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SCFSkp2-IN-2

SKU: orb1737461

Description

SCFSkp2-IN-2 is a Skp2 inhibitor with a K_D of 28.77 μM. It induces apoptosis in non-small cell lung cancer (NSCLC) cells, demonstrating antitumor activity in vitro, and serves as a research tool for studying Skp2's role in oncology and cell cycle pathways.

Research Area

Cell Biology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number1375060-02-8
MW312.37
Purity99.86% (May vary between batches)
FormulaC17H20N4O2
SMILESN(CC)(CC)C1=CC(O)=C(/C=N/NC(=O)C=2C=CC=NC2)C=C1
TargetE1/E2/E3 Enzyme,Apoptosis
SolubilityDMSO:112.5 mg/mL (360.15 mM)

Bioactivity

Target IC50
Skp2:28.77 μM(kd)
In Vivo
SCFSkp2-IN-2 (Compound AAA-237) administered at 15 or 45 mg/kg intraperitoneally on a daily basis for 14 days demonstrated antitumor activity in an A549 lung cancer xenograft mouse model.
In Vitro
SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM; 24-72 h) binds directly to Skp2, leading to its proteasome-mediated degradation without affecting Skp2 mRNA expression but inhibiting Skp2 protein expression in a time-dependent manner in NSCLC cells. SCFSkp2-IN-2 inhibits the proliferation of A549 and H1299 cells and induces apoptosis in a dose- and time-dependent manner, blocks the cell cycle at the G0/G1 checkpoint by regulating the Skp2-Cip/Kip and PI3K/Akt-FOXO1 signaling pathways, and induces NSCLC cell senescence (0.3 μM; 1-7 days).

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

E3Enzyme, E3 Enzyme, E2 Enzyme, E2Enzyme, E1/E2/E3 Enzyme, E1 Enzyme, E1Enzyme, Apoptosis, SCFSkp2IN2, SCFSkp2-IN-2, Skp2
Quality Guarantee

Quality Guarantee

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Key Properties

No computed properties available.

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SCFSkp2-IN-2 (orb1737461)

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Available Sizes

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1 ml x 10 mM (in DMSO)
¥ 910.00
10 mg
¥ 1,040.00
25 mg
¥ 1,560.00
50 mg
¥ 2,210.00
100 mg
¥ 3,510.00
200 mg
¥ 4,810.00
DispatchUsually dispatched within 3-5 working days
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