Itk Inhibitor

Soquelitinib (CPI-818) is an orally active and highly selective covalent interleukin-2-inducible kinase (ITK) inhibitor. Soquelitinib is active in six different models of T cell-mediated inflammatory and immune disease, including acute and chronic asthma, pulmonary fibrosis, systemic sclerosis (scleroderma), psoriasis, and acute graft versus host disease with Th2 cytokine product inhibition. Soquelitinib increases tumor infiltration of normal CD8⁺ cells that possess enhanced T effector function.

BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC₅₀ of 19 nM.

PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC₅₀s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo.

PF-06465469 is a covalent inhibitor of ITK with an IC₅₀ of 2 nM. PF-06465469 also inhibits BTK. PF-06465469 inhibits cell migration in response to CXCL12. PF-06465469 decreases PD-1 and LAG-3 expression. PF-06465469 can be used to study leukemia and T-cell lymphoma.

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

PF-07245303 is a ITK/TRK inhibitor. PF-07245303 reduces the production of inflammatory cytokines such as IL-4 and IFNγ, and inhibits the phosphorylation of PLCγ1. PF-07245303 inhibits nerve growth factor-induced basophil activation and the phosphorylation of TRKA. PF-07245303 reduces oxazolone-induced ear swelling in mouse ear tissues. PF-07245303 is applicable to research related to atopic dermatitis.

ITK-IN-7 is a selective ITK inhibitor with an IC₅₀ of 16 nM and a K_i of 0.48 nM. ITK-IN-7 reduces IL-2 secretion levels in T cells and in mouse models stimulated by anti-CD3 monoclonal antibodies. ITK-IN-7 can be used for basic and translational research related to ITK inhibition, such as research on leukemia.

FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.

ITK inhibitor 2 is a ITK inhibitor with an IC₅₀ of 2 nM. ITK inhibitor 2 is used for research on inflammatory diseases, allergic diseases, autoimmune diseases and transplant rejection.

GNE-9822 is a potent, orally active and selective ITK inhibitor with a K_i value of 0.7 nM, and an EC₅₀ value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.

GSK-2250665A (Compound 13) is a selective Itk inhibitor with a pK_i of 9.2.

Modzatinib (ITK kinase-IN-1) is an oral active, selective, covalent ITK/JAK3 dual-target inhibitor with IC₅₀ values of 8 nM and 23 nM, respectively. Modzatinib exhibits anti-inflammatory activity and can be used in the research of autoimmune and inflammatory diseases.

BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC₅₀ of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.

ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC₅₀s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities.

ITK-IN-6 is a highly potent and selective ITK inhibitor (K_d = 387 nM). ITK-IN-6 directly binds to the ITK kinase domain. ITK-IN-6 blocks 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 and IgE production. ITK-IN-6 significantly inhibits airway inflammation and is used in asthma research.

ITK antagonist (compound 10 n) is a potent, orally active and selective ITK (Interleukin-2 inducible T-cell kinase) antagonist (IC₅₀=1 and 20 nM in different assays). ITK antagonist inhibits insulin receptor kinase (IRK) with an IC₅₀ of 160 nM.

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

ITK inhibitor 5 (compound 27) is a potent and selective ITK inhibitor with IC₅₀s of 5.6, 25 nM for ITK, BTK, respectively.

ITK/TRKA-IN-1 is 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 and 96 % inhibition, respectively.

ITK ligand 1 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). ITK ligand 1 can be used in the synthesis of PROTACs (e.g. HY-149917).