sgk3

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

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]

OTs-C6-OBn, an alkyl chain-based PROTAC linker, is utilized in the synthesis of PROTAC SGK3 degrader-1[1].

Ald-CH2-PEG3-CH2-Boc, a PEG- and Alkyl ether-based PROTAC linker, is utilized for the synthesis of SGK3 kinase PROTAC degrader[1].

Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PEG-based PROTAC linker used in the synthesis of various PROTACs, including PROTAC SGK3 degrader-1. PROTACs consist of two distinct ligands connected by a linker; one ligand binds to an E3 ubiquitin ligase, while the other specifically interacts with the target protein, enabling selective degradation of target proteins via the intracellular ubiquitin-proteasome system[1].

PEG3-C4-OBn, a polyethylene glycol (PEG)-based PROTAC linker, is utilized in crafting the PROTAC SGK3 degrader-1, a potent SKG3 degrader leveraging PROTAC technology [1][2].

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 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.