PROTAC-O4I2

SKU: orb1983144

Description

PROTAC-O4I2 is a heterobifunctional degrader that targets the splicing factor SF3B1, inducing its degradation with an IC50 of 0.244 µM in K562 cells and triggering apoptosis. This molecule serves as a valuable chemical probe for studying RNA splicing mechanisms and cancer cell survival in leukemia research models.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2785323-62-6
• MW: 609.1
• Purity: 97.45%
• Formula: C₂₉H₂₉ClN₆O₅S
• SMILES: O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2NCCCCCCNC(=O)C=4N=C(NC5=CC=C(Cl)C=C5)SC4
• Target: PROTACs,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (8.21 mM);DMSO:200 mg/mL (328.35 mM)

Bioactivity

• In Vivo:
  Flies were fed on a round filter paper loaded with PROTAC-O4I2 (10 μM) in a 5% sucrose solution, maintained at 18℃, and flipped into a freshly prepared vial every 2 days. PROTAC-O4I2 significantly improves Drosophila survival in a Drosophila intestinal tumor model by interfering with tumor maintenance and proliferation.
• In Vitro:
  PROTAC-O4I2 introduces thalidomide into the ubiquitin E3 ligase cereblon (CRBN), thereby selectively degrading SF3B1 and inhibiting tumor growth in cells. PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 has anti-proliferative effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC50 of 228, 63, and 90 nM, respectively. PROTAC-O4I2 induces FLAG-SF3B1 degradation in a concentration-dependent manner, with a half-maximal inhibitory concentration (IC50) value of 0.244 μM in K562 cells.

Storage & Handling

• Storage: keep away from direct sunlight | 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

Apoptosis, PROTAC

Compound Identifiers

PubChem CID

162641046