cells[1].
DDO-2728 (20 μM, 24 h) decreases the half-lives of TACC3 mRNA in MOLM-13 and MV4 11 cells[1].
DDO-2728 (0-10 μM, 48 h) significantly reduces the abundance of TACC3 and c-Myc in MOLM-13 and MV4 11 cells at both mRNA and protein levels[1].
Metabolic Stability in Rat and Human Plasma and Liver Microsomes[1]
| Species | Plasma T1/2 (min) | Microsome T1/2 (min) | Microsome CL (μL/min/mg) |
| Human | 624 | 430 | 3.2 |
| Rat | 251 | 13.8 | 100.4 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13, MV4-11, HEK293, HUVEC
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Concentration:0.01-100 μM
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Incubation Time:72 h
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Result:Inhibited the proliferation of MOLM-13 and MV4−11 cells with IC50s of 0.45 and 1.2 μM respectively, didn't show visual cytotoxicity in HEK293 and HUVECs under 1 μM.
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Cell Line:MOLM-13, MV4-11
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Concentration:0, 5, 10 μM
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Incubation Time:48 h
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Result:Induced cell apoptosis of MV4−11 and MOLM-13 cells concentration-dependently, apoptosis rate for MV4−11 increased from 7.17% to 55.4%, apoptosis rate for MOLM-13 increased from 6.49% to 31.5%.
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Cell Line:MOLM-13, MV4-11
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Concentration:20 μM
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Incubation Time:48 h
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Result:Arrested the cell cycle of MOLM-13 and MV4−11 cells at the G1/M phase as no G2/M phase cells exist.
Pharmacokinetic Parameters of DDO-2728 in Rats[1]
| Parameter | Rat (i.v., 2mg/kg) | Rat (i.p., 10mg/kg) |
| T1/2 (min) | 36.7 ± 3.2 | 148.3 ± 4.6 |
| Cmax (ng/mL) | 13388.3 ± 784.5 | 2337.5 ± 295.7 |
| Tmax (min) | 30 | |
| AUC0-∞ (min·μg/mL) | 404.3 ± 58.6 | 349.1 ± 26.1 |
| Vz_F_obs (mL/kg) | 263.6 ± 17.5 | 6177.6 ± 650.2 |
| Cl_F_obs (mL/min/kg) | 5.0 ± 0.5 | 28.8 ± 2.2 |
| MRT (min) | 77.8 ± 15.5 | 168.2 ± 1.2 |
| F (%) | 17.3 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4−11 xenograft nude mice [1]
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Dosage:10, 20, and 40 mg/kg
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Administration:Intraperitoneal injection (i.p.) daily for 14 d
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Result:Inhibited tumor growth significantly even at a concentration of 10 mg/kg. No significant change in the weight of the mice and the main organs during the treatment, the organ weight of test group mice was the same as vehicle group, no obvious injury damage was observed in the HE staining images of organ tissues.
Chemical Information
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No. CAS 3029515-97-4
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Appearance Solid
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Peso molecular 578.45
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Fòrmula C28H17F3N4O7
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Color Off-white to light yellow
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SMILES
OC1=C(C(O)=C(C=C1)[N+]([O-])=O)C(C(C=N2)=CN3C2=CC(C4=CC=C(C=C4)C(OCC5=CC=C(C=C5)C(F)(F)F)=O)=N3)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
ALKBH5 aggravates scarring after glaucoma surgery via m6A-YTHDF2-mediated NLRP3 mRNA stabilization. [Abstract]2026 May 31. PMID: 42218253 -
J Transl Med
Retinal ALKBH5 inhibition induces myopia protection through selective regulation of ERK1/2 signaling. [Abstract]2025 Nov 12;23(1):1271. PMID: 41225555 -
Biochem Pharmacol
ALKBH5 reverses romidepsin-mediated anti-multiple myeloma activity via regulation of m6A modification of FOXM1. [Abstract]2025 May 24:239:116998. PMID: 40419197
Solvente y solubilidad
DMSO : 125 mg/mL (216.09 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. 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)
Pureza y Documentación
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Ficha de datos (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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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. 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 | 1.7288 mL | 8.6438 mL | 17.2876 mL | 43.2189 mL |
| 5 mM | 0.3458 mL | 1.7288 mL | 3.4575 mL | 8.6438 mL | |
| 10 mM | 0.1729 mL | 0.8644 mL | 1.7288 mL | 4.3219 mL | |
| 15 mM | 0.1153 mL | 0.5763 mL | 1.1525 mL | 2.8813 mL | |
| 20 mM | 0.0864 mL | 0.4322 mL | 0.8644 mL | 2.1609 mL | |
| 25 mM | 0.0692 mL | 0.3458 mL | 0.6915 mL | 1.7288 mL | |
| 30 mM | 0.0576 mL | 0.2881 mL | 0.5763 mL | 1.4406 mL | |
| 40 mM | 0.0432 mL | 0.2161 mL | 0.4322 mL | 1.0805 mL | |
| 50 mM | 0.0346 mL | 0.1729 mL | 0.3458 mL | 0.8644 mL | |
| 60 mM | 0.0288 mL | 0.1441 mL | 0.2881 mL | 0.7203 mL | |
| 80 mM | 0.0216 mL | 0.1080 mL | 0.2161 mL | 0.5402 mL | |
| 100 mM | 0.0173 mL | 0.0864 mL | 0.1729 mL | 0.4322 mL |
DDO-2728 Related Classifications
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