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| 25mg |
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Purity: ≥98%
BML-210 (also known as BML210; CAY-10433) is novel and potent HDAC inhibitor (IC50 value: 5 μM) with anticancer activity. BML-210 induces growth inhibition and apoptosis and regulates HDAC and DAPC complex expression levels in cervical cancer cells. BML-210 can inhibit cell growth and induce apoptosis in cervical cancer cells, what correlates with down-regulation of HDAC class I and II and changes in the DAPC expression levels. Cell cycle analysis indicated that HeLa cell treatment with 20 and 30 μM concentration of BML-210 increased the proportion of cells in G0/G1 phase, and caused accumulation in subG1, indicating that the cells are undergoing apoptosis.
| Targets |
HDAC4; HDAC4-VP16-driven reporter
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|---|---|
| ln Vitro |
NB4 cells are inhibited in their growth and proliferation by BML-210 (10, 20 μM; 24, 48 hours) [2]. The amount of S phase NB4 cells was reduced by BML-210 (10, 20 μM; 24, 48 hours), and at 20 μM, G0 BML-210 (10, 20 μM; 24, 48 hours) had a cytotoxic effect on NB4 cells. A dose of 10 μM is sufficient for BML-210 to cause cell death [2]. In NBT4 cells, BML-210 (10, 20 μM; 24, 48 hours) suppresses HDAC expression and activity [2]. HDAC4-VP16 expression is not downregulated by BML-210[1].Cell lines. NB4 cells Concentration: 10, 20 μM Incubation period: 24, 48 hours Outcomes: Reduced NB4 cell growth and proliferation in a time- and dose-dependent manner.
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| ln Vivo |
BML-210 (20 mg/kg; intraperitoneal injection; three times weekly for two weeks) markedly reduced the amount of body weight and tumor growth. In immunodeficient nude mice, BML-210 has no influence on tumor growth or body weight (Nu/J).
In this study, researchers show that the epigenetic inhibitors GSK-LSD1, CUDC-101 and BML-210, identified by the screen, display antitumour activities in orthotopic mammary tumours in mice, that they upregulate antigen presentation mediated by the major histocompatibility complex class I on breast tumour cells and that treatment with BML-210 substantially sensitized breast tumours to the inhibitor of the checkpoint programmed death-1. Standardized measurements of tumour-cell killing activity facilitated by tumour-organoid-T-cell screens may help with the identification of candidate immunotherapeutics for a range of cancers[3]. |
| Enzyme Assay |
HDAC Activity Analysis[2]
Proteins were isolated using ProteoJET™ Mammalian Cell Lysis Reagent (Fermentas, Vilnius, Lithuania) according to the manufacturer's instructions. HDAC activity analysis was determined using EpiQuik™ HDAC Activity/Inhibition Assay Kit according to the manufacturer’s instructions. Absorbance was measured using Tecan-Control, Infinite 200 microplate reader at 450 nm. Activity (ng/h/mL) was calculated using formula.[2] Drug treatment and luciferase assay[1] For the two-hybrid assay, cells were treated with 10 µM drug overnight unless indicated otherwise. The amount of DMSO was kept below 0.2% V/V. A luciferase assay was performed according to the manufacturer’s protocol. The luciferase response was normalized against the Renilla Luciferase as an internal control. The data are presented as a mean ± SD (n = 2) of normalized HDAC4:MEF2 luciferase response against the normalized response values for GAL4-VP16 for each condition to correct for non-specific inhibition of the luciferase signal. |
| Cell Assay |
Cell proliferation assay[2]
Cell Types: NB4 cells Tested Concentrations: 10, 20 μM Incubation Duration: 24, 48 hrs (hours) Experimental Results: Inhibited cell proliferation and inhibited the growth of NB4 cells in a dose- and time-dependent manner. Cell cycle analysis [2] Cell Types: NB4 cells Tested Concentrations: 10, 20 μM Incubation Duration: 24, 48 hrs (hours) Experimental Results: The proportion of S phase of NB4 cells diminished and the proportion of G0/G1 phase increased. 10 μM increased the G0/G1 phase by up to 70% at 24 and 48 hrs (hours). Cytotoxicity assay [2] Cell Types: NB4 cells Tested Concentrations: 10, 20 μM Incubation Duration: 24, 48 hrs (hours) Experimental Results: Cytotoxic effects on NB4 cells were dose- and time-dependent. Apoptosis analysis [2] Cell Types: NB4 Cell Tested Concentrations: 10, 20 μM Incubation Duration: 24, 48 hrs (hours) Experimental Results: 10 μM dose induced apoptosis. Western Blot Analysis[2] Cell Types: NB4 Cell Tested Concentrations: 10, 20 μM Incubation Duration: 24, 48 hrs (hours) Experimental Results: After 48 hrs (hours) of treatment with 10 μM dose, HDAC1 gene expression was inhibited by up to 36% Aft |
| Animal Protocol |
Animal/Disease Models: Female C57BL/6 mice, mouse breast cancer EO771 cells [3]
Doses: 20 mg/kg Route of Administration: IP ;[3]. Three times a week for two weeks. Experimental Results: Significant inhibition of tumor growth and weight. |
| References |
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| Additional Infomation |
BML-210 is a dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and 1,2-diaminobenzene. It has a role as an EC 3.5.1.98 (histone deacetylase) inhibitor and an antineoplastic agent. It is functionally related to a suberic acid.
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| Molecular Formula |
C20H25N3O2
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|---|---|
| Molecular Weight |
339.4314
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| Exact Mass |
339.194
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| Elemental Analysis |
C, 70.77; H, 7.42; N, 12.38; O, 9.43
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| CAS # |
537034-17-6
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| PubChem CID |
9543540
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
632.5±40.0 °C at 760 mmHg
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| Flash Point |
336.3±27.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.633
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| LogP |
2.58
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
25
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| Complexity |
408
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C(N([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)N([H])C1=C([H])C([H])=C([H])C([H])=C1N([H])[H]
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| InChi Key |
RFLHBLWLFUFFDZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25N3O2/c21-17-12-8-9-13-18(17)23-20(25)15-7-2-1-6-14-19(24)22-16-10-4-3-5-11-16/h3-5,8-13H,1-2,6-7,14-15,21H2,(H,22,24)(H,23,25)
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| Chemical Name |
N-(2-aminophenyl)-N'-phenyl-octanediamide
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| Synonyms |
BML-210; CAY10433; BML 210; CAY-10433; BML210; BML-210; 537034-17-6; N1-(2-aminophenyl)-N8-phenyloctanediamide; BML-210(CAY10433); N-(2-aminophenyl)-N'-phenyl-octanediamide; CHEBI:61077; Octanediamide, N-(2-aminophenyl)-N'-phenyl-; CAY 10433.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 30 mg/mL (~88.38 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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