BML-210
Based on 2 publication(s) in Google Scholar
BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice.
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- Pureté : 98.04%
- CAS No.: 537034-17-6
- Formule: C20H25N3O2
- Masse moléculaire:339.43
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BML-210
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Activité biologique
Description
IC50 & Target
[1]|
HDAC4:MEF2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
87 μM
Compound: 4c, BML-210
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Inhibition of HDAC in human HeLa cell extract by fluorescence plate reader assay
Inhibition of HDAC in human HeLa cell extract by fluorescence plate reader assay
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[PMID: 16921367] |
| MV4-11 | IC50 |
7244 nM
Compound: 4
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Antiproliferative activity against human MV4-11 cells
Antiproliferative activity against human MV4-11 cells
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[PMID: 35580726] |
In Vitro
BML-210 (10, 20 μM; 24, 48 hours) inhibits cell proliferation and growth inhibition of NB4 cells[2].
BML-210 (10, 20 μM; 24, 48 hours) causes a decrease in the proportion of NB4 cells in the S phase and an increase in the G0/G1 phase[2].
BML-210 (10, 20 μM; 24, 48 hours) causes cytotoxic effects on NB4 cells at 20 μM. BML-210 at a dose of 10 μM induces apoptotic cell death[2].
BML-210 (10, 20 μM; 24, 48 hours) inhibits HDAC Expression and Activity in NB4 Cells[2].
BML-210 (1.0 μM; for 48 h) causes higher expression levels differential expressed genes (DEGs) in mouse EO771 cells[3].
BML-210 does not reduce the expression of HDAC4-VP16[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:NB4 cells
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Concentration:10, 20 μM
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Incubation Time:24, 48 hours
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Result:Inhibited cell proliferation and growth inhibition of NB4 cells in a dose- and time-dependent manner.
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Cell Line:NB4 cells
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Concentration:10, 20 μM
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Incubation Time:24, 48 hours
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Result:Caused a decrease in the proportion of NB4 cells in the S phase and an increase in the G0/G1 phase.
Caused an increase in the G0/G1 phase up to 70% at 24 and 48 h with 10 μM.
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Cell Line:NB4 cells
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Concentration:10, 20 μM
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Incubation Time:24, 48 hours
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Result:Caused cytotoxic effects on NB4 cells in a dose- and time-dependent manner.
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Cell Line:NB4 cells
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Concentration:10, 20 μM
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Incubation Time:24, 48 hours
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Result:At a dose of 10 μM induced apoptotic cell death.
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Cell Line:NB4 cells
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Concentration:10, 20 μM
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Incubation Time:24, 48 hours
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Result:At 10 μM dose inhibited HDAC1 gene expression up to 36% after 48 h of treatment Inhibited HDAC expression up to 74% at 8 h point at 20 μM.
Had very low effect on HDAC 2 and HDAC 3 expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6 mice with mouse breast cancer EO771 cells[3]
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Dosage:20 mg/kg
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Administration:IP; three times per week for two weeks
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Result:Notably suppressed the tumour growth and weight.
Chemical Information
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CAS No. 537034-17-6
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Appearance Solid
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Masse moléculaire 339.43
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Formule C20H25N3O2
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Color White to off-white
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SMILES
O=C(NC1=CC=CC=C1N)CCCCCCC(NC2=CC=CC=C2)=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 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Transl Stroke Res
HDAC9 Deficiency Upregulates cGMP-dependent Kinase II to Mitigate Neuronal Apoptosis in Ischemic Stroke. [Abstract]2025 Jun;16(3):868-881. PMID: 38940872
Solvant et solubilité
In Vitro:
DMSO : ≥ 30 mg/mL (88.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
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.
Protocole
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (760 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL | 73.6529 mL |
| 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL | 14.7306 mL | |
| 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 mL | 7.3653 mL | |
| 15 mM | 0.1964 mL | 0.9820 mL | 1.9641 mL | 4.9102 mL | |
| 20 mM | 0.1473 mL | 0.7365 mL | 1.4731 mL | 3.6826 mL | |
| 25 mM | 0.1178 mL | 0.5892 mL | 1.1784 mL | 2.9461 mL | |
| 30 mM | 0.0982 mL | 0.4910 mL | 0.9820 mL | 2.4551 mL | |
| 40 mM | 0.0737 mL | 0.3683 mL | 0.7365 mL | 1.8413 mL | |
| 50 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4731 mL | |
| 60 mM | 0.0491 mL | 0.2455 mL | 0.4910 mL | 1.2275 mL | |
| 80 mM | 0.0368 mL | 0.1841 mL | 0.3683 mL | 0.9207 mL |
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