Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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Targets |
FKBP12[1]
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ln Vitro |
Treatment with KB02-SLF (2 µM; 4-72 hours; HEK293T cells) significantly reduces nuclear FKBP12 and this effect lasts for the full 4-72 hours[1]. The selective loss of nuclear-localized FKBP12 in KB02-SLF-treated cells is confirmed by cell imaging experiments. Over a concentration range of approximately 0.5–5µM, KB02-SLF facilitates the loss of FKBP12_NLS, although at higher concentrations, it exhibits varying declines in activity. DCAF16 mediates the FKBP12_NLS degradation brought on by KB02-SLF[1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293T cells Tested Concentrations: 2 µM Incubation Duration: 4 hrs (hours), 8 hrs (hours), 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: Promoted a substantial reduction in nuclear FKBP12 that was sustained across a 4-72 h time frame. |
References |
[1]. Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nat Chem Biol. 2019 Jul;15(7):737-746.
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Molecular Formula |
C50H65CLN4O12
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Molecular Weight |
949.52
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CAS # |
2384184-40-9
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Related CAS # |
KB02-COOH;2375196-30-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
ClCC(N1C2C=CC(=CC=2CCC1)OCC(NCCOCCOCCC(NC1=CC=CC(=C1)[C@@H](CCC1C=CC(=C(C=1)OC)OC)OC([C@@H]1CCCCN1C(C(C(C)(C)CC)=O)=O)=O)=O)=O)=O
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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 : 100 mg/mL (105.32 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (5.27 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 50.0 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: 5 mg/mL (5.27 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 ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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: ≥ 5 mg/mL (5.27 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 | 1.0532 mL | 5.2658 mL | 10.5316 mL | |
5 mM | 0.2106 mL | 1.0532 mL | 2.1063 mL | |
10 mM | 0.1053 mL | 0.5266 mL | 1.0532 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.