| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Cereblon
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|---|---|
| References | |
| Additional Infomation |
Ligand-dependent protein degradation has become a highly attractive strategy for pharmacologically modulating cellular protein content. However, to date, only a handful of E3 ubiquitin ligases have been found to participate in this process. This study employs a chemical proteomics strategy, utilizing broadly reactive, cysteine-directed electrophilic fragments coupled with selective ligands targeting intracellular proteins (e.g., SLF for FKBP12, JQ1 for BRD4), to screen for heterobifunctional degradative compounds (or proteolytic-targeting chimeras, PROTACs) that function by covalently binding to E3 ubiquitin ligases. This method identified DCAF16—a substrate recognition component of the previously little-studied CUL4-DDB1 E3 ubiquitin ligase—as a target for electrophilic PROTACs that promote the degradation of nuclear proteins. We found that modification of only a small fraction (~10–40%) of DCAF16 supports protein degradation, suggesting that electrophilic PROTACs have the potential to induce novel substrate degradation without significantly interfering with the function of the involved E3 ligases.
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| Molecular Formula |
C13H14CLNO4
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|---|---|
| Molecular Weight |
283.707562923431
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| Exact Mass |
283.061
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| CAS # |
2375196-30-6
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| Related CAS # |
KB02-SLF;2384184-40-9;KB02-JQ1;2384184-44-3
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| PubChem CID |
137347746
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
350
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZWIYQLVGARZWJJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H14ClNO4/c14-7-12(16)15-5-1-2-9-6-10(3-4-11(9)15)19-8-13(17)18/h3-4,6H,1-2,5,7-8H2,(H,17,18)
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| Chemical Name |
2-[[1-(2-chloroacetyl)-3,4-dihydro-2H-quinolin-6-yl]oxy]acetic acid
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| Synonyms |
KB02-COOH; 2375196-30-6; SCHEMBL22075942; Acetic acid, 2-[[1-(2-chloroacetyl)-1,2,3,4-tetrahydro-6-quinolinyl]oxy]-; 2-{[1-(2-chloroacetyl)-1,2,3,4-tetrahydroquinolin-6-yl]oxy}acetic acid; 2-((1-(2-chloroacetyl)-1,2,3,4-tetrahydroquinolin-6-yl)oxy)acetic acid; KB02-COOH?; 2-[[1-(2-chloroacetyl)-3,4-dihydro-2H-quinolin-6-yl]oxy]acetic acid;
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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) |
DMSO :~66.67 mg/mL (~234.99 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (17.62 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 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 (17.62 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 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 (17.62 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 | 3.5247 mL | 17.6236 mL | 35.2473 mL | |
| 5 mM | 0.7049 mL | 3.5247 mL | 7.0495 mL | |
| 10 mM | 0.3525 mL | 1.7624 mL | 3.5247 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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