sgk1-in-2

SGK1-IN-2 (14h) is a selective inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1), with an IC50 of 5 nM at a 10 μM ATP concentration.

SGK1-IN-1 (compound 14n) is a highly potent SGK1 (Serum/Glucocorticoid Regulated Kinase 1) inhibitor, with inhibitory activities of 41 nm, 128 nm, and 310 nm against hSGK1/2/3 at 500 μM ATP, respectively, and can be used for studying SGK1-related cancers and metabolic diseases.

PT109 is a multikinase inhibitor that targets JNK and other kinases, playing a crucial role in anti-inflammatory, antioxidative, neurogenic, and synaptogenic processes. Specifically, PT109 inhibits JNK isoforms with the following IC50 values: JNK1 at 0.143 μM, JNK2 at 0.831 μM, and JNK3 at 0.285 μM. It also inhibits SGK isoforms (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM) and ROCK2 (IC50=34 μM). Additionally, PT109 reprograms polymorphic glioblastoma multiforme (GBM) into oligodendroglia via the PTBP1/PKM1/2 pathway and alters the metabolic pattern of GBM to exhibit antiglioma activity.

PROTACSGK3degrader-2 is the cis-diastereomer of PROTACSGK3degrader-1 (SGK3-PROTAC1), featuring a cis-hydroxy group in its VH032 section, which prevents binding to the VHL E3 ligase. This compound inhibits SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but does not degrade SGK3. It serves as a control compound for studying the specific degradation effects mediated by SGK3-PROTAC1.