PeptideDB

SW2_110A

SW2_110A

CAS No.:

SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor (antagonist) with a Kd of 800 nM. SW2_110A is 5-fo
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SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor (antagonist) with a Kd of 800 nM. SW2_110A is 5-fold less selective for CBX8 ChD than all other CBX paralogues in vitro.

Physicochemical Properties


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)

Biological Activity


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].
References

[1]. Optimization of Ligands Using Focused DNA-Encoded Libraries To Develop a Selective, Cell-Permeable CBX8 Chromodomain Inhibitor. ACS Chem Biol. 2020 Jan 17;15(1):112-131.


Solubility Data


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.

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.
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 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 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.