1-NM-PP1
Based on 7 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 98.93%
- CAS No.: 221244-14-0
- Formula: C20H21N5
- Molecular Weight:331.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) 1-NM-PP1
More- Amyloid. 2019 Mar;26(1):24-33. [Abstract]
- Cell Rep. 2024 Mar 5;43(3):113905. [Abstract]
- Cell Biosci. 2021 May 21;11(1):93. [Abstract]
- Int J Parasitol. 2016 Jul;46(8):479-83. [Abstract]
- Life Sci Alliance. 2024 Jun 17;7(9):e202302562. [Abstract]
- bioRxiv. 2023 Dec 19.
- Friedrich-Alexander University Erlangen-Nuremberg. 2022 May.
Biological Activity
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)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | IC50 |
23 μM
Compound: 1-NM-PP1
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Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| HCT-116 | IC50 |
>100 μM
Compound: 1-NM-PP1
|
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| HFF | EC50 |
1.31 μM
Compound: 6
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Antiparasitic activity against wild type tachyzoites of Toxoplasma gondii RH type 1 infected in HFF cells incubated for 20 mins prior to inoculation followed by compound washout at 4 hrs measured after 72 hrs by beta-galactoside reporter assay
Antiparasitic activity against wild type tachyzoites of Toxoplasma gondii RH type 1 infected in HFF cells incubated for 20 mins prior to inoculation followed by compound washout at 4 hrs measured after 72 hrs by beta-galactoside reporter assay
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[PMID: 23470217] |
| HL-60 | IC50 |
24.1 μM
Compound: 1-NM-PP1
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Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| K562 | IC50 |
>36.3 μM
Compound: 1-NM-PP1
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Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| LN-229 | IC50 |
>100 μM
Compound: 1-NM-PP1
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Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| NCI-H460 | IC50 |
>100 μM
Compound: 1-NM-PP1
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Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| Z-138 | IC50 |
>23.7 μM
Compound: 1-NM-PP1
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Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
Cdk7 from Cdk7as/as 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 Cdk7as/as also rendered growth of HCT116 cells sensitive to 1-NM-PP1. In the absence of 1-NM-PP1, the wild-type andCdk7as/as 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 Cdk7as/as 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 Cdk7as/as 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 Cdk7as/as 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[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 221244-14-0
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Appearance Solid
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Molecular Weight 331.41
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Formula C20H21N5
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Color White to off-white
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SMILES
CC(N1N=C(CC2=CC=CC3=C2C=CC=C3)C4=C(N)N=CN=C41)(C)C
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Synonyms
PP1 Analog II
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Amyloid
2019 Mar;26(1):24-33. PMID: 30739503 -
Cell Rep
NRG1-ErbB4 signaling in the medial amygdala controls mating motivation in adult male mice. [Abstract]2024 Mar 5;43(3):113905. PMID: 38446660 -
Cell Biosci
The ketogenic diet increases Neuregulin 1 expression via elevating histone acetylation and its anti-seizure effect requires ErbB4 kinase activity. [Abstract]2021 May 21;11(1):93. PMID: 34020711 -
Int J Parasitol
2016 Jul;46(8):479-83. PMID: 27018127 -
Life Sci Alliance
Congress of multiple dimers is needed for cross-phosphorylation of IRE1α and its RNase activity. [Abstract]2024 Jun 17;7(9):e202302562. PMID: 38886017 -
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Solvent & Solubility
DMSO : 27.5 mg/mL (82.98 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Immunoblotting and immunoprecipitation, and kinase assays of immune complexes, are carried out. To measure Cdk1/cyclin B assembly, extracts (200 μg total protein) from cells in mitosis or G2 are pre-incubated with 2 μM 1-NM-PP1 or DMSO, then added 500 ng purified cyclin B1, amino-terminally tagged with hexahistidine and the Myc epitope, and an ATP-regenerating system. Where indicated, incubations are supplemented with 400 ng purified Csk1 or 600 ng wild-type or analog-sensitive, T-loop-phosphorylated Cdk7/cyclin H/Mat1 complex. After 90 min at room temperature, Myc-cyclin B and associated proteins are immunoprecipitated with anti-Myc antibodies and immune complexes are subjected to immunoblotting, with anti-Myc and anti-Cdk1 antibodies, and tested for histone H1 kinase activity[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Wild-type or Cdk7as/as HCT116 cells are synchronized by incubation in serum-free medium for 48 h and released into medium containing 10% fetal calf serum. Synchronization with thymidine or nocodazole, and analysis of cell-cycle distribution by flow cytometry, are performed. Cell viability is measured by MTT assay[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (289 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[2]. Bishop AC, et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21;407(6802):395-401. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0174 mL | 15.0871 mL | 30.1741 mL | 75.4353 mL |
| 5 mM | 0.6035 mL | 3.0174 mL | 6.0348 mL | 15.0871 mL | |
| 10 mM | 0.3017 mL | 1.5087 mL | 3.0174 mL | 7.5435 mL | |
| 15 mM | 0.2012 mL | 1.0058 mL | 2.0116 mL | 5.0290 mL | |
| 20 mM | 0.1509 mL | 0.7544 mL | 1.5087 mL | 3.7718 mL | |
| 25 mM | 0.1207 mL | 0.6035 mL | 1.2070 mL | 3.0174 mL | |
| 30 mM | 0.1006 mL | 0.5029 mL | 1.0058 mL | 2.5145 mL | |
| 40 mM | 0.0754 mL | 0.3772 mL | 0.7544 mL | 1.8859 mL | |
| 50 mM | 0.0603 mL | 0.3017 mL | 0.6035 mL | 1.5087 mL | |
| 60 mM | 0.0503 mL | 0.2515 mL | 0.5029 mL | 1.2573 mL | |
| 80 mM | 0.0377 mL | 0.1886 mL | 0.3772 mL | 0.9429 mL |
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