sgk

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

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-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.

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]

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

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.

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-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.

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.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1 2 3, p70S6K, PKA, and ROCKI II.

BN201 (OCS-05) is a drug with neuroprotective and myelin repair effects, which acts mainly by activating serum glucocorticoid kinase-2 (SGK2), which in turn activates the FOXO3 pathway to promote neuronal survival and myelin repair. It is mainly used for the treatment of inflammatory neurological diseases such as multiple sclerosis (MS) and experimental autoimmune encephalomyelitis (EAE).BN201 is able to regulate multiple kinases in the insulin growth factor 1 (IGF1) pathway and cross the blood-brain barrier.

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.

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

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.

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).

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

11-Dehydrocorticosterone is a metabolite of glucocorticoids, a sodium-retaining agent that increases SGK mRNA expression in cardiac fibroblasts and dose-dependently inhibits aldosterone.

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.

AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1

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].