Lomeguatrib

SKU: orb1305396

Description

Lomeguatrib (PaTrin-2) is a small molecule inhibitor of the DNA repair protein MGMT (O⁶-methylguanine-DNA methyltransferase). It is used in research to sensitize tumor cells to alkylating agents like temozolomide, both in vitro and in vivo, for studying chemotherapeutic resistance mechanisms.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 192441-08-0
• MW: 326.2
• Purity: >98%
• Formula: C₁₀H₈BrN₅O₃S
• SMILES: O(CC1=CC(Br)=CS1)C2=C3C(=NC(N)=N2)N=CN3
• Target: Methyltransferase
• Solubility: Soluble in DMSO (up to 10 mg/ml with warming)

Bioactivity

• Target IC50:
  MGMT:5 nM
• In Vivo:
  In Raji cells, Lomeguatrib inhibits ATase activity with an IC50 value of 10 nM, while in MCF-7 cells, it effectively inhibits MGMT with an IC50 of 6 nM.
• In Vitro:
  In the A375M human melanoma xenograft model, intraperitoneal injection of Lomeguatrib (20 mg/kg) treatment was found to inhibit ATase activity.

Storage & Handling

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

Alternative Names

O6-(4-Bromothenyl)guanine

Compound Identifiers

PubChem CID

3025944