1-Naphthyl PP1 (1-NA-PP 1) 是 src 家族激酶的选择性抑制剂。 1-Naphthyl PP1 抑制 v-Src 和 c-Fyn、c-Abl、CDK2 和 CAMK II，IC50 分别为 1.0、0.6、0.6、18 和 22 μM。
| Cas No. | 221243-82-9 |
| 别名 | 4-氨基-1-叔丁基-3-(1'-萘基)吡唑并[3,4-D]嘧啶,1-NA-PP 1 |
| 化学名 | 1-tert-butyl-3-naphthalen-1-ylpyrazolo[3,4-d]pyrimidin-4-amine |
| Canonical SMILES | CC(C)(C)N1C2=C(C(=N1)C3=CC=CC4=CC=CC=C43)C(=NC=N2)N |
| 分子式 | C19H19N5 |
| 分子量 | 317.39 |
| 溶解度 | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:5): 0.15 mg/ml,DMSO: 1 mg/ml,Ethanol: 2 mg/ml |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).IC50 Value:1.0 uM (v-Src); 0.6 uM (c-Fyn); 18 uM (c-Abl) [1]Target: Src Family kinase1-NA-PP1 was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. 1-NA-PP1 was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Overexpression of PKD1 or PKD3 almost completely reversed the growth arrest and the inhibition of tumor cell invasion caused by 1-NA-PP1, indicating that its anti-proliferative and anti-invasive activities were mediated through the inhibition of PKD. Interestingly, a 12-fold increase in sensitivity to 1-NA-PP1 could be achieved by engineering a gatekeeper mutation in the active site of PKD1, suggesting that 1-NA-PP1 could be paired with the analog-sensitive PKD1(M659G) for dissecting PKD-specific functions and signaling pathways in various biological systems [2]. References:
[1]. Bishop AC, et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21;407(6802):395-401.
[2]. Tandon M, et al. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells. PLoS One. 2013 Sep 23;8(9):e75601. |
