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关于此项目
经验公式(希尔记法):
C17H21N5
化学文摘社编号:
分子量:
295.38
MDL number:
UNSPSC Code:
12352202
NACRES:
NA.77
产品名称
PP1 Analog III, 3-MB-PP1, PP1 Analog III, 3-MB-PP1 primarily used in Inhibition.
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
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
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
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.
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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