PP1 Chemical Properties

Melting point:

205-207°C

storage temp. 

room temp

solubility 

DMSO: >20mg/mL

form 

powder

color 

white to off-white

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

HS Code 

2933599590

PP1 Usage And Synthesis

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

A highly potent and uniquely specific tyrosine kinase inhibitor of a rationally engineered v-Src tyrosine kinase

Uses

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.

storage

+4°C (desiccate)

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

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