| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
BML-266 targets multiple molecular entities. Its primary target is sirtuin 2 (SIRT2), an NAD+-dependent class III histone deacetylase that is present in prokaryotes and all eukaryotes. SIRT2 plays a role in various cellular processes, including cell cycle regulation, genomic stability, and aging. BML-266 also inhibits CLK2, a protein kinase involved in alternative splicing modulation. Additionally, it has antiviral activity against SARS-CoV-2 Nsp-16 and predicted Marburg virus methyltransferase binding. This multi-target profile distinguishes it from more target-specific SIRT2 inhibitors.
|
|---|---|
| ln Vitro |
Prostate cancer cell lines show growth inhibition from JFD00244 (50 nM–50 μM; 48 h) with IC50s of 200 nM (22Rv1) and 1 μM (DU145) [3].
In vitro, BML-266 is a SIRT2 inhibitor with an IC50 of 56.7 µM. It induces granulocytic differentiation in the acute promyelocytic leukemia (APL) cell line NB4. As a patented senolytic agent, it selectively eliminates senescent cells and can be used in studies of the senescence-associated secretory phenotype (SASP). Its multi-target activity across SIRT2 inhibition, CLK2 inhibition, and antiviral effects makes it a unique chemical probe for studying diverse biological pathways. |
| ln Vivo |
In vivo, BML-266 has potential anticancer and anti-tumor effects based on its SIRT2 inhibition and senolytic activity. It has also demonstrated antiviral potential against SARS-CoV-2. However, specific in vivo data, such as efficacy in animal models of cancer or viral infection, are not detailed in the available literature. Its patented senolytic activity suggests it may have applications in clearing senescent cells in vivo, which could have implications for age-related diseases and cancer therapy.
|
| Enzyme Assay |
Non-cellular in vitro assays for BML-266 involve measuring its inhibition of SIRT2 deacetylase activity. A typical protocol uses purified recombinant human SIRT2 enzyme and a fluorogenic peptide substrate that is acetylated at a specific lysine residue. The enzyme is incubated with NAD+ and varying concentrations of BML-266 in a reaction buffer. After incubation, the deacetylated product is detected by the addition of a developer that produces a fluorescent signal. The IC50 is determined from the concentration-response curve. For CLK2 inhibition, a similar kinase assay with a peptide substrate and ATP is used.
|
| Cell Assay |
Cell Viability Assay[3]
Cell Types: 22Rv1 and DU145 Cell Tested Concentrations: 50 nM, 100 nM, 200 nM, 500 nM, 1 μM, 5 μM, 10 μM, 50 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of prostate cancer cell lines Dramatically. Cellular assays for BML-266 are performed using cell lines such as NB4 acute promyelocytic leukemia cells. Cells are treated with BML-266 at various concentrations for 24-72 hours. Granulocytic differentiation is assessed by measuring cell surface markers (e.g., CD11b) using flow cytometry. Senolytic activity can be assessed in mixed populations of senescent and non-senescent cells, where the selective elimination of senescent cells is measured by quantifying senescence-associated β-galactosidase activity or by flow cytometry. Cell viability is measured using an MTT assay. |
| Animal Protocol |
In vivo animal studies for BML-266 have not been extensively reported in the available literature. As a research compound with senolytic and antiviral potential, it could be tested in mouse models of aging, senescence-associated diseases, or viral infection. For example, in a model of pulmonary fibrosis, mice could be administered BML-266 to assess its ability to clear senescent cells and reduce fibrosis. However, specific published protocols are not available.
|
| ADME/Pharmacokinetics |
BML-266 has a molecular weight of 478.5 g/mol and a molecular formula of C30H26N2O4. It is a solid powder that is soluble in DMSO. For storage, it should be kept dry, dark, and at 0-4°C for short term (days to weeks) or at -20°C for long term (months to years). Detailed pharmacokinetic parameters such as half-life, bioavailability, and clearance have not been fully reported in the available literature.
|
| Toxicity/Toxicokinetics |
Detailed toxicological data for BML-266 have not been extensively reported. As a research chemical, it is not intended for human use and is strictly for preclinical research purposes. Standard safety precautions should be followed when handling BML-266, including the use of personal protective equipment. No specific toxicity data, such as LD50 values, are available in the provided literature.
|
| References |
|
| Additional Infomation |
1,4-Bis[2-(4-hydroxyphenyl)ethylamino]anthraphen-9,10-dione is an anthraquinone.
BML-266 (JFD00244) is a multi-target small molecule with SIRT2 inhibition (IC50 = 56.7 µM), CLK2 inhibition, and patented senolytic activity. It also has antiviral potential against SARS-CoV-2 and Marburg virus. The compound induces granulocytic differentiation in NB4 cells. Its unique combination of activities across oncology, senescence, and virology distinguishes it from more target-specific inhibitors. BML-266 is not a clinically approved drug and has not entered clinical trials. Its primary application is in academic and pharmaceutical research as a chemical probe for studying SIRT2, senescence, and viral targets. |
| Molecular Formula |
C30H26N2O4
|
|---|---|
| Molecular Weight |
478.54
|
| Exact Mass |
478.189
|
| CAS # |
96969-83-4
|
| PubChem CID |
2817242
|
| Appearance |
Dark purple to black solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
780.2±60.0 °C at 760 mmHg
|
| Flash Point |
425.7±32.9 °C
|
| Vapour Pressure |
0.0±2.8 mmHg at 25°C
|
| Index of Refraction |
1.733
|
| LogP |
4.45
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
36
|
| Complexity |
681
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
UUJHFIBEJJLZBF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C30H26N2O4/c33-21-9-5-19(6-10-21)15-17-31-25-13-14-26(32-18-16-20-7-11-22(34)12-8-20)28-27(25)29(35)23-3-1-2-4-24(23)30(28)36/h1-14,31-34H,15-18H2
|
| Chemical Name |
1,4-bis[2-(4-hydroxyphenyl)ethylamino]anthracene-9,10-dione
|
| Synonyms |
BML-266 BML266 BML 266
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~104.48 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0897 mL | 10.4484 mL | 20.8969 mL | |
| 5 mM | 0.4179 mL | 2.0897 mL | 4.1794 mL | |
| 10 mM | 0.2090 mL | 1.0448 mL | 2.0897 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
