3MB-PP1

• CAT Number: R008559
• CAS Number: 956025-83-5
• Molecular Formula: C17H21N5
• Molecular Weight: 295.39
• Purity: ≥95%
• Target: PLK
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• IUPAC Name: 1-tert-butyl-3-[(3-methylphenyl)methyl]pyrazolo[3,4-d]pyrimidin-4-amine
• InChI: 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)
• InChIKey: FYCOTGCSHZKHPR-UHFFFAOYSA-N
• SMILES: CC1=CC(=CC=C1)CC2=NN(C3=C2C(=NC=N3)N)C(C)(C)C

3MB-PP1(cas 956025-83-5) is a highly potent and uniquely specific tyrosine kinase inhibitor of a rationally engineered v-Src tyrosine kinase. At 10 μM, it can block mitotic progression in cells expressing analog-sensitive Plk1 alleles and has been used to selectively sensitize Plk1 to small-molecule inhibitors.

Reference

1. Cell Cycle. 2011 Oct 15;10(20):3527-32. doi: 10.4161/cc.10.20.17792. Epub 2011
Oct 15.

Generation of a set of conditional analog-sensitive alleles of essential protein
kinases in the fission yeast Schizosaccharomyces pombe.

Cipak L(1), Zhang C, Kovacikova I, Rumpf C, Miadokova E, Shokat KM, Gregan J.

Author information:
(1)Max F Perutz Laboratories, University of Vienna, Vienna, Austria.

The genome of the fission yeast Schizosaccharomyces pombe encodes for 17 protein
kinases that are essential for viability. Studies of the essential kinases often
require the use of mutant strains carrying conditional alleles. To inactivate
these kinases conditionally, we applied a recently developed chemical genetic
strategy. The mutation of a single residue in the ATP-binding pocket confers
sensitivity to small-molecule inhibitors, allowing for specific inactivation of
the modified kinase. Using this approach, we constructed conditional
analog-sensitive alleles of 13 essential protein kinases in the fission yeast S.
pombe.