sgk1

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.

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.

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.

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

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).

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

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

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.

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

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.

SGK1-IN-3 hydrochloride (compound 3a) is an efficacious, orally bioavailable SGK1 inhibitor. The serine/threonine kinase SGK1 acts as an activator of the β-catenin pathway and strongly stimulates cartilage degradation, being upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 hydrochloride holds potential for osteoarthritis research.

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.

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

Dracorhodin perchlorate inhibits cell growth, and induces apoptosis in fibroblasts in a dose-and time-dependent manner, arresting cell cycle at G1 phase, may as a candidate for anti-breast cancer. Dracorhodin perchlorate can inhibit high glucose-induced serum and glucocorticoid induced protein kinase 1 (SGK1) and fibronectin(FN) expression in human mesangial cells, and this may be part of the mechanism of preventing and treating renal fibrosis of DN.

Dracorhodin perchlorate (Standard) is a reference standard for research and analysis in studies involving Dracorhodin perchlorate. Dracorhodin perchlorate inhibits cell growth, and induces apoptosis in fibroblasts in a dose-and time-dependent manner, arresting cell cycle at G1 phase, may as a candidate for anti-breast cancer. Dracorhodin perchlorate can inhibit high glucose-induced serum and glucocorticoid induced protein kinase 1 (SGK1) and fibronectin(FN) expression in human mesangial cells, and this may be part of the mechanism of preventing and treating renal fibrosis of DN.