itk

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

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.

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.

Rilzabrutinib (PRN1008) is a small-molecule inhibitor and a reversible covalent inhibitor of Bruton's tyrosine kinase (BTK) (IC50 = 1.3 nM), featuring high selectivity, oral activity, and favorable cell permeability, exhibiting anti-inflammatory and immunomodulatory activities.

BMS-509744 is a selective, ATP-competitive Itk inhibitor with an IC50 of 19 nM. It inhibits IL-8 expression and HIV infection, ameliorates pulmonary inflammation in allergic asthma mouse models, and reduces Imiquimod-induced skin inflammation in mice.

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.

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

PF-06465469 is a covalent ITK inhibitor (IC₅₀ = 2 nM) that also inhibits BTK. PF-06465469 suppresses CXCL12-mediated cell migration, decreases PD-1 and LAG-3 expression. PF-06465469 shows strong potential application in leukemia and T-cell lymphoma research.

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

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.

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

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

Ibrutinib-biotin, a probe consisting of Ibrutinib linked to biotin via a long-chain linker, has an IC50 of 0.755-1.02 nM for BTK.

Modzatinib (ITKkinase-IN-1) (compound I) is an inhibitor targeting ITK kinase with an IC50 of 8 nM in Jurkat cells, useful for researching inflammatory diseases. In hPBMC cells, it inhibits JAK3 with an IC50 of 23 nM (based on IL-2/pSTAT5 levels) and shows no inhibitory effect on JAK2.

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

ITK-IN-6 is a potent and selective ITK inhibitor (Kd = 387 nM). It binds directly to the ITK kinase domain. This compound prevents the release of pro-inflammatory cytokines and the activation and differentiation of Th2 and Th17 cells. ITK-IN-6 improves asthma progression by reducing inflammatory cell infiltration, mucus production, and IgE generation. It significantly inhibits airway inflammation and is used in asthma research.

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

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.

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Y-27632 is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

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