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SCFSkp2-IN-2, a Skp2 inhibitor, exhibits a dissociation constant (K_D) of 28.77 μM. It demonstrates antitumor activities by inducing apoptosis in non-small cell lung cancer (NSCLC) cells.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $38 | In Stock | |
25 mg | $77 | In Stock | |
50 mg | $128 | In Stock | |
100 mg | $223 | In Stock | |
200 mg | $328 | In Stock | |
1 mL x 10 mM (in DMSO) | $30 | In Stock |
Description | SCFSkp2-IN-2, a Skp2 inhibitor, exhibits a dissociation constant (K_D) of 28.77 μM. It demonstrates antitumor activities by inducing apoptosis in non-small cell lung cancer (NSCLC) cells. |
Targets&IC50 | Skp2:28.77 μM(kd) |
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).[1] |
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.[1] |
Molecular Weight | 312.37 |
Formula | C17H20N4O2 |
Cas No. | 1375060-02-8 |
Smiles | N(CC)(CC)C1=CC(O)=C(/C=N/NC(=O)C=2C=CC=NC2)C=C1 |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 112.5 mg/mL (360.2 mM ), Sonication and heating to 60℃ are recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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