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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $39 | In Stock | |
10 mg | $64 | In Stock | |
25 mg | $128 | In Stock | |
50 mg | $213 | In Stock | |
100 mg | $372 | In Stock | |
500 mg | $869 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | 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. |
In vitro | SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM ; 24-72 h) binds directly to Skp2, leading to degradation of Skp2 by the proteasome.AAA-237 has no significant effect on Skp2 mRNA expression, but has a time-dependent inhibitory effect on Skp2 protein expression in NSCLC cells.[1] SCFSkp2-IN-2 (0.3-3 μM ; 24-72 h) inhibited the proliferation of A549 and H1299 cells in a dose- and time-dependent manner.[1] SCFSkp2-IN-2 (0.3-3 μM ; 24-72 h) blocks the cell cycle at the G0/G1 checkpoint by regulating the Skp2-Cip/Kip and PI3K/Akt-FOXO1 signaling pathways.[1] SCFSkp2-IN-2 (0.3-3 μM ; 24-72 h) induces apoptosis in A549 and H1299 cells in a dose- and time-dependent manner.[1] SCFSkp2-IN-2 (0.3 μM ; 1-7 days) induces NSCLC cell senescence.[1] |
In vivo | SCFSkp2-IN-2 (Compound AAA-237) (15 or 45 mg/kg ; i.p. ; daily for 14 days) showed antitumor activity in a mouse model of lung cancer A549 xenograft.[1] |
Molecular Weight | 312.37 |
Formula | C17H20N4O2 |
Cas No. | 1375060-02-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 112.5 mg/mL (360.2 mM ) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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