RB-CO-PEG5-C2-CO-VH032
RB-CO-PEG5-C2-CO-VH032 is a VHL-recruiting TRIM24 PROTAC degrader composed of an RB-derived short peptide SPRT, a PEG5-C2 linker, and the VHL ligand VH032. RB-CO-PEG5-C2-CO-VH032 recognizes proteins containing the FXXXV motif and recruits VHL to induce degradation of proteins such as TRIM24, thereby upregulating DUSP2, inhibiting ERK/mTOR signaling, and suppressing prostate cancer cell proliferation. RB-CO-PEG5-C2-CO-VH032 can be used for TRIM24 degradation and prostate cancer-related research.
(Pink: TRIM24 ligand (HY-161394); Blue: VHL ligand (HY-125845); Black: linker (HY-116006)).
For research use only. We do not sell to patients.
- Formula: C54H85N11O17S
- Molecular Weight:1192.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
TRIM24 |
In Vitro
RB-CO-PEG5-C2-CO-VH032 decreases TRIM24 and p65 protein levels in C4-2 and 22Rv1 cells without reducing their mRNA levels; the VHL ligand VL285 blocks the decrease of TRIM24/p65 proteins, whereas the ASPRAT-PROTAC negative control does not decrease the protein levels of either, supporting its VHL-dependent and sequence recognition-related degradation mechanism[1].
RB-CO-PEG5-C2-CO-VH032 decreases multiple FXXXV motif-containing proteins, including TRIM24, p65, HDAC8, TBK1, and EZH1, in quantitative proteomic analysis of C4-2 cells, indicating that it is not a strictly protein-selective degrader[1].
RB-CO-PEG5-C2-CO-VH032 (0.5-10 μM) modulates multiple signaling pathways in C4-2 cells in a concentration-dependent manner and inhibits pathways including PI3K-AKT and TNF[1].
RB-CO-PEG5-C2-CO-VH032 (0-1 μM) decreases TRIM24, pERK1/2, and pS6K1 T389 levels and increases DUSP2 in C4-2 and 22Rv1 cells, supporting its inhibition of mTOR signaling through the TRIM24-DUSP2-ERK/mTOR axis[1].
RB-CO-PEG5-C2-CO-VH032 (5 days; alone or in combination with RAD001) inhibits the proliferation of C4-2 and 22Rv1 cells, with a stronger inhibitory effect observed in combination[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
RB-CO-PEG5-C2-CO-VH032 (10 mg/kg; i.p.; 30 days; in combination with RAD001 3 mg/kg/day) further suppresses tumor volume and tumor weight in prostate cancer PDX tumor-bearing NSG mice, with a stronger effect than either single-agent group[1].
RB-CO-PEG5-C2-CO-VH032 inhibits tumor growth and reduces tumor weight in C4-2 prostate cancer xenografts in BALB/c nude mice, and its inhibitory effect is further enhanced when combined with RAD001[1].
RB-CO-PEG5-C2-CO-VH032 alone or in combination with RAD001 does not significantly alter body weight, liver function, or kidney function indicators in PDX and C4-2 xenograft mouse models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (male)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 4 days; 30 days
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Result:Improved the antitumor effect of RAD001 in the PDX mouse model.
Did not significantly change the body weight or liver or renal function of the mice.
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Animal Model:BALB/C-nude (male, 6 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; 30 days
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Result:Improved the antitumor effect of RAD001 in the C4-2 xenograft mouse model.
Did not significantly change the body weight or liver or renal function of the mice.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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Molecular Weight 1192.38
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Formula C54H85N11O17S
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SMILES
O[C@@H](C)[C@H](NC([C@H](CCCNC(N)=N)NC([C@H]1N(C([C@@H](NC(CCOCCOCCOCCOCCOCCC(N[C@H](C(N2C[C@H](O)C[C@H]2C(NCC3=CC=C(C4=C(C)N=CS4)C=C3)=O)=O)C(C)(C)C)=O)=O)CO)=O)CCC1)=O)=O)C(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RB-CO-PEG5-C2-CO-VH032 Related Classifications
HY-161393 Related Classifications
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