Molecular Formula | C16H19N5 |
Molar Mass | 281.36 |
Melting Point | 205-207°C |
Solubility | DMSO: >20mg/mL |
Appearance | powder |
Color | white to off-white |
Storage Condition | room temp |
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. |
MDL | MFCD01076570 |
Use | PP1 |
In vitro study | PP1 is a nanomolar Lck and FynT inhibitor that acts on T cells and inhibits protein-tyrosine kinase activity induced by anti-CD3 with an IC50 of 0.5 μm, the selectivity for Lck and FynT was higher than that of ZAP-70, and compared with the T cell proliferation induced by non-T cell-dependent 12-myristic acid -13-acetate/IL-2, PP1 preferentially inhibited T-cell receptor-dependent anti-CD3-induced T-cell proliferation (IC50 0.5 μm). PP1 (1 μm) selectively inhibited the induction of IL-2 genes, but did not inhibit granulocyte-macrophage colony-stimulating factor or IL-2 receptor genes. PP1 also inhibited Src(IC50 of 170 nM) and Hck(IC50 of 20 nM). PP1 inhibits A- 431 epidermal growth factor receptor autophosphorylation (IC50 of 0.25 μm) 50-100 times less effectively. PP1 also inhibited Kit and Bcr-Abl tyrosine kinase with an IC50 of ∼ 75 nM and 1 μm, respectively. PP1 completely abolished M07e cell proliferation in response to SCF with an IC50 of 0.5-1 μm. PP1 (1 μm) acts on intact cells, inhibiting SCF-induced autophosphorylation by c-Kit, and inhibiting activation of MAPK and Akt. PP1 inhibits the activity of c-Kit of The constitutively mutated activated forms found in mast cell disease (D814V and D814Y), acts on the rat basophilic leukemia cell line c-Kit expressing mutant RBL-2H3, and triggers apoptosis. PP1 acts on FDCP1 cells expressing Bcr-Abl, reduces signal transduction and activation of transcription factor 5 and MAPK, and promotes apoptosis. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.554 ml | 17.771 ml | 35.542 ml |
5 mM | 0.711 ml | 3.554 ml | 7.108 ml |
10 mM | 0.355 ml | 1.777 ml | 3.554 ml |
5 mM | 0.071 ml | 0.355 ml | 0.711 ml |
biological activity | PP1 (AGL 1872, EI 275) is a potent Src selective inhibitor, the IC50 for Lck/Fyn was 5 nM/6 nM. |
Target | TargetValue LCK (Cell-free assay) 5 nM Fyn (Cell-free assay) 6 nM Kit (Cell-free assay) ~ 75 nM EGFR (Cell-free assay) 250 nM |
Target | Value |
LCK (Cell-free assay) | 5 nM |
Fyn (Cell-free assay) | 6 nM |
Kit (Cell-free assay) | ~75 nM |
EGFR (Cell-free assay) | 250 nM |
in vitro study | PP1 is a nanomolar Lck and FynT inhibitor that acts on T cells, inhibition of protein-tyrosine kinase activity induced by anti-CD3, IC50 was 0.5 μm, and the selectivity of Lck and FynT was higher than that of ZAP-70, and compared with the T cell proliferation induced by the non-T cell-dependent 12-myristic acid -13-acetic acid phorbol alcohol/IL-2, PP1 preferentially inhibited T-cell receptor-dependent anti-CD3-induced T-cell proliferation (IC50 0.5 μm). PP1 (1 μm) selectively inhibited the induction of IL-2 genes, but did not inhibit granulocyte-macrophage colony-stimulating factor or IL-2 receptor genes. PP1 also inhibited Src(IC50 of 170 nM) and Hck(IC50 of 20 nM). PP1 inhibits A- 431 epidermal growth factor receptor autophosphorylation (IC50 of 0.25 μm) 50-100 times less effectively. PP1 also inhibited Kit and Bcr-Abl tyrosine kinase with an IC50 of ∼ 75 nM and 1 μm, respectively. PP1 completely abolished M07e cell proliferation in response to SCF with an IC50 of 0.5-1 μm. PP1 (1 μm) acts on intact cells, inhibiting SCF-induced autophosphorylation by c-Kit, and inhibiting activation of MAPK and Akt. PP1 inhibits the activity of c-Kit of The constitutively mutated activated forms found in mast cell disease (D814V and D814Y), acts on the rat basophilic leukemia cell line c-Kit expressing mutant RBL-2H3, and triggers apoptosis. PP1 acts on FDCP1 cells expressing Bcr-Abl, reduces signal transduction and activation of transcription factor 5 and MAPK, and promotes apoptosis. |