product name WH-4-023
Description: WH-4-023 is a potent, selective and orally active Lck/Src inhibitor with IC50 of 2 nM and 6 nM in cell-free assays, respectively. The lymphocyte-specific kinase ( Lck ) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and NK cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling mediated by the T cell receptor (TCR), which leads to normal T cell development and activation.
References: J Med Chem. 2006 Aug 10;49(16):4981-91.
568.67
Formula
C32H36N6O4
CAS No.
837422-57-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 12 mg/mL (21.1 mM)
Water: <1 mg/mL
Ethanol: 6 mg/mL (10.55 mM)
Solubility (In vivo)
Synonyms
KIN001-112, KIN112
other peoduct :
| In Vitro |
In vitro activity: WH-4-023 inhibited a number of protein tyrosine kinases that possess a Thr residue at the gatekeeper site, such as FGF and Ephrin receptors, Src family members (Src, Lck, and Yes) and BTK. WH-4-023 also inhibited the SIKs and did not inhibit any other member of the AMPK-related kinase subfamily, which all possess a large hydrophobic residue (Met or Leu) at the gatekeeper site. WH-4-023 inhibited SIK 1, 2 and 3 with IC50 values of 10, 22 and 60 nM, respectively. Also, WH-4-023 increased LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2006 Aug 10;49(16):4981-91 |
