Home>>Signaling Pathways>> Tyrosine Kinase>> Src>>1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride)
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) 目录号 GC34119

1-NaphthylPP1(1-NA-PP1)盐酸盐是src家族抑制剂,对v-Src,c-Fyn,c-Abl,CDK2和CAMKII的IC50分别为1.0,0.6,0.6,18和22μM。

规格 价格 库存 购买数量
10mM*1mLinDMSO
¥811.00
现货
5mg
¥736.00
现货
10mg
¥1,296.00
现货
50mg
¥5,213.00
现货
100mg
¥8,836.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 956025-47-1 SDF Download SDF
别名 N/A
化学名 N/A
Canonical SMILES CC(N1N=C(C2=C3C=CC=CC3=CC=C2)C4=C(N)N=CN=C41)(C)C.[H]Cl
分子式 C19H20ClN5 分子量 353.85
溶解度 DMSO : ≥ 73 mg/mL (206.30 mM) 储存条件 Store at -20°C
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
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产品描述

1-Naphthyl PP1(1-NA-PP1) hydrochloride 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].

[1]. 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. [2]. Bishop AC, et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21;407(6802):395-401.