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You are here:Home-Inhibitors & Agonists-Tyrosine Kinase-ITK

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Itk (Interleukin-2-inducible T-cell kinase) is a member of the TEC family of kinases and is highly expressed in T cells. Itk plays a role in T-cell proliferation, differentiation, cytokine release and chemotaxis. Itk is functionally important for the development and effector function of Th2 and Th17 cells. Itk is an attractive target for the treatment of T-cell-mediated inflammatory diseases.

Cat. No. Product Name CAS No. Information
H7945

PRN694

 		1575818-46-0

PRN694 (PRN-694) is a highly selective, potent, covalent inhibitor of ITK and RLK with IC50 of 0.3 and 1.4 nM, respectively; also potently inhibits family member TEC (IC50=3.3 nM), weakly inhibits BTK (IC50=17 nM), has no activity against EGFR, ERBB2 and ERBB4 in a panel of 250 kinases; prevents T-cell receptor- and Fc receptor-induced cellular and molecular activation, inhibits T-cell receptor-induced T-cell proliferation, and blocks proinflammatory cytokine release as well as activation of Th17 cells; demonstrates inhibitory activity against T-cell prolymphocytic leukemia cells in ex vivo assays; PRN694 is a potent inhibitor of Th1 and Th17 differentiation and cytokine production, markedly reduces disease progression in models of colitis.
H7944

ITK inhibitor

 		439574-61-5

ITK inhibitor (CAS 439574-61-5 )?is a Interleukin-2-inducible T-cell kinase (Itk) inhibitor.
H7943

CTA056

 		1265822-30-7

CTA056 (CTA 056) is a potent, selective inhibitor of interleukin-2-inducible T-cell kinase (Itk) with IC50 of ~100 nM, also inhibits Btk (IC50=400 nM), but shows no significant inhibition for Etk (BMX kinase, IC50=5 uM); CTA056 shows selectivity for Itk over other Tec family members; inhibits the phosphorylation of Itk and its effectors including PLC-γ, Akt, and ERK, as well as the decreased secretion of targeted genes such as IL-2 and IFN-γ in treated Jurkat and MOLT-4 cells; also exhibits apoptosis-inducing potential in Jurkat cells; demonstrates cytotoxic effect in xenograft models of T-cell leukemia and lymphoma.
H7942

BMS-509744

 		439575-02-7

A potent, selective, ATP-competitive ITK inhibitor with IC50 of 19 nM; displays >200-fold selectivity over others Tec family tyrosine kinases and > 30-fold over a broad panel protein kinases; reduces TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion and T-cell proliferation in vitro; significantly diminishes lung inflammation in mouse model of allergy/asthma; also potently blocks wild-type HIV-1 infectivity and replication in vitro.

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