WH-4-023

SKU: orb1307398

Description

WH-4-023 is an orally bioavailable small molecule that acts as a potent dual inhibitor of the Lck and Src tyrosine kinases, as well as salt-inducible kinase (SIK). It is a valuable research tool for investigating T-cell signaling and immune regulation in both cellular and animal models.

Research Area

Cell Biology, Immunology & Inflammation, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 837422-57-8
• MW: 568.7
• Purity: >98%
• Formula: C₃₂H₃₆N₆O₄
• SMILES: COc1ccc(N(C(=O)Oc2c(C)cccc2C)c2ccnc(Nc3ccc(cc3)N3CCN(C)CC3)n2)c(OC)c1
• Target: Kinase
• Solubility: Soluble in DMSO (60 mg/ml)

Bioactivity

• Target IC50:
  Lck:2 nM|Src:6 nM
• In Vitro:
  WH-4-023 shows little activity on p38 and KDR.
• Cell Research:
  WH-4-023 is dissolved in DMSO and stored, and then diluted with appropriate medium before use. The purpose of this assay is to test the potency of T cell receptor (TCR; CD3) and CD28 signaling pathway inhibitors in human T cells. T cells are purified from human peripheral blood lymphocytes (hPBL) and preincubated with or without compound prior to stimulation with a combination of an anti-CD3 and an anti-CD28 antibody in 96-well tissue culture plates (1×105 T cells/well). Cells are cultured for ~20 h at 37°C in 5% CO2 and then secreted IL-2 in the supernatants is quantified by cytokine ELISA. The cells remaining in the wells are then pulsed with 3H-thymidine overnight to assess the T cell proliferative response. Cells are harvested onto glass fiber filters and 3H-thymidine incorporation into DNA is analyzed by liquid scintillation counter. For comparison purposes, phorbol myristic acid (PMA) and calcium ionophore are used in combination to induce IL-2 secretion from purified T cells. Potential inhibitor compounds are tested for inhibition of this response as described above for anti-CD3 and -CD28 antibodies. Human whole-blood anti-CD3/CD28-induced IL-2 secretion assays are run in a similar fashion as described above using whole blood from normal volunteers diluted 50% in tissue culture medium prior to stimulation.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dual LCK/SRC inhibitor, KIN 112, KIN001-112, KIN112, KIN-112, inhibit, Inhibitor, Lck, WH 4 023, WH4023, WH-4-023, Src

Compound Identifiers

PubChem CID

11844351