172889-26-8 Usage
Description
PP1 (172889-26-8) is a potent and selective inhibitor of Src family tyrosine kinases. IC50=5 nM (p65lck), IC50=6 nM(P59fynT), IC50=170 nM (p60src). Cell permeable.
Chemical Properties
Off-White to Grey Solid
Uses
Different sources of media describe the Uses of 172889-26-8 differently. You can refer to the following data:
1. A highly potent and uniquely specific tyrosine kinase inhibitor of a rationally engineered v-Src tyrosine kinase
2. PP1 has been used as: an inhibitor of sarcoma (Src) family kinases (SFK) like hematopoietic cell kinase (hck) and fyn a selective Src tyrosine kinase inhibitor in hippocampal neuronal cultures to test its effect on neurite growth a Src-kinase blocker to test its effect on brimonidine (BMD)-induced phosphorylation in extracellular signal-activated kinases(ERK1/2)
Biological Activity
Potent inhibitor of Src-family tyrosine kinases. Inhibits p56 lck and p59 fynT (IC 50 values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over ZAP-70 and JAK2. Also moderately inhibits p38, CSK, PDGF receptors, RET-derived oncoproteins, c-Kit and Bcr-Abl.
Biochem/physiol Actions
PP1 is a pyrazolopyrimidine compound that acts as a competitive inhibitor of adenosine triphosphate (ATP) binding. It also inhibits protein tyrosine kinase (PTK6) and may be useful in the therapeutic management of PTK6 positive based breast cancer malignancy.
in vitro
it was reported that pp1 specifically inhibited the expression and activity of lyn, a src family kinase, in rbl-2h3 cells. based on the immune-complex kinase assays in vitro, pp1 suppressed the activity of lyn at nanomolar levels without any effect on syk kinase activity. in contrast, phosphorylation of both syk and lyn kinases were both blocked in rbl cells. fcεri- and thy-1-mediated early and late activation events were also interrupted by pp1 in a similar mannar. moreover, pp1 was found to inhibited ret-derived oncoproteins with ic50 of 80 nm. ret/ptc3-transformed cells received pp1 treatment with a dose of 5 μm lost proliferative autonomy and showed morphological reversion. [2, 3]
in vivo
under in vivo conditions pp1 was suggested to suppress tyrosine phosphorylation and proliferation in t cells stimulated with anti-cd3 and mitogen. studies using mice tumor model also showed that pp1 upregulated the expression of the il-2 gene rather than the granulocyte macrophage colony-stimulating factor or the il-2 receptor genes. based on these, pp1 could be adopted as a useful agent to investigate the role of lck and fyn t cell activation. [2]
IC 50
a potent and selective inhibitor of src-family tyrosine kinases, with an ic50 of 5 and 6 nm respectively for p56lck and p59fynt.
References
1) Hanke et al. (1996), Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation; J. Biol. Chem., 271 695
Check Digit Verification of cas no
The CAS Registry Mumber 172889-26-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,2,8,8 and 9 respectively; the second part has 2 digits, 2 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 172889-26:
(8*1)+(7*7)+(6*2)+(5*8)+(4*8)+(3*9)+(2*2)+(1*6)=178
178 % 10 = 8
So 172889-26-8 is a valid CAS Registry Number.
InChI:InChI=1/C16H19N5/c1-10-5-7-11(8-6-10)13-12-14(17)18-9-19-15(12)21(20-13)16(2,3)4/h5-9H,1-4H3,(H2,17,18,19)
172889-26-8Relevant articles and documents
Microwave-assisted synthesis of N1- and C3-substituted pyrazolo[3,4-d] pyrimidine libraries
Todorovic, Nick,Awuah, Emelia,Shakya, Tushar,Wright, Gerard D.,Capretta, Alfredo
, p. 5761 - 5763 (2011/12/03)
The parallel synthesis of a library N1- and C3-substituted-pyrazolo[3,4-d] pyrimidines is described. The microwave-assisted approach involves the de novo generation of the heterocyclic scaffold, facile alkylation at N1 via either a Mitsunobu or a direct alkylation reaction and arylation at C3 via a Suzuki reaction.
Kinase antagonists
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Page/Page column 29; 30, (2008/06/13)
The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tryosine kinase, PI3Kinase and mTOR, or PI3Kinase, mTOR and tryosine kinase.
