KB02-SLF
Based on 1 Customer Validation
KB02-SLF is a nuclear FKBP12 covalent PROTAC degrader. KB02-SLF covalently modifies cysteine residues in DCAF16, forms a ternary complex with nuclear FKBP12, and mediates degradation via the CUL4-DDB1 E3 ubiquitin ligase pathway. KB02-SLF promotes polyubiquitination and proteasomal degradation of nucleus-localized FKBP12. KB02-SLF can be used in breast cancer research.
(Pink: FKBP12 ligand (HY-114872); Blue: Cereblon ligand (HY-131385); Black: linker (HY-42149)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.25%
- No. CAS: 2384184-40-9
- Fòrmula: C50H65ClN4O12
- Peso molecular:949.52
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Covalent Screening Library
HY-L036
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Ver todos los productos específicos de isoformas PROTACs
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Actividad biológica
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FKBP12 |
KB02-SLF (2 µM; 4-72 h) promotes sustained, concentration-dependent degradation of nuclear-localized FLAG-FKBP12_NLS in HEK293T cells via a polyubiquitination- and Cullin-RING ubiquitin ligase-dependent pathway[1].
KB02-SLF promotes the degradation of nuclear-localized FLAG-FKBP12_NLS in MDA-MB-231 cells[1].
KB02-SLF (2-10 µM; 2 h) promotes the formation of a complex between nuclear-localized FLAG-FKBP12NLS and DCAF16-containing components of the Cullin-RING ubiquitin ligase in HEK293T and MDA-MB-231 cells[1].
KB02-SLF (2 µM; 24 h) induces selective degradation of ACAT1 in HEK293T cells, but does not degrade BRD4, BRD2 or BRD3[1].
KB02-SLF (0.625-40 µM; 24 h) exhibits cytotoxicity against HEK293T cells, with an IC50 value of 14 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells stably expressing nuclear-localized FLAG-FKBP12_NLS
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Concentration:2 µM
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Incubation Time:4， 8， 24， 48， 72 h
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Result:Induced a substantial, sustained reduction in nuclear FKBP12_NLS levels across 4-72 h of treatment.
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Cell Line:HEK293T cells
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Concentration:0.625-40 µM
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Incubation Time:24 h
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Result:Showed cytotoxicity at concentrations >10 µM, with an IC50 of 14 µM.
Chemical Information
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No. CAS 2384184-40-9
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Appearance Solid
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Peso molecular 949.52
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Fòrmula C50H65ClN4O12
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Color White to yellow
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SMILES
O=C([C@H]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[C@@H](C2=CC=CC(NC(CCOCCOCCNC(COC3=CC4=C(N(C(CCl)=O)CCC4)C=C3)=O)=O)=C2)CCC5=CC=C(OC)C(OC)=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
DMSO : 100 mg/mL (105.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (5.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (5.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0532 mL | 5.2658 mL | 10.5316 mL | 26.3291 mL |
| 5 mM | 0.2106 mL | 1.0532 mL | 2.1063 mL | 5.2658 mL | |
| 10 mM | 0.1053 mL | 0.5266 mL | 1.0532 mL | 2.6329 mL | |
| 15 mM | 0.0702 mL | 0.3511 mL | 0.7021 mL | 1.7553 mL | |
| 20 mM | 0.0527 mL | 0.2633 mL | 0.5266 mL | 1.3165 mL | |
| 25 mM | 0.0421 mL | 0.2106 mL | 0.4213 mL | 1.0532 mL | |
| 30 mM | 0.0351 mL | 0.1755 mL | 0.3511 mL | 0.8776 mL | |
| 40 mM | 0.0263 mL | 0.1316 mL | 0.2633 mL | 0.6582 mL | |
| 50 mM | 0.0211 mL | 0.1053 mL | 0.2106 mL | 0.5266 mL | |
| 60 mM | 0.0176 mL | 0.0878 mL | 0.1755 mL | 0.4388 mL | |
| 80 mM | 0.0132 mL | 0.0658 mL | 0.1316 mL | 0.3291 mL | |
| 100 mM | 0.0105 mL | 0.0527 mL | 0.1053 mL | 0.2633 mL |
KB02-SLF Related Classifications
HY-129610 Related Classifications
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