| Identification | Back Directory | [Name]
2-[(4-Chlorophenyl)amino]-N-[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]hexyl]-4-thiazolecarboxamide | [CAS]
2785323-62-6 | [Synonyms]
PROTAC-O4I2 2-[(4-Chlorophenyl)amino]-N-[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]hexyl]-4-thiazolecarboxamide | [Molecular Formula]
C29H29ClN6O5S | [MOL File]
2785323-62-6.mol | [Molecular Weight]
609.1 |
| Hazard Information | Back Directory | [Uses]
PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells[1]. | [in vivo]
PROTAC-O4I2 (10 μM) significantly increases survival by interference with the maintenance and proliferation of tumor in a Drosophila intestinal tumor model[1]. | Animal Model: | Drosophila melanogaster[1] | | Dosage: | 10 μM | | Administration: | Flies were fed on a round filter paper loaded with PROTAC-O4I2 in a 5% sucrose solution, maintained at 18℃ and flipped into a freshly prepared vial every 2 days | | Result: | Decreased stem cell activity, blocked the initiation and growth of tumor, and improved the survival of the Drosophila ISC tumor model. |
| [IC 50]
Cereblon | [References]
[1] Rodrigo A Gama-Brambila, et al. A PROTAC targets splicing factor 3B1. Cell Chem Biol. 2021 Nov 18;28(11):1616-1627.e8. DOI:10.1016/j.chembiol.2021.04.018 |
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