| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 25mg | |||
| Other Sizes |
| Targets |
BLL5 Maleate primarily targets protein arginine methyltransferase 5 (PRMT5), a type II arginine methyltransferase that catalyzes symmetric dimethylation of arginine residues on histone and non-histone proteins. PRMT5 is frequently overexpressed in various cancers and plays a critical role in regulating gene expression, cell proliferation, and survival. By selectively inhibiting PRMT5, BLL5 Maleate disrupts its methyltransferase activity, leading to changes in gene expression that specifically block EBV-driven transformation of B lymphocytes.
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|---|---|
| ln Vitro |
In vitro, BLL5 Maleate acts as a potent and selective inhibitor of PRMT5 enzymatic activity. It effectively blocks EBV-driven B lymphocyte transformation and survival in cell-based assays, while leaving normal B cells unaffected. This selectivity is a key feature of its activity, as it demonstrates that PRMT5 inhibition specifically targets the transformed state of EBV-infected B cells without affecting normal B-cell function. The compound's potency and selectivity make it a valuable tool for studying PRMT5 biology.
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| ln Vivo |
Specific in vivo activity data for BLL5 Maleate is not detailed in the provided search results. As a PRMT5 inhibitor with selective activity against EBV-driven B-cell transformation in vitro, it is being investigated for its potential in treating EBV-associated malignancies. Further studies are needed to characterize its in vivo efficacy, pharmacokinetics, and safety profile in animal models of EBV-driven lymphoproliferative disorders.
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| Enzyme Assay |
The in vitro activity of BLL5 Maleate as a PRMT5 inhibitor is assessed using cell-free enzymatic activity assays. Recombinant PRMT5 enzyme is incubated with a peptide or protein substrate and S-adenosylmethionine (SAM) as the methyl donor in the presence of varying concentrations of BLL5 Maleate. The incorporation of methyl groups into the substrate is measured, typically using radioactive (e.g., ³H-SAM) or fluorescence-based detection methods. The IC50 is determined from dose-response curves.
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| Cell Assay |
For cellular assays, B lymphocytes (both EBV-transformed and normal) are cultured in appropriate media. Cells are treated with various concentrations of BLL5 Maleate (typically 0.1-100 µM) for defined periods (24-72 hours). Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays. The effects on EBV-driven transformation are evaluated by measuring the expression of EBV-associated genes and markers of B-cell activation. Cell cycle analysis and apoptosis assays are performed to characterize the mechanism of cell death.
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| Animal Protocol |
In vivo, BLL5 Maleate would be administered to animal models of EBV-driven lymphoproliferative disorders, such as immunocompromised mice engrafted with EBV-transformed human B cells. The compound is formulated in a suitable vehicle and administered at various doses via intraperitoneal or oral routes. Tumor growth and EBV-driven B-cell expansion are monitored. At the end of the study, tissues are analyzed for PRMT5 inhibition, B-cell transformation markers, and apoptosis.
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| ADME/Pharmacokinetics |
BLL5 Maleate has a molecular weight of 431.49 g/mol (maleate salt) and a molecular formula of C25H25N3O4. The free base has a molecular weight of 315.41 g/mol and a formula of C21H21N3. It is soluble in DMSO. The compound should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 1 year. Specific pharmacokinetic parameters are not detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BLL5 Maleate is not available in the provided search results. The compound's selective activity against EBV-transformed B cells while leaving normal B cells unaffected suggests a favorable safety profile. However, as a PRMT5 inhibitor, it may affect normal cellular processes in other cell types. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
BLL5 Maleate is a first-in-class selective PRMT5 inhibitor that blocks EBV-driven B lymphocyte transformation. It is a valuable research tool for studying the role of PRMT5 in viral oncogenesis and B-cell biology. EBV is associated with various malignancies, including Burkitt's lymphoma, Hodgkin's lymphoma, and nasopharyngeal carcinoma. BLL5 Maleate offers a unique opportunity to explore PRMT5 as a therapeutic target in these EBV-associated cancers. The compound is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C21H21N3
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|---|---|
| Molecular Weight |
315.41
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| Exact Mass |
315.173
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| CAS # |
880813-30-9
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| PubChem CID |
4722575
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| Appearance |
White to off-white solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
399
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(CC)C2=CC=CC=C2C2C=C(CN([H])CC3=CC=CN=C3)C=CC=21
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| InChi Key |
GAVUWQFIRGBDHN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21N3/c1-2-24-20-8-4-3-7-18(20)19-12-16(9-10-21(19)24)13-23-15-17-6-5-11-22-14-17/h3-12,14,23H,2,13,15H2,1H3
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| Chemical Name |
1-(9-ethylcarbazol-3-yl)-N-(pyridin-3-ylmethyl)methanamine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1705 mL | 15.8524 mL | 31.7048 mL | |
| 5 mM | 0.6341 mL | 3.1705 mL | 6.3410 mL | |
| 10 mM | 0.3170 mL | 1.5852 mL | 3.1705 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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