2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. Skp2 inhibitor 1

Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor against the Skp2-Cks1 interaction with an IC50 of 2.8 μM. Skp inhibitor 1 exhibits anticancer activity.

For research use only. We do not sell to patients.

Skp2 inhibitor 1 Chemical Structure

Skp2 inhibitor 1 Chemical Structure

CAS No. : 2760612-63-1

Size Price Stock Quantity
1 mg USD 420 In-stock
5 mg USD 1050 In-stock
10 mg USD 1680 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Skp2 inhibitor 1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor against the Skp2-Cks1 interaction with an IC50 of 2.8 μM. Skp inhibitor 1 exhibits anticancer activity[1].

IC50 & Target

Growth arrest-specific protein 6(Gas6)-Cell Cyclin Kinase Subunit 1(Cks1) [1] IC50：2.8 μM(Growth arrest-specific protein 6,Gas6; Cell Cyclin Kinase Subunit 1,Cks1)[1]
In Vitro

Skp2 inhibitor 1 (2.8 μM,72 h) interferes the Skp2−Cks1 interaction, against PC-3 and MGC-803 cells with IC50 values of 4.8 and 7.0 μM, respectively[1].
Skp2 inhibitor 1 (10 μM, 48h) inhibits the proliferation and migration of PC-3 and MGC-803 cell, causing them to block in the S phase and promote cell apoptosis [1].

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

Skp2 inhibitor 1 Related Antibodies

Cell Viability Assay[1]

Cell Line: PC-3 , MGC-803
Concentration: 0-10 μM
Incubation Time: 72 h
Result: Against the Skp2−Cks1 interaction with an IC50 value of 2.8 μM, and against PC-3 and MGC-803 cells with IC50 values of 4.8 and 7.0 μM, respectively.

Apoptosis Analysis[1]

Cell Line: PC-3 , MGC-803
Concentration: 2.5 μM , 5 μM , 10 μM
Incubation Time: 0-48 h
Result: Leaded to cell cycle S-phase arrest in a dose-dependent manner, and induced apoptosis in a dose-dependent manner, such as nuclear fragmentation, condensation, and cell shrinkage.

Cell Proliferation Assay[1]

Cell Line: PC-3 , MGC-803
Concentration: 0.5 μM , 1 μM , 2 μM
Incubation Time: 10 days
Result: Inhibited colony-forming abilities in a dose-dependent manner.

Cell Migration Assay [1]

Cell Line: PC-3 , MGC-803
Concentration: 2.5 μM , 5 μM , 10 μM
Incubation Time: 48 h
Result: Inhibited migration in a dose-dependent manner.

Cell Invasion Assay[1]

Cell Line: PC-3 , MGC-803
Concentration: 0.5 μM , 1 μM , 2 μM
Incubation Time: 48 h
Result: Inhibited invasion in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: PC-3 , MGC-803
Concentration: 2.5 μM , 5 μM , 10 μM
Incubation Time: 0-48 h
Result: Inhibited the protein levels of Skp2 in a dose-dependent manner, restored the expression of p21 and p27 in a time-dependent manner.
In Vivo

Skp2 inhibitor 1 (50 mg/kg, intraperitoneal injection/2 day, 21 days) inhibits tumor growth significantly in NOD-SCID xenograft models without obvious toxicity. In addition, the tumor treated with Skp2 inhibitor 1 (50 mg/Kg/2 day) was completely suppressed in vivo[1].
Skp2 inhibitor 1 decreases tumor malignancy via suppressing the Skp2 signal pathway and increase the proportion of apoptosis in the tumor tissue[1].
Pharmacokinetic Parameters of Compound 14i in the Plasma and Tumor Tissue[1]

药代动力学分析[1]

PK parameters plasma tumor tissue
t1/2 14.1±1.5(h) 12.6±7.8(h)
Cmax 176.1±30.3(ng/mL) 182.0±80.9(ng/g)
AUClast 3231.5±407.2(h.ng/mL) 2443.9±474.9(h.ng/g)
AUCINF 3551.5±465.3(h.ng/mL) 2636.0±619.7(h.ng/g)
VZ 143.3±9.2(L/kg) 170.8±80.1(mg/kg)
CL 7.1±0.8(L/h/kg) 15.7±4.2(mg/h/kg)
MRTlast 13.4±0.64(h) 9.9±2.5(h)

t1/2 of 14i in the Liver Microsomes and Liver S9 ofDifferent Species[1]

体外代谢分析[1]
species human rat mouse
t1/2 liver microsomes 66.0 16.3 15.3
t1/2 liver S9 64.8 15.4 16.5

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

Animal Model: The xenograft models of PC-3 and MGC-803 cells in NOD-SCID mice[1].
Dosage: 10 mg/kg; 25 mg/kg, 50 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Inhibited tumor growth without obvious toxicity, the tumor growth inhibition ratio was 55.68, 71.86, and 90.42% with 10, 25, and 50 mg/Kg/2 day, respectively.
Molecular Weight

406.91

Formula

C23H23ClN4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1CCN(C2=NC(C3=CC=CC=C3)=C(N=C2)C4=CC=CC=C4)CC1)CCl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (122.88 mM; Need ultrasonic; 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 2.4575 mL 12.2877 mL 24.5755 mL
5 mM 0.4915 mL 2.4575 mL 4.9151 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 (sealed storage, away from moisture and light). 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 2.4575 mL 12.2877 mL 24.5755 mL 61.4386 mL
5 mM 0.4915 mL 2.4575 mL 4.9151 mL 12.2877 mL
10 mM 0.2458 mL 1.2288 mL 2.4575 mL 6.1439 mL
15 mM 0.1638 mL 0.8192 mL 1.6384 mL 4.0959 mL
20 mM 0.1229 mL 0.6144 mL 1.2288 mL 3.0719 mL
25 mM 0.0983 mL 0.4915 mL 0.9830 mL 2.4575 mL
30 mM 0.0819 mL 0.4096 mL 0.8192 mL 2.0480 mL
40 mM 0.0614 mL 0.3072 mL 0.6144 mL 1.5360 mL
50 mM 0.0492 mL 0.2458 mL 0.4915 mL 1.2288 mL
60 mM 0.0410 mL 0.2048 mL 0.4096 mL 1.0240 mL
80 mM 0.0307 mL 0.1536 mL 0.3072 mL 0.7680 mL
100 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.6144 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Skp2 inhibitor 1 Related Classifications

Help & FAQs
  • 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:

Skp2 inhibitor 12760612-63-1E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasePC-3 MGC-803xenograftanticancerPPIInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Skp2 inhibitor 1
Cat. No.:
HY-149293
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.