JMV7048 | PXR PROTAC | Probechem Biochemicals

Chemical Structure : JMV7048

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JMV7048 (JMV-7048)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	957.19
分子式	C53H64N8O7S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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]-

参考文献

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.

JMV7048 (JMV-7048)

生物&药学活性

物理化学性质&存储条件

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JMV7048 (JMV-7048)

生物&药学活性

物理化学性质&存储条件

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