Skp2-IN-C1

SKU: orb1225063

Description

Skp2-IN-C1 is a specific small molecule inhibitor of Skp2-mediated p27 degradation, induced p27 accumulation in a Skp2-dependent manner and promoted cell-type-specific blocks in the G1 or G2/M phases.

Key Properties

• CAS Number: 432001-69-9
• MW: 465.336
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₃BrN₂O₄S₂
• SMILES: O=C(O)COC1=CC=C(Br)C=C1/C=C(SC(N2CC3=CC=CN=C3)=S)/C2=O
• Target: E3 Ubiquitin Ligase
• Solubility: DMSO : 6.4 mg/mL 13.75 mM

Bioactivity

• In Vivo:
  Skp2 Inhibitor C1 (5 mg/kg and 10 mg/kg; 3 times within 24 h: 24, 5, and 1 h before the test) shows the antidepressant-like effect in mouse models following chronic treatment by using the tail suspension test (TST), forced swimming test (FST), and social interaction test (SIT).
• In Vitro:
  Skp2 Inhibitor C1 (10-50 μM; 12 hr) decreases the viability of THP-1, U266 and RPMI 8226 cells. Skp2 Inhibitor C1 (25 μM) increases p27 protein levels in U266 and RPMI 8226 cells by inhibiting ubiquitination. Skp2 Inhibitor C1 (25 μM) inhibits cell cycle of U266 and RPMI 8226 cells. Cell Cycle Analysis Cell line: B lymphocytes, THP-1, U266 and RPMI 8226 cells. Concentration: 0, 5, 10, 25, and 50 μM. Incubation time: 12 hr, 24 hr, 36 hr, and 48 hr. Result: Significantly decreased the viability of U266 and RPMI 8226 cells at 10 μM for 12 hours. Decreased THP-1 cell viability at 50 μM for 12 hours. Cell Viability Assay Cell line: U266 and RPMI 8226 cells. Concentration: 0, 5, 10, 25, and 50 μM. Incubation time: 12 hr. Result: Increased the percentages of U266 and RPMI 8226 cells in the G0/G1 phase, while decreased the percentages in S and G2/M phases.

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

MDK-1699 | MDK 1699 | MDK1699 | Skp2 inhibitor C1 and SKPin C1.

Quick Database Links

Gene Symbol

E3 Ubiquitin Ligase