PhiKan 083

SKU: orb1220056

Description

PhiKan 083 is a carbazole derivative PhiKan 083 reduces the cell viability of engineered variants of Ln229 cells, in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W).

Key Properties

• CAS Number: 880813-36-5
• MW: 238.33
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₈N₂
• SMILES: CCN1C2=CC=CC=C2C2=C1C=CC(CNC)=C2
• Target: MDM2-p53
• Solubility: DMSO:115 mg/mL (482.52 mM; Need ultrasonic); Ethanol:100 mg/mL (419.59 mM; Need ultrasonic)

Bioactivity

• In Vitro:
  PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM, shows a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells. PhiKan 083 slows down its thermal denaturation rate. PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells. PhiKan 083 (100 μM) in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W). Cell Viability Assay Cell line: Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells. Concentration: 125 μM. Incubation time: 48 hours. Result: Caused ~70 ± 5% reduction in cell viability of variants of Ln229 cells.

Storage & Handling

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

Quick Database Links

Gene Symbol

MDM2-p53