22-SLF
Based on 1 Customer Validation
22-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM. 22-SLF interacts with C227 and C228 in FBXO22 to induce a ternary complex between FKBP12 and FBXO22, and degrades FKBP12 in a FBXO22-dependent manner. 22-SLF can be used for fundamental cancer research as a probe to study the FBXO22 degradation pathway.
(Pink: FKBP12 ligand (HY-114872); Blue: VHL ligand (HY-163826); Black: linker (HY-163821)).
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- Reinheit: 95.72%
- CAS. Nr.: 3079209-82-5
- Formel: C60H76ClN5O13S
- Molecular Weight:1142.79
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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FKBP12 |
22-SLF (2-5 μM, 24 h) has no effect on FKBP12-EGFP levels in the SFFV promoter system but induces a mild yet significant reduction of FKBP12 (~30 %) in the hPGK promoter system[1].
22-SLF (0.025-15 μM, 2-24 h) recruits FBXO22 to FKBP12, resulting in the proteasomal degradation of FKBP12 in an FBXO22-dependent manner, with a Dmax of ~ 89%[1].
22-SLF (2 μM, 2 h) effectively drives the formation of a ternary complex involving 22-SLF, FBXO22 and FKBP12 by engaging C227/228 in FBXO22, with approximately 20% engagement of FBXO22 C228 at 2 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 and A549 cells
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Concentration:0.025, 0.1, 0.25, 0.5, 0.75, 1, 2, 5, 7.5, 10 and 15 μM for HEK293T cells, 2, 10, and 50 μM for A549 cells
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Incubation Time:2, 4, and 8 h for HEK293T cells, 2, and 24 h for A549 cells
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Result:Induced FKBP12 degradation in a FBXO22-dependent manner.
Its FKBP12 degradation was blocked by the proteasome inhibitor MG132 (HY-13259), the neddylation inhibitor MLN4924 (HY-70062) and the FKBP12 ligand SLF (HY-114872).
Induced rapid and nearly complete degradation of FKBP12 within 2 hours.
Degraded FKBP12 in a dose- and time-dependent manner.
Induced FKBP12 degradation in A549 wildtype, but not FBXO22 knockout cells at 2 μM. Competed with 22-biotin-enriched FBXO22 in a dose-dependent manner, thereby further confirming its direct binding to FBXO22.
Its FKBP12 degradation was partially blocked by single mutation of C227 or C228, and completely abolished by the double mutant C227A/C228A.
Its FKBP12 degradation was supported by mouse FBXO22.
Its FKBP12 degradation was abolished by mutation of both C226 and C227 in mouse FBXO22.
The formation of the 22-SLF/FKBP12/FBXO22 ternary complex was confirmed by co-immunoprecipitation.
Chemical Information
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CAS. Nr. 3079209-82-5
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Appearance Solid
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Molecular Weight 1142.79
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Formel C60H76ClN5O13S
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Color Light yellow to brown
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SMILES
CCC(C)(C(C(N1CCCC[C@H]1C(O[C@@H](C2=CC(OCC(NCCCOCCOCCOCCCN(C(C3=NC4=C(S3)C=CC=C4)C(NCC5=CC=CC=C5)=O)C(CCl)=O)=O)=CC=C2)CCC6=CC=C(C(OC)=C6)OC)=O)=O)=O)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
22-SLF Related Classifications
HY-163807 Related Classifications
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