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

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PROTAC SKP2 Degrader-1 Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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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.
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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC SKP2 Degrader-1 Related Classifications

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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

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