1-NM-PP1

This product is for research use only, not for human use. We do not sell to patients.

1-NM-PP1
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Cat #: V3628 CAS #: 221244-14-0 Purity ≥ 98%

Description: 1-NM-PP1, a C3-modified analog of PP1, is a novel, potent and cell permeable protein kinase D (PKD) inhibitor with an IC50 of 0.398 μM.

References: 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.

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Molecular Weight (MW)331.41
Molecular FormulaC20H21N5
CAS No.221244-14-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SMILES CodeNC1=C2C(N(C(C)(C)C)N=C2CC3=C4C=CC=CC4=CC=C3)=NC=N1
Synonyms1NM-PP1; 1NM PP1; 1NMPP1l PP1 analog II
ProtocolIn VitroCdk7 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM3.0174 mL15.0871 mL30.1741 mL60.3482 mL
5mM0.6035 mL3.0174 mL6.0348 mL12.0696 mL
10mM0.3017 mL1.5087 mL3.0174 mL6.0348 mL
20mM0.1509 mL0.7544 mL1.5087 mL3.0174 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.