| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
SW2_110A targets the CBX8 Chromodomain (ChD). It is a selective inhibitor with a Kd of 800 nM and shows 5-fold selectivity for CBX8 ChD over all other CBX paralogs. It binds CBX8 ChD with a Kd of 800 nM and shows minimal 5-fold selectivity over all other CBX paralogs in vitro. It shows no binding to CBX4/CBX6.
|
|---|---|
| ln Vitro |
SW2_110A selectively prevents CBX8 from binding to chromatin in cells and stops THP1 leukemia cells from proliferating due to the MLL-AF9 translocation with an IC50 of 26 microM. Treatment with SW2_110A significantly reduces the expression of MLL-AF9 target genes, such as HOXA9, in THP1 cells[1].
In vitro, SW2_110A selectively inhibits the association of CBX8 with chromatin in cells. It inhibits the proliferation of THP1 leukemia cells driven by the MLL-AF9 translocation with an IC50 of 26 µM. It has a Kd of 800 nM for CBX8 ChD and is 5-fold selective for CBX8 ChD over other CBX paralogs. |
| ln Vivo |
Specific in vivo activity data for SW2_110A are not detailed in the search results.
|
| Enzyme Assay |
Non-cellular binding assays for SW2_110A involve measuring its binding affinity to the CBX8 Chromodomain. These assays can be performed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) with purified CBX8 protein.
|
| Cell Assay |
In vitro cellular assays for SW2_110A are performed using THP1 leukemia cells driven by the MLL-AF9 translocation. Cells are treated with the compound, and its ability to inhibit the association of CBX8 with chromatin is assessed by chromatin immunoprecipitation (ChIP). Cell proliferation is measured to determine the IC50.
|
| Animal Protocol |
In vivo animal experiments for SW2_110A would typically be conducted in mouse xenograft models using THP1 leukemia cells. The compound would be administered via intraperitoneal or intravenous routes, and tumor growth inhibition and CBX8 target engagement would be assessed.
|
| ADME/Pharmacokinetics |
SW2_110A has a molecular formula of C42H60N6O7 and a molecular weight of 760.98. It is a synthetic peptide compound. It should be stored as a powder at -20°C for 3 years or in solvent at -80°C for 1 year.
|
| Toxicity/Toxicokinetics |
Toxicological data for SW2_110A are not detailed in the search results.
|
| References | |
| Additional Infomation |
SW2_110A is a novel, selective, cell-permeable inhibitor of the CBX8 Chromodomain (ChD). It inhibits the proliferation of THP1 leukemia cells driven by the MLL-AF9 translocation. It is a research compound for studying CBX8 function.
|
| Molecular Formula |
C42H60N6O7
|
|---|---|
| Molecular Weight |
760.96
|
| Appearance |
White to off-white solid powder
|
| 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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 :~125 mg/mL (~164.27 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3141 mL | 6.5706 mL | 13.1413 mL | |
| 5 mM | 0.2628 mL | 1.3141 mL | 2.6283 mL | |
| 10 mM | 0.1314 mL | 0.6571 mL | 1.3141 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
