2. PROTAC Metabolic Enzyme/Protease Cell Cycle/DNA Damage Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. PROTACs E1/E2/E3 Enzyme DNA/RNA Synthesis JAK STAT Apoptosis
  4. PROTAC SKP2 Degrader-1

PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research.
(Pink: Skp2 ligand (HY-N0256); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).

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

PROTAC SKP2 Degrader-1

PROTAC SKP2 Degrader-1 Chemical Structure

CAS No. : 3120650-15-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 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 Customer Validation

PROTAC SKP2 Degrader-1 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All DNA/RNA Synthesis Isoform Specific Products:

View All Isoforms
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research[1]. (Pink: Skp2 ligand (HY-N0256); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).

IC50 & Target[1]

Skp2

 

STAT1

 

In Vitro

PROTAC SKP2 Degrader-1 (compound HD15) (48 h) inhibits the proliferation of Jurkat cells with an IC50 value of 0.98 μM[1].
PROTAC SKP2 Degrader-1 (0.0625-1 μM; 48 h) induces proteasome-dependent degradation of SKP2 in Jurkat cells, with a DC50 of 0.29 μM[1].
PROTAC SKP2 Degrader-1 (0.0625-1 μM; 48 h) modulates the SOCS1/JAK/STAT1/immunoproteasome axis in Jurkat cells, upregulates SOCS1, inhibits p-STAT1, and downregulates the immunoproteasome subunits PSMB8, PSMB9 and PSMB10 in a concentration-dependent manner[1].
PROTAC SKP2 Degrader-1 (0-6 μM; 48 h) inhibits DNA synthesis and proliferation in Jurkat and Hut78 cells in a dose-dependent manner[1].
PROTAC SKP2 Degrader-1 (0.1875-6 μM; 48 h) induces apoptosis in Jurkat cells in a dose-dependent manner[1].

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

PROTAC SKP2 Degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.0625, 0.125, 0.25, 0.5 and 1 μM
Incubation Time: 48 h
Result: Induced concentration-dependent degradation of SKP2 protein in Jurkat cells, with a DC50 of 0.29 μM.
Blocked SKP2 degradation when cotreated with MG132, confirming proteasome-dependent activity.

Apoptosis Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.1875, 0.75, 1.5, 3 and 6 μM
Incubation Time: 48 h
Result: Induced apoptosis in Jurkat cells in a dose-dependent manner.
Parmacokinetics
Species Dose Route T1/2 MRT0-inf CL AUC0-t AUC0-inf Tmax Cmax CL/F
Mice[1] 10 mg/kg i.v. 1.81 h 0.92 h 48.8 mL/min/kg 3387 ng·h/mL 3441 ng·h/mL / / /
Mice[1] 40 mg/kg i.p. 3.71 h / / 26714 ng·h/mL 26876 ng·h/mL 2.0 h 4497 ng/mL 25 mL/min/kg
In Vivo

PROTAC SKP2 Degrader-1 (10-40 mg/kg; i.p.; daily; 14 days) dose-dependently inhibits subcutaneous Jurkat xenograft tumor growth in female NCG mice[1].

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

Animal Model: NCG mice (female, 6-7 weeks old, 20-25 g, subcutaneous xenograft via Jurkat cell inoculation)[1]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.p.; daily; 14 days
Result: Achieved a 66% tumor growth inhibition (TGI) rate at 40 mg/kg.
Achieved a TGI exceeding 50% at 20 mg/kg.
Reduced tumor volume and weight significantly across all doses compared to vehicle control.
Suppressed SKP2, phosphorylated STAT1, and immunoproteasome subunits PSMB8, PSMB9, and PSMB10 in a dose-dependent manner in tumor tissue.
Upregulated SOCS1 expression in tumor tissue.
Induced dose-dependent tumor cell apoptosis and necrosis.
Reduced microvascular density and proliferation in a dose-dependent manner.
Caused no significant changes in body weight, liver function biomarkers, or kidney function biomarkers across all doses.
Showed no pathological alterations in heart, liver, spleen, lung, or kidney tissues.
Molecular Weight

1074.46

Formula

C60H91N5O10S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOCCOCCNC([C@]45[C@](CC(C)(CC5)C)([H])C6=CC[C@@]([C@@]7([C@@]([C@@](C)([C@H](CC7)O)CO)([H])CC8)C)([H])[C@]8(C)[C@@]6(CC4)C)=O)=O
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 : 100 mg/mL (93.07 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 0.9307 mL 4.6535 mL 9.3070 mL
5 mM 0.1861 mL 0.9307 mL 1.8614 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.

  • 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 0.9307 mL 4.6535 mL 9.3070 mL 23.2675 mL
5 mM 0.1861 mL 0.9307 mL 1.8614 mL 4.6535 mL
10 mM 0.0931 mL 0.4654 mL 0.9307 mL 2.3268 mL
15 mM 0.0620 mL 0.3102 mL 0.6205 mL 1.5512 mL
20 mM 0.0465 mL 0.2327 mL 0.4654 mL 1.1634 mL
25 mM 0.0372 mL 0.1861 mL 0.3723 mL 0.9307 mL
30 mM 0.0310 mL 0.1551 mL 0.3102 mL 0.7756 mL
40 mM 0.0233 mL 0.1163 mL 0.2327 mL 0.5817 mL
50 mM 0.0186 mL 0.0931 mL 0.1861 mL 0.4654 mL
60 mM 0.0155 mL 0.0776 mL 0.1551 mL 0.3878 mL
80 mM 0.0116 mL 0.0582 mL 0.1163 mL 0.2908 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.

PROTAC SKP2 Degrader-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:

PROTAC SKP2 Degrader-13120650-15-6PROTACsE1/E2/E3 EnzymeDNA/RNA SynthesisJAKSTATApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseJanus kinaseJAK/STAT pathwaySKP2T lymphoblastic leukemia cellsHut78 T-ALL cellsJurkat T-ALL cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC SKP2 Degrader-1
Cat. No.:
HY-181653
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

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

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