itk

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton's Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.

JAK3-IN-1 is an orally active, selective and potent JAK3 inhibitor that can be used to study immune system diseases.

ITK Degrader 1, a highly selective interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice) degrader, induces rapid and prolonged degradation of ITK and effectively suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibody in vivo. Additionally, it demonstrates favorable plasma exposure levels [1].

ITK ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACS) that is used in the synthesis of PROTACs.

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminomethyl)benzamide) is the analogue of BMS-509744, which can potently and selectively inhibit Itk kinase activity. In vitro: BMS-509744 could reduce TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells [1]. In vivo: BMS-509744 suppressed the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1]. Clinical trial: Up to now, both BMS-509744 and ITK inhibitor is still in the preclinical development stage.

ITK inhibitor 6 is a selective and potent ITK inhibitor that acts on ITK (IC50: 4 nM), BTK (IC50: 133 nM), JAK3 (IC50: 320 nM), EGFR (IC50: 2360 nM), LCK (IC50: 155 nM). ITK inhibitor 6 inhibited the phosphorylation of PLCγ1 and ERK1 2 and showed anti-proliferative effect.

ITK inhibitor 2 (compound 4) is a potent and selective ITK inhibitor with an IC50= 2 nM.

ITK inhibitor 5 (compound 27) is a highly potent and selective ITK inhibitor, demonstrating IC50 values of 5.6 nM for ITK and 25 nM for BTK [1].

ITK TRKA-IN-1 is a chemical compound that functions as a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA). With an IC50 value of 1.0 nM, it effectively inhibits ITK activity and demonstrates a remarkable 96% inhibition of TRKA.

ITK Degrader 2 (Compound 30) functions as a modulator for targeted ubiquitination and serves as a molecule for targeted protein degradation, specifically degrading ITK [1].

PARP11 Inhibitor ITK7 (ITK7) is a potent, selective inhibitor of PARP11, demonstrating significant efficacy with an IC50 value of 14 nM. It is primarily utilized in research focused on cellular localization.

Vecabrutinib (SNS-062) is a potent, noncovalent inhibitor of BTK (Kd: 0.3 nM) and ITK (Kd: 2.2 nM), with an IC50 of 24 nM for ITK.

Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM 6 nM 8 nM 0.5 nM and 32 nM for JAK1 JAK2 JAK3 TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

GNE-4997 is a potent and selective inhibitor of the interleukin-2-inducible T-cell kinase (Ki: 0.09 nM). The correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.

CTA 056 is an interleukin-2 induced T cell kinase (ITK) inhibitor, inhibits the growth of MOLT-4 xenograft tumors in mice, induces apoptosis in Jurkat cells, and can be used in the study of autoimmune disorders and T cell malignancies.

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

BMS-986142 is a potent and highly selective reversible BTK inhibitor (IC50: 0.5 nM).

BMS-986143, an orally active, reversible BTK inhibitor with an IC50 value of 0.26 nM, is designed for autoimmune disease research. Additionally, it targets TEC, BLK, BMX, TXK, FGR, YES1, and ITK, exhibiting IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM, 19 nM, and 21 nM, respectively [1].

GSK-2250665A is a Itk inhibitor with pKi value of 9.2.

Cerdulatinib (PRT2070) is an novel oral dual Syk JAK inhibitor.

PROTAC BTK Degrader-13 (Compound 25) is a targeted BTK PROTAC degrader with a DC50 of 0.27 μM. It inhibits BTK activity with an IC50 of 0.44 μM and suppresses IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. This compound also inhibits the p38 MAPK signaling pathway, thereby blocking the activation of the BCR (B cell receptor) signaling pathway. [Pink: ligand for target protein BTK ligand 15; Black: linker; Blue: ligand for E3 ligase cereblon]

PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting ly

BAY 61-3606 (Syk inhibitor IV) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM), exhibiting no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.