sgk-1

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.

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 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.

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

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-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.

SGK1-IN-3 (compound 3a) is a potent serum- and glucocorticoid-regulated kinase 1 (SGK1) inhibitor with an IC50 value of less than 1 μM, SGK1-IN-3 is applied in musculoskeletal research to explore SGK1-mediated signaling pathways and its potential role in osteoarthritis pathogenesis and therapeutic intervention.

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.

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.

CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. It also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

CKI-7 free base is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor, also inhibiting SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC coupler that targets SGK3 and binds ligand to VH032 VHL, inducing degradation of endogenous SGK3. It inhibits GDC0941-induced proliferation of cancer cells. [5017-88-83-4]

PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1 and also shows significant inhibitory activity against SGK-1, PKA, CaMK-1, GSK3β, and MSK1, making it potentially valuable for cancer research [1].