1. Cell Cycle/DNA Damage
  2. ClpP
  3. WY165

WY165 is a bifunctional molecule comprising TR79, an activator of the mitochondrial protease complex caseinolytic protease P (ClpP), linked to desthiobiotin. WY165 mediates selective degradation of monomeric streptavidin (mSA) and its fusion proteins localized to the mitochondrial matrix with a DC50 of 197 nM. WY165 restores mitochondrial morphology by reducing the level of mSA fused to short transmembrane protein 1 (mSA-STMP1) in cells overexpressing mSA-STMP1. WY165 can be used for research in cancer, neurodegenerative diseases, cardiovascular diseases, and metabolic diseases.

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

WY165

WY165 Chemical Structure

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Description

WY165 is a bifunctional molecule comprising TR79, an activator of the mitochondrial protease complex caseinolytic protease P (ClpP), linked to desthiobiotin. WY165 mediates selective degradation of monomeric streptavidin (mSA) and its fusion proteins localized to the mitochondrial matrix with a DC50 of 197 nM. WY165 restores mitochondrial morphology by reducing the level of mSA fused to short transmembrane protein 1 (mSA-STMP1) in cells overexpressing mSA-STMP1. WY165 can be used for research in cancer, neurodegenerative diseases, cardiovascular diseases, and metabolic diseases[1].

IC50 & Target

caseinolytic protease P (ClpP), monomeric streptavidin (mSA)

In Vitro

WY165 (10-10000 nM; 24 h) decreases mSA in a dose-dependent manner[1].
WY165's (1 μM; 24 h) mSA degradation activity is inhibited by excess desthiobiotin (1 mM), suggesting that the formation of the [mSA-WY165-ClpP] ternary complex is required[1].
WY165 (0.3-30 μM; 2-12 h) reduced mitochondrial mSA levels in HeLa and MCF7 cells transiently expressing mitochondrial cox8-mSA-FLAG in a dose- and time-dependent manner, with DC50 values for mSA of 4.8 μM and 0.96 μM, respectively[1].
WY165-induced (10 μM; 48 h) degradation of mSA depends on ClpP in HeLa cells[1].
WY165 (1-30 μM) decreases mSA-STMP1 in a dose-dependent manner in HeLa cells transiently expressing cox8-His6-mSA-STMP1-FLAG[1].
WY165 (1 μM) successfully restores the changes in mitochondrial morphology in HeLa cells expressing mSA-STMP1 and do not change mitochondrial morphology in HeLa cells not expressing mSA-STMP1[1].

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

Western Blot Analysis[1]

Cell Line: HeLa cells transiently expressing mitochondrial cox8-mSA-FLAG
Concentration: 1 μM; 3 μM; 10 μM; 30 μM
Incubation Time: 12 h
Result: Successfully reduced the mSA level in the concentration of 10 μM and 30 μM.

Western Blot Analysis[1]

Cell Line: HeLa cells transiently expressing mitochondrial cox8-mSA-FLAG
Concentration: 10 μM
Incubation Time: 2 h; 4 h; 6 h; 12 h
Result: Successfully reduced the mSA level upon 4 h treatment.

Western Blot Analysis[1]

Cell Line: MCF7 cells transiently expressing mitochondrial cox8-mSA-FLAG
Concentration: 0.3 μM; 1 μM; 3 μM; 10 μM; 30 μM
Incubation Time: 12 h
Result: Significantly reduced the mSA level when concentration over 1 μM.

Western Blot Analysis[1]

Cell Line: MCF7 cells transiently expressing mitochondrial cox8-mSA-FLAG
Concentration: 3 μM
Incubation Time: 2 h; 4 h; 6 h; 12 h
Result: Significantly reduced the mSA level upon 2 h treatment.

Western Blot Analysis[1]

Cell Line: HeLa cells with ClpP knockdown by transfection of siClpP
Concentration: 10 μM
Incubation Time: 48 h
Result: Failed to degrade mSA in the presence of ClpP RNAi.

Western Blot Analysis[1]

Cell Line: HeLa cells transiently expressing cox8-His6-mSA-STMP1-FLAG
Concentration: 1 μM; 3 μM; 10 μM; 30 μM
Incubation Time: 48 h
Result: Decreased mSA-STMP1 in a dose-dependent manner.
Molecular Weight

927.02

Formula

C46H61F3N8O9

SMILES

O=C(COCCOCCOCCOCCNC(CCCCC[C@H]([C@@H](N1)C)NC1=O)=O)NCCCN2C(N(CC3=CC=C(C(F)(F)F)C=C3)C(C4=C2CCN(CC5=CC(C#N)=CC=C5)C4)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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.

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WY165
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HY-182964
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