2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Itk

Itk

Interleukin-2 inducible T-cell kinase; IL2 inducible T-cell kinase

Itk

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Itk (Interleukin-2-inducible T-cell kinase) is a Tec family tyrosine kinase that mediates signaling processes after T cell receptor engagement. Activation of Itk requires recruitment to the membrane via its pleckstrin homology domain, phosphorylation of Itk by the Src kinase, Lck, and binding of Itk to the SLP-76/LAT adapter complex. After activation, Itk phosphorylates and activates phospholipase C-gamma1 (PLC-gamma1), leading to production of two second messengers, DAG and IP3. IP3 and DAG stimulate the release of calcium ions from the endoplasmic reticulum and activate Protein Kinase C, respectively. In addition, Itk regulates the development of Th2 cells and their subsequent cytokine secretion, thereby modulating the immune response.

Studies have shown that ITK is involved in the pathogenesis of autoimmune diseases as well as in carcinogenesis. The loss of ITK or its activity either by mutation or by the use of inhibitors led to a beneficial outcome in experimental models of asthma, inflammatory bowel disease and multiple sclerosis among others. In humans, biallelic mutations in the ITK gene locus result in a monogenetic disorder leading to T cell dysfunction, etc. These findings put ITK in the strong focus as a target for drug development.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-150298
    Soquelitinib
    		Inhibitor 99.71%
    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.
    Soquelitinib
  • HY-11092
    BMS-509744
    		Inhibitor 98.05%
    BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC50 of 19 nM.
    BMS-509744
  • HY-12680
    PRN694
    		Inhibitor ≥99.0%
    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.
    PRN694
  • HY-108691
    PF-06465469
    		Inhibitor 99.48%
    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.
    PF-06465469
  • HY-109078
    Vecabrutinib
    		Inhibitor 99.76%
    Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC50 of 24 nM for ITK.
    Vecabrutinib
  • HY-185206
    BSJ-05-037
    		Degrader 99.83%
    BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma.
    BSJ-05-037
  • HY-182335
    PF-07245303
    		Inhibitor
    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.
    PF-07245303
  • HY-101321A
    Immepip dihydrobromide
    		Degrader 99.98%
    Immepip dihydrobromide is a H3 agonist. Immepip dihydrobromide can reduce cortical histamine release. Immepip dihydrobromide can be used for the research of neurological diseases.
    Immepip dihydrobromide
  • HY-128726
    ITK inhibitor 2
    		Inhibitor 99.50%
    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.
    ITK inhibitor 2
  • HY-148065
    FMF-06-098-1
    		Inhibitor 98.77%
    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.
    FMF-06-098-1
  • HY-12410
    GNE-9822
    		Inhibitor 98.47%
    GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki 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.
    GNE-9822
  • HY-120559
    GSK-2250665A
    		Inhibitor
    GSK-2250665A (Compound 13) is a selective Itk inhibitor with a pKi of 9.2.
    GSK-2250665A
  • HY-174280
    Modzatinib
    		Inhibitor
    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.
    Modzatinib
  • HY-150023
    BI-1622
    		Inhibitor
    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.
    BI-1622
  • HY-146672
    ITK inhibitor 6
    		Inhibitor
    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 inhibitor 6
  • HY-174903
    ITK-IN-6
    		Inhibitor 99.02%
    ITK-IN-6 is a highly potent and selective ITK inhibitor (Kd = 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-IN-6
  • HY-13232
    ITK antagonist
    		Inhibitor
    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.
    ITK antagonist
  • HY-149917
    ITK degrader 1
    		Degrader
    ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 consists of target protein ligand (red part) ITK ligand 1 (HY-168387), PROTAC linker (black part) Piperidine-C2-piperazine-Boc (HY-168388) and E3 ubiquitinase ligand (blue part) Thalidomide 5-fluoride (HY-W087383). E3 ubiquitinase and PROTAC linker can form Thalidomide-piperidine-C2-piperazine-Boc (HY-168389).
    ITK degrader 1
  • HY-16984
    GNE-4997
    		Inhibitor
    GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.
    GNE-4997
  • HY-E70833
    ITK Recombinant Human Active Protein Kinase
    ITK is the Tec family tyrosine kinase that has been implicated in T cell receptor (TCR) signaling. ITK Recombinant Human Active Protein Kinase is a recombinant ITK protein that can be used to study ITK-related functions.
    ITK Recombinant Human Active Protein Kinase
Cat. No. Product Name / Synonyms Application Reactivity