EN4 MYC inhibitor

SKU: orb1219043

Description

EN4 MYC inhibitor is a covalent ligand that targets cysteine 171 (C171) of MYC. It is selective for c-MYC over N-MYC and L-MYC, and inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

Research Area

Pharmacology & Drug Discovery; Cell Biology

Key Properties

• CAS Number: 1197824-15-9
• MW: 416.47
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₄N₂O₄
• SMILES: CCOC1=CC=C(C=C1)OC2=CC=CC=C2NC(=O)C3=CC=C(C=C3)CNC(=O)C=C
• Target: c-Myc
• Solubility: DMSO:250 mg/mL (600.28 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Animal model: SCID mice injected with 231MFP breast cancer cells. Dosage: 50 mg/kg. Administration: Intraperitoneal injection; daily; for 3 weeks. Result: Significantly attenuated tumor growth In vivo.
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• In Vitro:
  Cell Proliferation Assay Cell line: 231MFP breast cancer cells. Concentration: 1 μM, 10 μM, 50 μM. Incubation time: 72 hours. Result: Significantly impaired 231MFP breast cancer cell proliferation in a dose-dependent manner. Western blot analysis. Cell line: 231MFP breast cancer cells. Concentration: 50 μM. Incubation time: 60 hours. Result: The protein levels of CDK2 and CDC25A were significantly lowered.
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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

EN4

Quick Database Links

Gene Symbol

c-Myc