Art. -Nr.: HY-W1128879

XMU-MP-8

(Synonyms: SKPer1)

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Based on 1 Customer Validation

XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncoprotein SKP2. XMU-MP-8 simultaneously binds to the F-box domain of SKP2 (K_d ≈ 36 μM) and the N-terminal TPR domain of the E3 ligase STUB1 (K_d ≈ 2.5 μM), forming a stable SKP2-SKPer1-STUB1 ternary complex (K_d ≈ 8.9 nM) that induces SKP2 ubiquitination and proteasomal degradation. XMU-MP-8 selectively eliminates SKP2-expressing cancer cells. XMU-MP-8 exhibits substantial tumour suppression with good safety profiles in vivo. XMU-MP-8 can be used for cancer research, such as non-small cell lung adenocarcinoma (NSCLC) and prostatic adenocarcinoma.

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Reinheit: 99.23%
CAS. Nr.: 2271314-01-1
Formel: C₂₆H₂₁F₃N₈S
Molecular Weight:534.56

Speicherung:

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

XMU-MP-8 Chemical Structure

CAS. Nr.: 2271314-01-1

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

SKP2

36 μM (Kd)

In Vitro

XMU-MP-8 (10 μM, 24 h) produces a cell survival phenotype specifically in the SKP2-F-C cell line, with no survival observed in other F-C cell lines, ruling out the possibility that it generally interferes with the activation of the F-C death protein^[1].
XMU-MP-8 (1-10 μM, 0-24 h) triggers SKP2 ubiquitination and proteasomal degradation, significantly reducing its half-life and depleting endogenous SKP2 protein without affecting its mRNA levels^[1].
XMU-MP-8 (72 h) inhibits proliferation of SKP2-high cell lines with IC₅₀s of 3.7 μM (PC-3), 6.7 μM (A549), 3.7 μM (JHH-7), 6.2 μM (SW620), 4.5 μM (LoVo), 6.9 μM (RKO), 5.6 μM (Caco2) and 5.3 μM (HeLa)^[1].
XMU-MP-8 (10 μM ,72 h) completely blocks proliferation and induces massive cell death of SKP2-high cell lines^[1].
XMU-MP-8 (10 μM, 24 h) induces the degradation of SKP2 protein and the accumulation of p27 protein in SKP2-high cell lines (JHH-7 and PC-3), with no significant changes in SKP2-low cell lines (IMR-90 and MCF-10A)^[1].
XMU-MP-8 (2.5-10 μM, 0-5 days) shows no significant effect on the growth of normal mouse intestine organoids and human peripheral blood mononuclear cells^[1].
XMU-MP-8 (10 μM ,2.5 h) induces SKP2 degradation by recruiting the E3 ligase STUB1 to the F-box domain of SKP2, forming a ternary complex that enhances the SKP2-STUB1 interaction by 122-fold and ultimately leads to SKP2 ubiquitination and degradation^[1].

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

Western Blot Analysis^[1]

Cell Line:

JHH-7 and HeLa cells
Concentration:

1, 2, 5, and 10 μM
Incubation Time:

0, 2, 4, 6, 8, 12 and 24 h
Result:

Reduced SKP2 levels in JHH-7 and HeLa cells in a dose- and time-dependent manner.
Degraded SKP2 through the proteasome, but not the lysosome.
Induced ubiquitination of SKP2.
Significantly reduced the SKP2 half-life of SKP2 (from 10.8 h to 3.3 h in JHH-7 cells, and from 11.3 h to 6.2 h in HeLa cells).

Western Blot Analysis^[1]

Cell Line:

A549 and PC-3 cells and derived genetically modified lines.
Concentration:

5 and 10 μM
Incubation Time:

2.5 and 24 h
Result:

Failed to degrade SKP2-F-C when three lysine residues (3K>R) in its F-box domain were mutated.
Failed to induce ubiquitination of the SKP2 3K>R mutant protein.
Was unable to exert its anti-proliferative effect in cells where endogenous SKP2 had been replaced with the degradation-resistant 3K>R mutant.
Failed to induce SKP2 ubiquitination and degradation in STUB1 knockout cells.
Re-gained its ability to degrade SKP2 following the reconstitution of sgRNA-resistant STUB1 in STUB1 knockout cells.
Still recruited the 3K>R mutant to STUB1, even though this mutant was resistant to degradation.

In Vivo

XMU-MP-8 (15 and 30 mg/kg, i.v., daily for 14 days) demonstrates potent antitumor efficacy in A549 and PC-3 xenograft mice models, mediated through SKP2 degradation^[1].
XMU-MP-8 (30 mg/kg, i.v., daily for 14 days) shows no adverse effects in BALB/c nude mice^[1].

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

Animal Model:

Male BALB/c nude mice (6 weeks old)^[1]
Dosage:

30 mg/kg
Administration:

i.v., daily for 14 days
Result:

Exhibited no significant changes in body weight and liver function (ALT/AST levels).
Showed no histopathological damage in the heart, kidney, liver, lung, or spleen.

Animal Model:

Male BALB/c nude mice (6 weeks old) subcutaneously injected with A549 or PC-3 cells^[1]
Dosage:

15 and 30 mg/kg
Administration:

i.v., daily for 14 days
Result:

Completely ceased the growth of A549 tumors.
Caused a 95 % reduction in tumour growth in PC-3 xenograft model.
Caused depletion of SKP2 and an increase of p27 in the xenograft PC-3 tumour.

Chemical Information

CAS. Nr. 2271314-01-1
Appearance Solid
Molecular Weight 534.56
Formel C₂₆H₂₁F₃N₈S
Color White to off-white
SMILES

CN1N=CC2=C(NCC3=CC=CN=C3)N=C(C4=CC=CC(NC(NC5=CC=CC(C(F)(F)F)=C5)=S)=C4)N=C21
Synonyms

SKPer1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 116.67 mg/mL (218.25 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

1.8707 mL

9.3535 mL

18.7070 mL

5 mM

0.3741 mL

1.8707 mL

3.7414 mL

10 mM

0.1871 mL

0.9353 mL

1.8707 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[1]. Chu Y, et al. A rapid imaging-based screen for induced-proximity degraders identifies a potent degrader of oncoprotein SKP2. Nat Biotechnol. 2025 Sep 10. [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	1.8707 mL	9.3535 mL	18.7070 mL	46.7674 mL
	5 mM	0.3741 mL	1.8707 mL	3.7414 mL	9.3535 mL
	10 mM	0.1871 mL	0.9353 mL	1.8707 mL	4.6767 mL
	15 mM	0.1247 mL	0.6236 mL	1.2471 mL	3.1178 mL
	20 mM	0.0935 mL	0.4677 mL	0.9353 mL	2.3384 mL
	25 mM	0.0748 mL	0.3741 mL	0.7483 mL	1.8707 mL
	30 mM	0.0624 mL	0.3118 mL	0.6236 mL	1.5589 mL
	40 mM	0.0468 mL	0.2338 mL	0.4677 mL	1.1692 mL
	50 mM	0.0374 mL	0.1871 mL	0.3741 mL	0.9353 mL
	60 mM	0.0312 mL	0.1559 mL	0.3118 mL	0.7795 mL
	80 mM	0.0234 mL	0.1169 mL	0.2338 mL	0.5846 mL
	100 mM	0.0187 mL	0.0935 mL	0.1871 mL	0.4677 mL

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XMU-MP-8

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Anti-Lung Cancer Compound Library

Molecular Glue Compound Library

Metabolic Enzyme Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XMU-MP-8

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Anti-Lung Cancer Compound Library

Molecular Glue Compound Library

Metabolic Enzyme Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XMU-MP-8 Related Classifications

HY-W1128879 Related Classifications