Cat. No.: HY-181653

PROTAC SKP2 Degrader-1

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Based on 1 Customer Validation

PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a K_d 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.

Purity: 99.91%
CAS No.: 3120650-15-6
Formula: C₆₀H₉₁N₅O₁₀S
Molecular Weight:1074.46

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PROTAC SKP2 Degrader-1 Chemical Structure

CAS No.: 3120650-15-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a K_d 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

All PROTACs Isoforms :

All DNA/RNA Synthesis Isoforms :

All JAK Isoforms :

All STAT Isoforms :

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.

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	T_1/2	MRT_0-inf	CL	AUC_0-t	AUC_0-inf	T_max	C_max	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.

Chemical Information

CAS No. 3120650-15-6
Appearance Solid
Molecular Weight 1074.46
Formula C₆₀H₉₁N₅O₁₀S
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9307 mL

4.6535 mL

9.3070 mL

5 mM

0.1861 mL

0.9307 mL

1.8614 mL

10 mM

0.0931 mL

0.4654 mL

0.9307 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Chen L, et al. Natural Product-Inspired PROTACs for Leukemia Therapy: Hederagenin-Driven Targeted Degradation of SKP2. J Med Chem. 2026;69(4):4579-4601. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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PROTAC SKP2 Degrader-1

PROTAC Library

All PROTACs Isoforms

All DNA/RNA Synthesis Isoforms

All JAK Isoforms

All STAT Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PROTAC SKP2 Degrader-1 Related Classifications

HY-181653 Related Classifications