Lck Inhibitor - CAS 847950-09-8
Catalog number: 847950-09-8
Category: Inhibitor
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Lck Inhibitor is a small-molecule inhibitor. It takes participate in the T-cell receptor (TCR) signal transduction and affects the expression of genes associated with cell proliferation, cytokine release and T-cell survival. It has been designed and developed as therapeutic agents for the treatment for T-cell-mediated autoimmune and organ transplant rejection. It showed high selectivity against Lck over another Src family kinase Src and the kinases. It also showed more than 1000-fold greater selectivity over CDK, MAPK and the RSK family.
TC-S 7003; TC S 7003; TCS 7003; TC-S-7003; TCS7003; TCS-7003;
Canonical SMILES:
1.Co-targeting of Akt and Myc inhibits viability of lymphoma cells from Lck-Dlx5 mice.
Tan Y1, Sementino E, Pei J, Kadariya Y, Ito TK, Testa JR. Cancer Biol Ther. 2015;16(4):580-8. doi: 10.1080/15384047.2015.1018495. Epub 2015 Mar 20.
Constitutive activation of AKT is a frequent occurrence in the development of human T-cell acute lymphocytic leukemia/lymphomas (T-ALLs), due largely to inactivation of PTEN. Up regulation of MYC is also commonly observed in human T-ALLs. We previously demonstrated that expression of a constitutively active form of Lck-Akt2 alone is sufficient to initiate T-cell lymphoma in mice, and that tumor formation typically requires up regulation of Myc or Dlx5 caused by specific chromosomal rearrangements. Furthermore, Lck-Dlx5 mice develop T-ALLs that consistently acquire overexpression of Myc and activation of Akt, the latter due to loss of Pten expression. Proliferation of T-ALL cells from Lck-Dlx5 mice was found to be highly sensitive to the Akt pathway inhibitors BEZ235 and RAD001, as well as to JQ1, an inhibitor of bromodomain proteins, one of which (BRD4) regulates Myc transcription. Additionally, low concentrations of BEZ235 were found to cooperate with JQ1 to enhance cell cycle arrest.
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CAS 847950-09-8 Lck Inhibitor

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