ALKBH5-IN-5
Based on 1 publication(s) in Google Scholar
ALKBH5-IN-5 is a highly selective ALKBH5 (IC50 = 0.62 μM, Kd = 804 nM). ALKBH5-IN-5 disrupts ALKBH5 binding to m6A-RNA and 6mA-DNA substrates. ALKBH5-IN-5 promotes differentiation, induces apoptosis, cause G2-M phase arrest and exerts strong antiproliferative effects in cancer cells. ALKBH5-IN-5 reduces TACC3 and MYC protein levels and increases cleaved caspase-3 levels. ALKBH5-IN-5 exerts antitumor activity in tumor xenograft mice models. ALKBH5-IN-5 can be used for the research of acute myeloid leukemia.
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- Pureté : 99.66%
- CAS No.: 140481-05-6
- Formule: C13H13NO3
- Masse moléculaire:231.25
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
Publications Citing Use of MedChemExpress (MCE) ALKBH5-IN-5
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Activité biologique
Description
IC50 & Target
[1]|
ALKBH5 0.62 μM (IC50) |
ALKBH5 804 nM (Kd) |
Caspase 3 |
In Vitro
ALKBH5-IN-5 (Compound 18l) selectively inhibits ALKBH5 (IC50 = 0.62 ± 0.12 μM; Kd = 804 ± 117 nM) and shows minimal FTO inhibition[1].
ALKBH5-IN-5 disrupts ALKBH5 binding to m6A-RNA and 6mA-DNA substrates[1].
ALKBH5-IN-5 (20-80 μM) covalently modifies ALKBH5 at C200, C100, and C267, with IC50 of 0.7, 30.34 and 1.15 μM[1].
ALKBH5-IN-5 (72 h) inhibits proliferation of LM-13, MV4-11, NOMO-1, and NB4 cells (IC50 = 1.92, 1.50, 2.99 and 0.63 μM) and has low cytotoxicity in HEK293 cells[1].
ALKBH5-IN-5 (25-500 nM) suppresses NB4 cell colony formation, with near elimination at 500 nM[1].
ALKBH5-IN-5 (2-15 μM; 24-72 h) induces apoptosis, promotes differentiation, and arrests the cell cycle at G2-M phase in NB4 cells[1].
ALKBH5-IN-5 (5-10 μM; 48 h) reduces TACC3 and MYC protein levels and increases cleaved caspase-3 levels in NB4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NB4 cells
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Concentration:5, 10, 15 μM
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Incubation Time:48 h
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Result:Induced apoptosis dose-dependently (highest at 15 μM).
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Cell Line:NB4 cells
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Concentration:2, 5 μM
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Incubation Time:24 h
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Result:Caused cell cycle arrest at G2-M phase dose-dependently.
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Cell Line:NB4 cells
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Concentration:5, 10 μM
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Incubation Time:48 h
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Result:Decreased TACC3 and MYC protein levels and increased cleaved caspase-3 levels dose-dependently.
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 with acute myeloid leukemia (female)[1]
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Dosage:1 mg/kg; 2.5 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Inhibited tumor growth by 66.3% at 1 mg/kg and 76.8% at 2.5 mg/kg.
Observed no significant body weight loss or pathological changes in major organs.
Chemical Information
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CAS No. 140481-05-6
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Appearance Solid
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Masse moléculaire 231.25
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Formule C13H13NO3
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Color Off-white to light yellow
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SMILES
O=C(C=C1)N(CCC2=CC=CC=C2OC)C1=O
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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.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Mol Life Sci
ALKBH5 demethylation modification of SE-lncRNA ZMIZ1-AS1 promotes FGFR1-mediated proliferation and invasive metastasis in osteosarcoma. [Abstract]2025 Nov 22. PMID: 41275058
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (432.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (21.62 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (283 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
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3243 mL | 21.6216 mL | 43.2432 mL | 108.1081 mL |
| 5 mM | 0.8649 mL | 4.3243 mL | 8.6486 mL | 21.6216 mL | |
| 10 mM | 0.4324 mL | 2.1622 mL | 4.3243 mL | 10.8108 mL | |
| 15 mM | 0.2883 mL | 1.4414 mL | 2.8829 mL | 7.2072 mL | |
| 20 mM | 0.2162 mL | 1.0811 mL | 2.1622 mL | 5.4054 mL | |
| 25 mM | 0.1730 mL | 0.8649 mL | 1.7297 mL | 4.3243 mL | |
| 30 mM | 0.1441 mL | 0.7207 mL | 1.4414 mL | 3.6036 mL | |
| 40 mM | 0.1081 mL | 0.5405 mL | 1.0811 mL | 2.7027 mL | |
| 50 mM | 0.0865 mL | 0.4324 mL | 0.8649 mL | 2.1622 mL | |
| 60 mM | 0.0721 mL | 0.3604 mL | 0.7207 mL | 1.8018 mL | |
| 80 mM | 0.0541 mL | 0.2703 mL | 0.5405 mL | 1.3514 mL | |
| 100 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0811 mL |
ALKBH5-IN-5 Related Classifications
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