Molecular structure of Lck Inhibitor, CAS Number: 213743-31-8
Lck Inhibitor Inhibitor (CAS 213743-31-8)
See product citations (5)
Alternate Names:
7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine
Application:
Lck Inhibitor is A cell-permeable ATP-competitive inhibitor of Lck
CAS Number:
213743-31-8
Purity:
≥95%
Molecular Weight:
370.45
Molecular Formula:
C23H22N4O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Lck Inhibitor is a cell-permeable pyrrolopyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of Lck (IC50 at 5 muM ATP = < 1 nM, 2 nM, 70 nM, 1.57 muM and 1.98 muM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively IC50 at 1 mM ATP = 16 muM, 66 nM, 126 nM, 420 nM and 5.18 muM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC50 = 3.2 muM, > 33 muM, > 50 muM and > 50 muM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC50 < 1-40 nM in Jurkat T cells).
Lck Inhibitor Inhibitor (CAS 213743-31-8) References
- Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. | DiMauro, EF., et al. 2006. J Med Chem. 49: 5671-86. PMID: 16970394
- Discovery of thienopyridines as Src-family selective Lck inhibitors. | Abbott, L., et al. 2007. Bioorg Med Chem Lett. 17: 1167-71. PMID: 17234410
- Small molecule inhibitors of Lck: the search for specificity within a kinase family. | Meyn, MA. and Smithgall, TE. 2008. Mini Rev Med Chem. 8: 628-37. PMID: 18537718
- SVM model for virtual screening of Lck inhibitors. | Liew, CY., et al. 2009. J Chem Inf Model. 49: 877-85. PMID: 19267483
- Inhibition of Lck enhances glucocorticoid sensitivity and apoptosis in lymphoid cell lines and in chronic lymphocytic leukemia. | Harr, MW., et al. 2010. Cell Death Differ. 17: 1381-91. PMID: 20300113
- Update on lymphocyte specific kinase inhibitors: a patent survey. | Martin, MW. and Machacek, MR. 2010. Expert Opin Ther Pat. 20: 1573-93. PMID: 20831362
- An immunosuppressive antibody-drug conjugate. | Wang, RE., et al. 2015. J Am Chem Soc. 137: 3229-32. PMID: 25699419
- Glucocorticoid resistance is reverted by LCK inhibition in pediatric T-cell acute lymphoblastic leukemia. | Serafin, V., et al. 2017. Blood. 130: 2750-2761. PMID: 29101238
- Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. | Farag, AK., et al. 2017. Eur J Med Chem. 141: 657-675. PMID: 29107425
- Exploration of the therapeutic aspects of Lck: A kinase target in inflammatory mediated pathological conditions. | Kumar Singh, P., et al. 2018. Biomed Pharmacother. 108: 1565-1571. PMID: 30372858
- LCK inhibitor attenuates atherosclerosis in ApoE-/- mice via regulating T cell differentiation and reverse cholesterol transport. | Liu, J., et al. 2020. J Mol Cell Cardiol. 139: 87-97. PMID: 31972265
- Pretreatment with LCK inhibitors chemosensitizes cisplatin-resistant endometrioid ovarian tumors. | Crean-Tate, KK., et al. 2021. J Ovarian Res. 14: 55. PMID: 33888137
- New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011-2021) focussing on structure-activity relationship (SAR) and docking insights. | Elkamhawy, A., et al. 2021. J Enzyme Inhib Med Chem. 36: 1574-1602. PMID: 34233563
- Lck signaling inhibition causes improvement in clinical features of psoriatic inflammation through reduction in inflammatory cytokines in CD4+ T cells in imiquimod mouse model. | Al-Harbi, NO., et al. 2022. Cell Immunol. 376: 104531. PMID: 35576719
Inhibitor of:
Blk, Csk, E74 like ETS transcription factor (ELF), Fyn, LAIR-1, Lck, Lyn, SLA, and Tyrosine Kinase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Lck Inhibitor, 1 mg | sc-204052 | 1 mg | $362.00 |