SCFSkp2-IN-2
Based on 1 publication(s) in Google Scholar
SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities.
For research use only. We do not sell to patients.
- Purity : 99.01%
- CAS No.: 1375060-02-8
- Formula: C17H20N4O2
- Molecular Weight:312.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SCFSkp2-IN-2
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Biological Activity
Description
IC50 & Target
KD: 28.77 μM (Skp2)[1]
In Vitro
SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM; 24-72 h) can directly bind to Skp2, causing the degradation of Skp2 by proteasome. AAA-237 has no significant effect on the mRNA expression of Skp2 but inhibits the protein expression of Skp2 in NSCLC cells in a time-dependent manner[1].
SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) inhibits 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) arrests 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 of A549 and H1299 cells in a dose- and time-dependent manner[1].
SCFSkp2-IN-2 (0.3 μM; 1-7 days) induces cellular senescence of the NSCLC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:A549 and H1299 cells
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Concentration:0.3, 1 and 3 μM
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Incubation Time:24, 48 and 72 h
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Result:Increased the expression levels of p21Cip1 and p27Kip1. Decreased the level of Skp2.
Reduced the expression levels of CDK2, p-CDK2, cyclin E1, CDK4, p-CDK4 and cyclin D.
Increased the levels of cleaved PARP, cleaved caspase 3, cleaved caspase 9 and Bax. Decreased the expression of PARP and Bcl-2.
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Cell Line:A549 and H1299 cells
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Concentration:0.3, 1 and 3 μM
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Incubation Time:24, 48 and 72 h
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Result:Inhibited the proliferation of A549 and H1299 cells in a dose- and time-dependent manner. The IC50 for A549 was 3 μM at 24 h, 2.5 μM at 48 h and 0.7 μM at 72 h. The IC50 for H1299 was 3.9 μM at 24 h, 1.8 μM at 48 h and 1.1 μM at 72 h.
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Cell Line:A549 and H1299 cells
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Concentration:0.3, 1 and 3 μM
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Incubation Time:24, 48 and 72 h
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Result:Arrested the cell cycle at G0/G1 in a dose- and time-dependent manner.
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Cell Line:A549 and H1299 cells
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Concentration:0.3, 1 and 3 μM
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Incubation Time:24, 48 and 72 h
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Result:The ratio of JC-1 monomer/JC-1 polymer was increased in A549 and H1299 cells as the concentration was increased.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 xenograft model[1]
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Dosage:15 or 45 mg/kg
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Administration:Intraperitoneal administration, daily for 14 days
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Result:Significantly reduced tumor volume and weight. The tumor growth inhibition of the low dose and high dose was 55% and 64%, respectively. No obvious weight loss or abnormal behavior was observed. Reduced the expression of Ki67 in tumor tissue. Reduced the expression of Skp2 and Bcl-2 and increased the expression of p27, the cleaving of caspase 3, caspase 9, PARP and Bax.
Chemical Information
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CAS No. 1375060-02-8
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Appearance Solid
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Molecular Weight 312.37
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Formula C17H20N4O2
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Color Light yellow to yellow
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SMILES
CCN(C1=CC(O)=C(C=C1)/C=N/NC(C2=CN=CC=C2)=O)CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (400.17 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2013 mL | 16.0067 mL | 32.0133 mL | 80.0333 mL |
| 5 mM | 0.6403 mL | 3.2013 mL | 6.4027 mL | 16.0067 mL | |
| 10 mM | 0.3201 mL | 1.6007 mL | 3.2013 mL | 8.0033 mL | |
| 15 mM | 0.2134 mL | 1.0671 mL | 2.1342 mL | 5.3356 mL | |
| 20 mM | 0.1601 mL | 0.8003 mL | 1.6007 mL | 4.0017 mL | |
| 25 mM | 0.1281 mL | 0.6403 mL | 1.2805 mL | 3.2013 mL | |
| 30 mM | 0.1067 mL | 0.5336 mL | 1.0671 mL | 2.6678 mL | |
| 40 mM | 0.0800 mL | 0.4002 mL | 0.8003 mL | 2.0008 mL | |
| 50 mM | 0.0640 mL | 0.3201 mL | 0.6403 mL | 1.6007 mL | |
| 60 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3339 mL | |
| 80 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0004 mL | |
| 100 mM | 0.0320 mL | 0.1601 mL | 0.3201 mL | 0.8003 mL |
SCFSkp2-IN-2 Related Classifications
HY-148900 Related Classifications
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