FKBP12-PROTAC-RC32-RC32-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFKBP12 PROTAC RC32Cat. No.: HY-130835CAS No.: 2375555-66-9Synonyms: RC32分式: CHNO分量: 1426.69作靶点: PROTAC作通路: PROTAC储存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 FKBP12 PROTAC RC32

2、(RC32) PROTAC 的有效 FKBP12 降解剂。FKBP12 PROTAC RC32 包含雷帕霉素 (Rapamycin；HY-10219) 和 E3 泛素连接酶配体 (Pomalidomide；HY-10984)。IC50 & Target Cereblon体外研究 FKBP12 PROTAC RC32 (RC32; 0.1-1000 nM; for 12hours) results in 50% protein degradation (DC50) of0.3nM after only 12hours of treatment 1.Western Blot Analysis 1C

3、ell Line: Jurkat cellsConcentration: 0.1, 1, 10, 100, 1000 nMIncubation Time: For 12hoursResult: Resulted in 50% protein degradation (DC50) of 0.3nM after only 12h of treatment.体内研究RC32 (RC32; i.p.; 30mg/kg; twice a day; 1 day) degrades the FKBP12 protein in most of the organs oftreated mice, except

4、 for the brain after only 1 day of treatment in mice 1.RC32 (orally; 60mg/kg; twice a day; for 1 day) significantly degrades FKBP12 in mice 1.RC32 (i.p.; 8mg/kg; twice a day; for 2 days) efficiently degrades the FKBP12 protein in most of the organsexamined in Bama pigs (20kg) 1.1/2 Master of Small M

5、olecules 您边的抑制剂师www.MedChemERC32 (i.p.; 8mg/kg; twice a day; for 3 days) efficiently degrades FKBP12 in the heart, liver, kidney, spleen,lung, and stomach of rhesus monkeys 1.Animal Model: Male and female mice 1Dosage: 30mg/kgAdministration: IP; twice a day; 1 dayResult: Degraded the FKBP12 protein

6、in most of the organs of treated mice after only 1 day oftreatment.REFERENCES1. A chemical approach for global protein knockdown from mice to non-human primates. Cell Discov. 2019 Feb 5;5:10.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820