Skp2 inhibitor 1

SKU: orb2565282

Description

This small molecule inhibitor disrupts the Skp2-Cks1 interaction with an IC50 of 2.8 µM. It is a valuable research tool for studying Skp2-dependent oncogenic pathways and has demonstrated antitumor activity in both cellular assays and in vivo cancer models.

Research Area

Pharmacology & Drug Discovery; Cell Biology

Key Properties

• CAS Number: 2760612-63-1
• MW: 406.91
• Purity: 99.45% (May vary between batches)
• Formula: C₂₃H₂₃ClN₄O
• SMILES: O=C(NC1CCN(C2=NC(C3=CC=CC=C3)=C(N=C2)C=4C=CC=CC4)CC1)CCl
• Target: Others

Bioactivity

• Target IC50:
  MGC-803 cells:7.0 μM|PC3 cells:4.8 μM
• In Vivo:
  Skp2 inhibitor 1, administered at doses of 10 mg/kg, 25 mg/kg, and 50 mg/kg via intragastric administration every two days over a 21-day period, significantly suppressed tumor growth in xenograft models of PC-3 and MGC-803 cells within NOD-SCID mice, showing no notable toxicity. A dose of 50 mg/kg (every 2 days) completely inhibited tumor growth . The compound functions by inhibiting the Skp2 signaling pathway, thereby reducing tumor malignancy and increasing apoptotic cell proportions in tumor tissues . The tumor growth inhibition ratios were 55.68%, 71.86%, and 90.42% for 10, 25, and 50 mg/kg respectively.
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• In Vitro:
  Skp2 inhibitor 1 (2.8 μM, 72 h) was able to interfere with the interaction between Skp2 and Cks1, with IC50 values of 4.8 μM and 7.0 μM for PC-3 and MGC-803 cells, respectively. At a concentration of 10 μM, after 48 h treatment, Skp2 inhibitor 1 was able to inhibit the proliferation and migration of PC-3 and MGC-803 cells, induced cell arrest in S phase, and promoted apoptosis.
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Storage & Handling

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

Alternative Names

Skp2

Compound Identifiers

PubChem CID

162718203