SGK

EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.

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

GSK 650394 is a glucocorticoid- and serum-regulated kinase 1 (SGK1) inhibitor which displays antiproliferative properties against the LNCaP prostate carcinoma cell line.

EMD638683 is a potent inhibitor of SGK1 with an IC50 value of 3 uM.

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

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM.CKI-7 is a selective Cdc7 kinase inhibitor.

Serum/Glucocorticoid Regulated Kinase 1 Human Recombinant

SGK3-PROTAC1 is a PROTAC molecule designed to selectively degrade SGK3 by linking the 308-R SGK inhibitor to the VHL-binding ligand VH032. Through recruitment of the VHL E3 ligase, SGK3-PROTAC1 induces proteasomal degradation of SGK3, providing a targeted approach for studying SGK3 function in cellular signaling and disease.

HaloPROTAC-E is a potent and selective PROTAC designed to degrade Halo-tagged endoplasmic reticulum-localized proteins, including SGK3 and VPS34, with a DC₅₀ of 3–10 nM. It effectively induces degradation of endogenous VPS34 complexes (VPS34, VPS15, Beclin1, and ATG14) when Halo-tagged, leading to inhibition of autophagy. HaloPROTAC-E is a valuable tool for conditional protein degradation and autophagy research.

(S,S,S)-VH032 is a ligand for the E3 ubiquitin ligase von Hippel-Lindau (VHL), enabling targeted protein degradation through the formation of PROTACs. It plays a crucial role in the synthesis of PROTAC SGK3 degrader-2, facilitating the selective degradation of SGK3 and other target proteins. This compound is valuable for research in protein regulation and targeted therapeutic strategies.

SI-113 is an inhibitor of SGK1, demonstrating an IC50 of 600 nM. This compound is known to induce autophagy, making it a valuable tool for studying cellular mechanisms related to SGK1 activity. It has potential applications in research areas such as cancer biology and neurodegenerative diseases, where modulation of autophagy may be beneficial.

SGK1-IN-4 is a selective inhibitor of Serum/Glucocorticoid-regulated Kinase 1 (SGK1), demonstrating oral bioactivity. This compound has potential applications in the study of osteoarthritis, targeting pathways involved in inflammation and cellular signaling. Its ability to modulate SGK1 activity makes it a valuable tool for investigating SGK1's role in various biological processes and disease states.

SGK1-IN-2 is a selective inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1), characterized by an IC50 value of 5 nM at an ATP concentration of 10 μM. This compound effectively regulates SGK1 activity, influencing various cellular processes such as cell survival, proliferation, and metabolism. SGK1-IN-2 is valuable for research applications focused on cancer biology, cardiovascular diseases, and metabolic disorders.

SGK1-IN-3 is a potent selective inhibitor of SGK1, exhibiting an IC50 of less than 1 μM. This compound demonstrates significant inhibitory activity, making it a valuable tool for investigating the role of SGK1 in various biological processes. Its application in research may provide insights into the mechanisms underlying osteoarthritis and contribute to the development of novel therapeutic strategies.

308-R-C4-PEG3-C1-Boc is a SGK3 ligand-linker conjugate designed for use in the synthesis of PROTAC SGK3 degrader-2. This compound facilitates targeted protein degradation by effectively linking the SGK3 ligand with a degradation mechanism. Its application in chemical research is particularly valuable for studies involving SGK3 modulation and related cellular pathways.

SGK1-IN-6 is a selective inhibitor of SGK1, demonstrating a high potency with an IC50 value of 0.39 μM. This compound effectively suppresses tumor growth in the PC3 xenograft model in BALB/c nude mice while exhibiting no significant toxicity. SGK1-IN-6 is ideal for research applications focused on cancer biology and the exploration of SGK1's role in tumorigenesis.

PROTAC SGK3 degrader-2 is a selective PROTAC designed to engage SGK3 while targeting its degradation pathways. Unlike its trans counterpart, this compound possesses a cis hydroxyl group in the VH032 moiety, preventing its interaction with the VHL E3 ligase. It exhibits inhibitory effects on SGK3, SGK1, and S6K1, with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but does not induce SGK3 degradation. PROTAC SGK3 degrader-2 serves as an essential control reagent in research examining the specific biological effects of SGK3-PROTAC1-mediated degradation.

SGK1-IN-5 is a potent inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with an IC50 of 3 nM. This compound effectively inhibits SGK1-dependent phosphorylation of glycogen synthase kinase 3 beta (GSK3β) in U2OS cells, demonstrating an IC50 of 1.4 μM. SGK1-IN-5 is valuable for research applications related to osteoarthritis and rheumatism, contributing to the understanding of pathways involved in inflammatory and degenerative joint diseases.

Boc-C1-PEG3-C4-OBn is a versatile PROTAC linker that incorporates a polyethylene glycol (PEG) structure. This compound facilitates the synthesis of various PROTACs, including the SGK3 degrader-1. By connecting ligands for E3 ubiquitin ligases and target proteins, Boc-C1-PEG3-C4-OBn is instrumental in harnessing the ubiquitin-proteasome system for the selective degradation of target proteins, providing valuable insights for protein regulation studies and therapeutic applications.

OTs-C6-OBn is an alkyl chain-based PROTAC linker designed for the synthesis of PROTAC conjugates targeting the SGK3 protein. This compound facilitates targeted protein degradation by linking E3 ligases to specific protein substrates, thereby enhancing the efficacy of PROTACs in biological research. It is suitable for applications in drug development and proteostasis modulation studies.

PEG3-C4-OBn is a polyethylene glycol (PEG)-derived linker designed for use in PROTAC (Proteolysis Targeting Chimeras) applications. This compound facilitates the synthesis of PROTAC SGK3 degrader-1, which effectively induces targeted degradation of SGK3, a serine/threonine protein kinase. PEG3-C4-OBn is instrumental in advancing research related to targeted protein degradation and cellular regulation mechanisms.

Ald-CH2-PEG3-CH2-Boc is a PEG- and alkyl/ether-based PROTAC linker designed to facilitate the construction of proteolysis-targeting chimeras (PROTACs). This linker plays a crucial role in synthesizing SGK3 kinase PROTAC degraders, enabling selective degradation of target proteins. Its unique structure enhances solubility and promotes effective engagement with target proteins for research applications in targeted protein degradation and mechanistic studies of cellular pathways.

SGK1-IN-9 is an inhibitor of serum/glucocorticoid-regulated kinase 1 (SGK1). This compound exhibits potential anti-cancer activity by modulating cell survival pathways and influencing tumor cell proliferation. It is suitable for use in cancer research to investigate the role of SGK1 in various malignancies and explore therapeutic strategies targeting this kinase.

SGK1-IN-7 is a selective inhibitor of SGK1, exhibiting a blood-brain barrier permeability with an IC50 of 0.72 μM. This compound effectively reduces the phosphorylation of TAU protein at the Ser396 and Ser214 sites and counters the toxicity induced by Okadaic acid. SGK1-IN-7 is a valuable tool for research into the mechanisms underlying Alzheimer's disease.

SGK1-IN-8 is a potent inhibitor of SGK1 and GSK3β, exhibiting an IC50 of 0.11 μM against human SGK1 and 3.39 μM against human GSK3β. This compound effectively inhibits the catalytic activities of both SGK1 and GSK3β, leading to a reduction in the phosphorylation of the TAU protein at the Ser214 site. SGK1-IN-8 is utilized in research focused on Alzheimer's disease and related neurodegenerative disorders.