MDL | - |
---|---|
Molecular Weight | 949.52 |
Molecular Formula | C50H65ClN4O12 |
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 |
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF [1] .
FKBP12 [1]
KB02-SLF (2 µM; 4-72 hours; HEK293T cells) treatment promotes a substantial reduction in nuclear FKBP12 that is sustained across a 4-72 h time frame
[1]
.
Cell imaging studies confirms the selective loss of nuclear-localized FKBP12 in KB02-SLF-treated cells. KB02-SLF promotes the loss of FKBP12_NLS across a concentration of ~0.5-5µM, but shows varied reductions in activity at higher concentrations. The degradation of FKBP12_NLS induced by KB02-SLF is mediated by DCAF16
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
Cell Line: | HEK293T cells |
Concentration: | 2 µM |
Incubation Time: | 4 hours, 8 hours, 24 hours, 48 hours, 72 hours |
Result: | Promoted a substantial reduction in nuclear FKBP12 that was sustained across a 4-72 h time frame. |
Solid
Room temperature in continental US; may vary elsewhere.
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)
DMSO : 100 mg/mL ( 105.32 mM ; Need ultrasonic)
Concentration Solvent Mass | 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 |