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].

Product Specifications

CAS Number

[2381196-78-5]

UNSPSC

12352005

Target

PROTACs; SGK

Related Pathways

Metabolic Enzyme/Protease; PROTAC

Field of Research

Cancer

Smiles

O=C(N1[C@@H](C[C@@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOCCOCCCCCCN(CCO4)C[C@@H]4COC5=C(C=NN6)C6=NC(C7=CC=C(C=C7)NS(=O)(C8=C(C=CC(C)=C8)F)=O)=N5)=O

Molecular Formula

C57H73FN10O11S2

Molecular Weight

1157.38

References & Citations

[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.