[CAS NO. 537034-17-6] BML-210
PRODUCTS SPECIFICATIONS [537034-17-6]
DESCRIPTION [537034-17-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 339.43 |
| Molecular Formula | C20H25N3O2 |
| SMILES | O=C(NC1=CC=CC=C1N)CCCCCCC(NC2=CC=CC=C2)=O |
1 Publications Citing Use of MCE
Summary
BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC 50 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 [1] [2] [3] .
IC50 & Target
|
HDAC4:MEF2 |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [2]
| Cell Line: | NB4 cells |
| Concentration: | 10, 20 μM |
| Incubation Time: | 24, 48 hours |
| Result: | Inhibited cell proliferation and growth inhibition of NB4 cells in a dose- and time-dependent manner. |
Cell Cycle Analysis [2]
| Cell Line: | NB4 cells |
| Concentration: | 10, 20 μM |
| Incubation Time: | 24, 48 hours |
| 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. |
Cell Cytotoxicity Assay [2]
| Cell Line: | NB4 cells |
| Concentration: | 10, 20 μM |
| Incubation Time: | 24, 48 hours |
| Result: | Caused cytotoxic effects on NB4 cells in a dose- and time-dependent manner. |
Apoptosis Analysis [2]
| Cell Line: | NB4 cells |
| Concentration: | 10, 20 μM |
| Incubation Time: | 24, 48 hours |
| Result: | At a dose of 10 μM induced apoptotic cell death. |
Western Blot Analysis [2]
| Cell Line: | NB4 cells |
| Concentration: | 10, 20 μM |
| Incubation Time: | 24, 48 hours |
| 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
BML-210 (20 mg/kg; IP; three times per week for two weeks) notably suppresses the tumour growth and weight. BML-210 has no effect on tumour growth and weight in the immune-deficient nude (Nu/J) mice
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female C57BL/6 mice with mouse breast cancer EO771 cells [3] |
| Dosage: | 20 mg/kg |
| Administration: | IP; three times per week for two weeks |
| Result: | Notably suppressed the tumour growth and weight. |
Appearance
Solid
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
DMSO : ≥ 30 mg/mL ( 88.38 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL |
| 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL |
| 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
References
- [1] Nimanthi Jayathilaka, et al. Inhibition of the function of class IIa HDACs by blocking their interaction with MEF2. Nucleic Acids Res. 2012 Jul; 40(12): 5378–5388.
- [2] Veronika Borutinskaite, et al. The Histone Deacetylase Inhibitor BML-210 Influences Gene and Protein Expression in Human Promyelocytic Leukemia NB4 Cells via Epigenetic Reprogramming. Int J Mol Sci. 2015 Aug; 16(8): 18252–18269.
- [3] Zhuolong Zhou, et al. An organoid-based screen for epigenetic inhibitors that stimulate antigen presentation and potentiate T-cell-mediated cytotoxicity. Nat Biomed Eng. 2021 Nov;5(11):1320-1335.
Synonyms