1-NM-PP1|221244-14-0|(PP1 Analog II)-陌孚医药/Medlife

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1-NM-PP1 (Synonyms: PP1 Analog II)

目录号: PC16089 纯度: ≥98%

CAS No. :221244-14-0

商品编号	规格	价格	会员价
PC16089-5mg	5mg	¥911.40	请登录
PC16089-10mg	10mg	¥1440.60	请登录
PC16089-25mg	25mg	¥2469.60	请登录
PC16089-50mg	50mg	¥5017.60	请登录
PC16089-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥950.60	请登录

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中文名称

1-NM-PP1

中文别名

4-氨基-1-叔丁基-3-(1’-萘甲基)吡唑[3,4-d]嘧啶;4-氨基-1-叔丁基-3-(1-萘甲基)吡唑并[3,4-d]嘧啶;4-氨基1-叔丁基-3-(1'-萘甲基)吡唑并[3,4-D]嘧啶

英文名称

1-Tert-butyl-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

英文别名

1H-Pyrazolo[3,4-d]pyrimidin-4-amine,1-(1,1-dimethylethyl)-3-(1-naphthalenylmethyl)-;4-Amino-1-tert-butyl-3-(1’-naphthylmethyl)pyrazolo[3,4-d]pyrimidine;1NM-PP1(PP1 Analog II);1-(tert-butyl)-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine;1-NM-PP1;1NM-PP1;1-tert-Butyl-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-D]pyrimidin-4-amine;1-tert-butyl-3-(naphthalen-1-ylmethyl)pyrazolo[3,4-d]pyrimidin-4-amine;4-AMino-1-tert-butyl-3-(1'-naphthylMethyl)pyrazolo[3,4-d]pyriMidine;PP1 Analog II, 1NM-PP1;1-(1,1-dimethylethyl)-3-(1-naphthalenylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine;Mutant Kinases Inhibitor II;PP1 Analog II;1 NM-PP1;NM-PP1;MMV676599;C20H21N5;1-tert-but

Cas No.

221244-14-0

分子式

C₂₀H₂₁N₅

分子量

331.41

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

1-NM-PP1, a cell-permeable PP1 analog, is a potent Src family kinases inhibitor with IC₅₀s of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 4.3 nM (v-Src-as1), 3.2 nM (c-Fyn-as1), 28 μM (v-Src), 1 μM (c-Fyn), 3.4 μM (c-Abl), 29 μM (CDK2), 24 μM (CAMKII), 120 nM (cAbl-as2), 5 nM (CDK2-as1), 8 nM (CAMKII-as1)

体外研究(In Vitro)

Cdk7 from Cdk7 or Cdk7 cells is immunoprecipitated and tested its kinase activity towards both a Pol II CTD-containing fusion protein (GST-CTD) and human Cdk2. Cdk7 recovered from the mutant, but not the wild-type, cells is inhibited by 1-NM-PP1 (1-NMPP1), with an IC₅₀ of ~50 nM with either substrate. Replacement of wild-type Cdk7 with Cdk7 also rendered growth of HCT116 cells sensitive to 1-NM-PP1. In the absence of 1-NM-PP1, the wild-type andCdk7 cells had population doubling times of ~17.9 and ~20.2 h, respectively, with similar cell-cycle distributions in asynchronous culture, indicating minimal impairment of Cdk7 function by the F91G mutation per se. The homozygous Cdk7 cells are sensitive to 1-NM-PP1, however, with an IC₅₀ ~100 nM measured by cell viability (MTT) assays performed after 96 h of 1-NM-PP1 exposure. In contrast, wild-type HCT116 cells are resistant to 10 μM 1-NM-PP1. Addition of 10 μM 1-NM-PP1 retards G1/S progression by the mutant but not the wild-type cells. When added simultaneously with serum to the Cdk7 cells, 1-NM-PP1 prevents any progression into S phase in the next 15 h. After 24 h, there is evidence of progression into S-phase by a fraction of Cdk7 cells released from serum starvation directly into medium containing 1-NM-PP1, while a fraction remained in G1. The addition of 1-NM-PP1 3 h or 6 h after serum addition delays S-phase entry by ~7 h or by ~3 h, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Bishop A C, et al. Generation of Monospecific Nanomolar Tyrosine Kinase Inhibitors via a Chemical Genetic Approach. Journal of the American Chemical Society, 1999, 121(4):627-631.

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

[3]. Larochelle S, et al. Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells. Mol Cell. 2007 Mar 23;25(6):839-50. [Information]

溶解度数据

体外研究:

DMSO : 27.5 mg/mL (82.98 mM; Need ultrasonic and warming)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0174 mL	15.0871 mL	30.1741 mL
5 mM	0.6035 mL	3.0174 mL	6.0348 mL
10 mM	0.3017 mL	1.5087 mL	3.0174 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.54 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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