TCS PIM-1 1

SKU: orb1224952

Description

A potent, selective, ATP-competitive Pim-1 kinase inhibitor with IC50 of 50 nM; displays >400-fold selectivity over Pim-2 and MEK1/2.

Research Area

Cell Biology

Key Properties

• CAS Number: 491871-58-0
• MW: 367.1961
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₁BrN₂O₂
• SMILES: C1=CC=C(C=C1)C2=C(C(=O)NC(=C2)C3=C(C=CC(=C3)Br)O)C#N
• Target: Pim
• Solubility: DMSO: ≥ 52 mg/mL

Bioactivity

• In Vitro:
  TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SC 204330 | TCS PIM 1-1

Quick Database Links

Gene Symbol

Pim