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BMS-509744
Cat No.
CEI-1253
Description
BMS-509744 is a potent and selective inhibitor of Itk kinase with IC50 value of 19 nM.
Product Overview
BMS-509744 is a selective inhibitor of ITK with IC50 value of 15 nM. ITK (IL-2-inducible T cell kinase) is an enzyme and plays an important role in T cell receptor signaling. It has been reported that ITK involves in the Th2-mediated inflammatory process and thus be regarded as a promising target for Th2-mediated inflammatory/immunosuppressive diseases treatment, such as asthma, rhinitis, allergies and atopic dermatitis. BMS-509744 is a potent ITK inhibitor and is different from the reported ITK inhibitor RO5191614. When tested with human and murine cells, administration of BMS-509744 reduced TCR-induced functions by functioning on PLCgamma1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion and T-cell proliferation. In wild-typr HIV1 infected cells, BMS-509744 treatment blocked its infectivity and replication by inhibiting ITK, while has no effect on Nef-defective HIV1 infected cells. In mouse model of ovalbuim-induced allergy/asthma, administration of BMS-509744 suppressed the production of IL-2 and significantly diminished lung inflammation by inhibiting ITK activity.
CAS No.
439575-02-7
Molecular Weight
623.83
Purity
0.98
Storage
Store at -20°C
Synonyms
BMS 509744; BMS509744
Targets
Itk
IC50
19 nM
Molecular Formula
C32H41N5O4S2
Chemical Name
N-[5-[5-(4-acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenyl]sulfanyl-1,3-thiazol-2-yl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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