1-NM-PP1
This product is for research use only, not for human use. We do not sell to patients.
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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.
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Molecular Weight (MW) | 331.41 |
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Molecular Formula | C20H21N5 |
CAS No. | 221244-14-0 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
SMILES Code | NC1=C2C(N(C(C)(C)C)N=C2CC3=C4C=CC=CC4=CC=C3)=NC=N1 |
Synonyms | 1NM-PP1; 1NM PP1; 1NMPP1l PP1 analog II |
Protocol | In Vitro | 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. |
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These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 3.0174 mL | 15.0871 mL | 30.1741 mL | 60.3482 mL |
5mM | 0.6035 mL | 3.0174 mL | 6.0348 mL | 12.0696 mL |
10mM | 0.3017 mL | 1.5087 mL | 3.0174 mL | 6.0348 mL |
20mM | 0.1509 mL | 0.7544 mL | 1.5087 mL | 3.0174 mL |
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Method for preparing in vivo formulation:
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