1-NM-PP1

SKU: orb1306309

Description

1-NM-PP1

Research Area

Cardiovascular Research, Cell Biology, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 221244-14-0
• MW: 331.41
• Purity: 99.20%
• Formula: C₂₀H₂₁N₅
• SMILES: CC(C)(C)n1nc(Cc2cccc3ccccc23)c2c(N)ncnc12
• Target: CDK,Src,Serine/threonin kinase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.03 mM);DMSO:45 mg/mL (135.78 mM)

Bioactivity

• Target 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.
• Cell Research:
  1-NM-PP1 (1-NMPP1) is dissolved in DMSO and stored, and then diluted with appropriate media before use. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK7, 1NMPP1, 1-NM-PP1, 1-NM-PP-1, 1 NM PP1, 1 nM-PP1, Inhibitor, inhibit, Serinekinase, threonin kinase, threoninkinase, Serine kinase, PP1 Analog II, PKD, Src

Compound Identifiers

PubChem CID

5154691