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General description
A cell-permeable C3-enlarged PP1 (Cat. No. 567809 ) analog that is shown to act as a potent, ATP-competitive, and highly ASKA- (analog-sensitive kinase alleles) selective inhibitor against polo-like kinase 1C67V L130G (75% and 94% inhibition in cell-free kinase assays at 0.1 and 1 µM, respectively), ZAP-70C405V M414A/ZAP-70M414A (complete prevention and elimination, respectively, of αTCR-stimulated [Ca2+] elevation in ASKA transfectants when applied before or after αTCR stimulation at 6 µM), and SykM442A S505A (56% inhibition of phagocytosis of Ab-opsonized SRBC by ASKA macrophages at 6 µM), while exhibiting little or no activity toward the wild-type or other off-target cellular enzymes. Functional analog-sensitive allele mutants are valuable tools in pharmacological validation of drug development and in elucidating enzyme signalings and functions both in cultures in vitro and in animals in vivo when specific inhibitors against naturally occurring target enzymes are unavailable and/or generations of knockout animals/cells lacking the target enzymes appear to be difficult, infeasible, or simply impossible.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Miller, A.L., et al. 2009. J. Immunol.182, 988.
Levin, S.E., et al. 2008. J. Biol. Chem.283, 15419.
Burkard, M.E., et al. 2007. Proc. Natl. Acad. Sci. USA104, 4383.
Bishop, A.C., et al. 1999. J. Am. Chem. Soc.121, 627.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Level | 100 |
| assay | ≥97% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white |
| solubility | DMSO: 50 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | [n]1(nc(c3c1ncnc3N)Cc2cc(ccc2)C)C(C)(C)C |
| InChI | 1S/C17H21N5/c1-11-6-5-7-12(8-11)9-13-14-15(18)19-10-20-16(14)22(21-13)17(2,3)4/h5-8,10H,9H2,1-4H3,(H2,18,19,20) |
| InChI key | FYCOTGCSHZKHPR-UHFFFAOYSA-N |
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