Home Tools

1-NM-PP1

Catalog No. T2153 CAS 221244-14-0

Synonyms: PP1 Analog II, 1 nM-PP1

1-NM-PP1 (PP1 Analog II) is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

1-NM-PP1, CAS 221244-14-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 43.00
2 mg	In stock	$ 60.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 142.00
25 mg	In stock	$ 302.00
50 mg	In stock	$ 560.00
100 mg	In stock	$ 743.00
1 mL * 10 mM (in DMSO)	In stock	$ 87.00

Bulk Inquiry

Select Batch

Purity: 99.2%

Purity: 98.93%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	1-NM-PP1 (PP1 Analog II) is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.
Targets&IC50	PKD:0.398 μM
In vitro	Cdk7 from both mutant (Cdk7as/as) and wild-type (Cdk7+/+) cells was immunoprecipitated to assess its kinase activity on a Pol II CTD-containing fusion protein (GST-CTD) and human Cdk2. Interestingly, Cdk7 extracted from mutant cells, unlike that from wild-type cells, showed susceptibility to inhibition by 1-NM-PP1 (1-NMPP1), demonstrating an inhibitory concentration 50 (IC50) of approximately 50 nM for both substrates. Moreover, mutant HCT116 cells replaced with wild-type Cdk7 became sensitive to 1-NM-PP1, affecting growth. In the absence of 1-NM-PP1, both wild-type and mutant cells exhibited similar cell-cycle distributions and population doubling times (approximately 17.9 and 20.2 hours, respectively), indicating the F91g mutation alone minimally impacts Cdk7 function. However, mutant cells, but not wild-type, exhibited sensitivity to 1-NM-PP1 with an IC50 of approximately 100 nM, as determined by cell viability (MTT) assays after prolonged (96-hour) exposure. Additionally, 10 μM of 1-NM-PP1 hindered G1/S phase progression in mutant but not wild-type cells, with immediate effects observed when 1-NM-PP1 was introduced alongside serum, halting S phase entry for 15 hours. Even after releasing the mutant cells from serum starvation into a medium with 1-NM-PP1, there was a delayed and partial progression into S phase, while a fraction remained in G1. Further experimentation revealed that introducing 1-NM-PP1 3 or 6 hours post serum addition delayed S-phase entry by approximately 7 and 3 hours, respectively.
Kinase Assay	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[1].
Cell Research	1-NM-PP1 (1-NMPP1) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. 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[1].

Synonyms	PP1 Analog II, 1 nM-PP1
Molecular Weight	331.41
Formula	C20H21N5
CAS No.	221244-14-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.5 mg/mL

References and Literature

1. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Breast Cancer Compound Library Bioactive Compound Library Anti-Cancer Metabolism Compound Library Reprogramming Compound Library Anti-Cancer Compound Library Apoptosis Compound Library Bioactive Compounds Library Max Metabolism Compound Library

Related Products

Related compounds with same targets

CRT0066101 dihydrochloride CID 2011756 BMT-124110 Formate ML-7 hydrochloride GAK inhibitor 49 IPR-803 CID755673 CRT0066101 dihydrochloride(956121-30-5 free base)

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

1-NM-PP1 221244-14-0 Angiogenesis Cell Cycle/Checkpoint Metabolism Tyrosine Kinase/Adaptors Serine/threonin kinase CDK Src inhibit Inhibitor PP1 Analog II 1-NM-PP-1 1NMPP1 1 NM PP1 1 nM-PP1 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.