PTC-028

SKU: orb1307835

Description

PTC-028

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 1782970-28-8
• MW: 405.32
• Purity: 98.25%
• Formula: C₁₉H₁₂F₅N₅
• SMILES: Cc1nc2cc(F)c(F)cc2n1-c1cncc(Nc2ccc(cc2)C(F)(F)F)n1
• Target: Apoptosis,BMI-1
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.87 mM);DMSO:125 mg/mL (308.4 mM)

Bioactivity

• In Vivo:
  PTC-028 (10 mg/kg or 20mg/kg; single oral doses) is administrated to the CD-1 mice. The Cmax is reached at both dose levels 1h post-dose after which plasma concentrations slowly decrease. PTC-028 (15 mg/kg; administered orally twice weekly) induces ~94% (0.169 g) reduction in tumor weight compared to the control (average tumor weight, ~3g) .
• In Vitro:
  PTC-028 subsequently decreases BMI-1 in the biochemical functional readout. PTC-028 (100 nM; 2-12 hours) increases the phosphorylated BMI-1 species in a time-dependent manner. uH2A is observed up to 12 h with PTC-028 (100 nM) in both CP20 and OV90 cells while total H2A levels remain unchanged. PTC-028 (100 nM; 48 hours) decreases the expression of XIAP and RIPK1 while LC3B levels remain unchanged compared to that of the control. PTC-028 (25-500 nM; 48 hours) obviously reduces CP20, OVCAR4, and OV90 epithelial ovarian cancer cell viability. However, in normal ovarian surface epithelial cells (OSE) and fallopian tube epithelial cells (FTE) cells, up to 500 nM treatment with PTC-028 for 48 hours has a minimal effect (~18-30% decrease). Significant cleavage of Caspase 7, Caspase 9, and PARP is observed in PTC-028 (100 nM; 48 hours).

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

PTC028, PTC-028, PTC 028, Apoptosis, BMI1, BMI-1, inhibit, Inhibitor

Compound Identifiers

PubChem CID

73427235