sgk1 inhibitor

SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2. It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells and decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719. SGK1 inhibitor reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.

SI-113 is a potent and selective inhibitor of SGK1, a serine threonine protein kinase, that modulates several oncogenic signaling cascades.

EMD638683 is a highly selective SGK1 inhibitor with an IC50 of 3 μM. EMD638683 (R-Form) is the R-form of this compound.

EMD638683 is a highly selective SGK1 inhibitor with an IC50 of 3 μM [EMD638683 S-Form is the S-form of EMD638683].

SGK1-IN-1 is a highly active and selective SGK-1 inhibitor with an IC50 of 1 nM.

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.

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.

SGK1-IN-6 (compound 12f) is an SGK1 inhibitor with an IC50 value of 0.39 μM. In PC3 xenograft models using BALB c nude mice, SGK1-IN-6 effectively hinders tumor growth without causing any observable toxicity.

GSK 650394 is an inhibitor of serum- and glucocorticoid-regulated kinases (SGK) that inhibits SGK1 and SGK2 (IC50=62 103 nM). GSK 650394 has antitumor activity and also inhibits osteoclast differentiation and prevents bone loss.

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

SGK1-IN-3 is a potent, orally active SGK1 inhibitor. Among them, the serine threonine kinase SGK1, an activator of the β-linked protein pathway and a powerful stimulator of cartilage degradation, has been found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 shows research potential in osteoarthritis.

EMD638683,a novel SGK inhibitor with antihypertensive potency(with an IC50 of 3 μM).

SGK1-IN-4 is a selective inhibitor of SGK1 and can be used in studies about osteoarthritis.