| Identification | Back Directory | [Name]
PP1 | [CAS]
172889-26-8 | [Synonyms]
PP1
EI 275
AGL 1872
PP1 Base
AGL 1872,EI 275
Src Inhibitor, PP1
PP1 (Src Inhibitor)
PP 1 (enzyme inhibitor)
1-tert-butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine
4-Amino-5-(methylphenyl)-7-(t-butyl)pyrazolo-(3,4-d)pyrimidine
4-AMINO-5-(4-METHYLPHENYL)-7-(T-BUTYL)PYRAZOLO[3,4-D]PYRIMIDINE
4-Amino-1-tert-butyl-3-(4-methylphenyl)pyrazolo[3,4-d]pyrimidine
4-AMINO-5-(4-METHYLPHENYL)-7-(TERT-BUTYL)PYRAZOLO[3,4-D]PYRIMIDINE
1-(TERT-BUTYL)-3-(4-METHYLPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE
7-tert-Butyl-5-p-tolyl-6,7-dihydro-5H-pyrazolo[3,4-d]pyrimidin-4-amine
1-(TERT-BUTYL)-3-(4-METHYLPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE
1-(1,1-DIMETHYLETHYL)-1-(4-METHYLPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE
1-(1,1-Dimethylethyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-(1,1-dimethylethyl)-3-(4-methylphenyl)- | [Molecular Formula]
C16H19N5 | [MDL Number]
MFCD01076570 | [MOL File]
172889-26-8.mol | [Molecular Weight]
281.36 |
| Chemical Properties | Back Directory | [Appearance]
Off-White to Grey Solid | [Melting point ]
205-207°C | [storage temp. ]
Desiccate at +4°C | [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. |
| Hazard Information | Back Directory | [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 | [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. | [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. | [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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