2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. SCFSkp2-IN-2

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.

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SCFSkp2-IN-2 Chemical Structure

SCFSkp2-IN-2 Chemical Structure

CAS No. : 1375060-02-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

SCFSkp2-IN-2 Related Antibodies

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Description

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[1].

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.

SCFSkp2-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: A549 and H1299 cells
Concentration: 0.3, 1 and 3 μM
Incubation Time: 24, 48 and 72 h
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.

Cell Proliferation Assay[1]

Cell Line: A549 and H1299 cells
Concentration: 0.3, 1 and 3 μM
Incubation Time: 24, 48 and 72 h
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.

Cell Cycle Analysis[1]

Cell Line: A549 and H1299 cells
Concentration: 0.3, 1 and 3 μM
Incubation Time: 24, 48 and 72 h
Result: Arrested the cell cycle at G0/G1 in a dose- and time-dependent manner.

Apoptosis Analysis[1]

Cell Line: A549 and H1299 cells
Concentration: 0.3, 1 and 3 μM
Incubation Time: 24, 48 and 72 h
Result: The ratio of JC-1 monomer/JC-1 polymer was increased in A549 and H1299 cells as the concentration was increased.
In Vivo

SCFSkp2-IN-2 (Compound AAA-237) (15 or 45 mg/kg; i.p.; daily for 14 days) shows antitumor activity in lung cancer A549 xenograft mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A549 xenograft model[1]
Dosage: 15 or 45 mg/kg
Administration: Intraperitoneal administration, daily for 14 days
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.
Molecular Weight

312.37

Formula

C17H20N4O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CCN(C1=CC(O)=C(C=C1)/C=N/NC(C2=CN=CC=C2)=O)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2013 mL 16.0067 mL 32.0133 mL
5 mM 0.6403 mL 3.2013 mL 6.4027 mL
View the 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.

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Purity & Documentation
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
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SCFSkp2-IN-2 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SCFSkp2-IN-21375060-02-8E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseA549H1299NSCLCSkp2-Cip/KipPI3K/Akt-FOXO1CDK2CDK4Inhibitorinhibitorinhibit

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