10-SLF

10-SLF (0.1-5 μM; 2-24 h) selectively promotes proteasome- and Cullin-RING ligase-dependent degradation of FLAG-FKBP12_NLS in HA-FBXW7^R465C-expressing HEK293T cells, with maximal degradation observed after 8 h of 1 μM treatment^[1].
10-SLF (1 μM) induces UPS-dependent ubiquitination of FKBP12 exclusively in HA-FBXW7^R465C-expressing HEK293T cells, as measured by a significant increase in normalized NanoBRET ratio (*P < 0.001)^[1].
10-SLF (1 μM) induces UPS-dependent engagement of FKBP12 with the proteasomal subunit PSMD3 exclusively in HA-FBXW7^R465C-expressing HEK293T cells, as measured by a significant increase in normalized NanoBRET ratio (*P < 0.001)^[1].
10-SLF (5 μM) induces degradation of FLAG-FKBP12_NLS in parental FBXW7^R465C-expressing AsPC-1 cells, but not in FBXW7^R465C KO AsPC-1 cells, demonstrating dependence on endogenous FBXW7^R465C[1].
10-SLF (2 μM) promotes formation of a ternary complex between FLAG-FKBP12_NLS and FBXW7 variants containing the KRAS^G12C-like FBXW7^R465C mutation (FBXW7^R465C and FBXW7^R465C/C466A) in HEK293T cells, but not with FBXW7 WT or FBXW7^C466A[1].
10-SLF (0.01-10 μM) induces a dose-dependent interaction between FKBP12 and FBXW7^R465C in HEK293T cells (with a hook effect at 5 and 10 μM), but does not induce interaction with FBXW7 WT^[1].
10-SLF (1 μM) engages 8 off-target cysteines (≥50% engagement) in HA-FBXW7-R465C-expressing HEK293T cells, while the target FBXW7-R465C peptide was not detected in the assay^[1].