Chemical Structure : JMV7048
CAS No.:
2871774-88-6
JMV7048
(JMV-7048)
Catalog No.: PC-24992Not For Human Use, Lab Use Only.
JMV7048 is a potent, selective and effective PROTAC degrader of pregnane X receptor (PXR) with DC50 of 379 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
JMV7048 is a potent, selective and effective PROTAC degrader of pregnane X receptor (PXR) with DC50 of 379 nM.
JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome.
JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein.
JMV7048 specifically degrades PXR in colon carcinoma, hepatoma, and pancreatic cancer cell lines, but not in primary cultures of human hepatocytes.
Physicochemical Properties
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M.Wt
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957.19
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Formula
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C53H64N8O7S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-Piperazinehexanamide, 4-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-N-[7-[1-(phenylmethyl)-5-[[(2,4,6-trimethylphenyl)sulfonyl]amino]-1H-benzimidazol-2-yl]heptyl]-
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References
1. Lucile Bansar, et al. Targeting Pregnane X Receptor with a Potent Agonist-Based PROTAC to Delay Colon Cancer Relapse. bioRxiv - Cancer Biology Pub Date : 2024-06-22.
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