PROTAC SGK3 degrader-2 

PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC₅₀ values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation. (Pink: SGK3 ligand (HY-167701), Blue: VHL Ligand (HY-120217A), Black: Linker (HY-130618), SGK3 ligand-linker conjugate (HY-176824))^[1].

PROTAC SGK3 degrader-2 (cisSGK3-PROTAC1) (0.03-3 μM, 8 h) fails to induce SGK3 degradation in HEK293, CAMA-1, ZR-75-1 and JIMT-1 cells; only at >1 μM does it reduce NDRG1 phosphorylation in HEK293 cells^[1].
PROTAC SGK3 degrader-2 (0.3 μM, 5 days) has no effect on SGK3 level or phosphorylation of TSC2, S6K1 and S6 in CAMA-1 and ZR-75-1 cells treated with GDC0941(HY-50094) or AZD5363 (HY-15431)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1157.38

C₅₇H₇₃FN₁₀O₁₁S₂

2381196-78-5

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Tovell H, et al. Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader. ACS Chem Biol. 2019 Sep 20;14(9):2024-2034.  [Content Brief]