protein kinase g inhibitor-1

Protein kinase G inhibitor-1 is a potent Protein kinase G inhibitor, IC50= 0.9 uM.

BMT-090605 is a potent, selective AAK1 inhibitor with an IC50 of 0.6 nM, and inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively[1]. BMT-090605 also exhibits antinociceptive activity.

ATRkinase-IN-2 (Compound I-G-27) is an inhibitor of the ATR protein kinase, with a Ki value ranging from 0.01 to 1 μΜ. It is utilized in tumor research.

ATRkinase-IN-3 (Compound I-G-28) is an inhibitor of the ATR protein kinase, exhibiting a Ki value ranging from 0.01 to 1 μM, and is utilized in cancer research.

BMT-090605 hydrochloride is an effective and selective inhibitor of connexin-2 associated kinase 1 (AAK1) (IC50=0.6 nM). BMT-090605 hydrochloride inhibits BMP-2 induced protein kinase (BIKE) (IC50=45 nM) and cyclin G-related kinase GAK (IC50=60 nM). BMT-090605 hydrochloride shows anti-injury activity. BMT-090605 hydrochloride has research value in neuropathic pain.

GRK6-IN-1 (compound 18) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM, and has potential for study in multiple myeloma.

GDC-0623 (RG 7421) is a potent, ATP-uncompetitive MEK1 inhibitor with a Ki of 0.13 nM, currently in Phase 1.

Larixol acts as both an fMLP inhibitor and a modulator of various signaling pathways by inhibiting Src kinase, ERK1 2, p38, and AKT phosphorylation critical for immune responses. It disrupts the interaction between the βγ subunit of the Gi protein and downstream effectors linked to the fMLP receptor, thus abrogating fMLP-induced respiratory bursts. Additionally, larixol effectively reduces fMLP (0.1 μM)-triggered superoxide anion generation (IC50: 1.98 μM), cathepsin G secretion (IC50: 2.76 μM), and cellular chemotaxis, mitigating neutrophil hyperactivation and subsequent inflammation or tissue injury. Derivatives of larixol also demonstrate inhibitory activity on TRPC6 functional mutants associated with FSGS [1] [2].

GRL018-21 is a potent, highly selective inhibitor of G protein-coupled receptor kinase 5 (GRK5), exhibiting an IC50 of 10 nM [1].

(S)-Ro 32-0432 is a potent, selective inhibitor of protein kinase C (PKC) and G protein-coupled receptor kinase 5 (GRK5), demonstrating ATP-competitive and oral activity. It presents IC50 values of 9.3 nM for PKCα, 28 nM for PKCβI, 30 nM for PKCβII, 36.5 nM for PKCγ, and 108.3 nM for PKCε, showcasing its effectiveness against multiple PKC isoforms. Additionally, (S)-Ro 32-0432 inhibits T-cell activation, indicating its potential application in the research of chronic inflammatory and autoimmune diseases [1] [2].

GRK6-IN-3 is an inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 1.03 μM [1].

Isomaltulose monohydrate is an fMLP inhibitor that also inhibits Src kinase, ERK1 2, p38, and AKT phosphorylation signals in immune regulation. It interferes with the interaction between the βγ subunit of the fMLP receptor Gi protein and downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC_{50< sub>: 1.98 μM), cathepsin G release (IC50< sub>: 2.76 μM), and chemotaxis. It can improve excessive activation of neutrophils and reduce inflammation or tissue damage. Derivatives of Isomaltulose monohydrate have been found to inhibit FSGS-related TRPC6 functional mutants [1].}