2407449-49-2
Chemical Structure
MS40
- CAS No.: 2407449-49-2
- Formula:C52H61F3N10O7
- Molecular Weight:995.10
IUPAC Name: 3-bromo-9-(phenyl-d5)-9H-carbazole
InChIKey: STBAQMSNPQNEBZ-UHFFFAOYSA-N
SMILES: O=C1C=C(C(F)(F)F)C(C(NC2=CC(C3=CC(CN4CCN(CC4)CCNC(CCCCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=O)=CC=C3)=CC=C2N8CCN(CC8)C)=O)=CN1
Biological Activity: MS40 is a WDR5 PROTAC degrader with a DC50 of 42 nM in MV4;11 MLL-rearranged acute myeloid leukemia (AML) cells. MS40 induces WDR5 degradation dependent on WDR5, CRBN and the proteasome, dissociates the MLL/KMT2A complex from chromatin, reduces H3K4me2 levels, degrades IKZF1/IKZF3, the novel substrates of CRBN, inhibits the transcription of WDR5/MLL and IKZF target genes, and suppresses cancer cell growth. MS40 can be used in the research of MLL-rearranged acute myeloid leukemia, breast cancer, Burkholderia infection and cystic fibrosis-associated bacterial infections[1][2].
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MS40 | MS40 is a WDR5 PROTAC degrader with a DC50 of 42 nM in MV4;11 MLL-rearranged acute myeloid leukemia (AML) cells. MS40 induces WDR5 degradation dependent on WDR5, CRBN and the proteasome, dissociates the MLL/KMT2A complex from chromatin, reduces H3K4me2 levels, degrades IKZF1/IKZF3, the novel substrates of CRBN, inhibits the transcription of WDR5/MLL and IKZF target genes, and suppresses cancer cell growth. MS40 can be used in the research of MLL-rearranged acute myeloid leukemia, breast cancer, Burkholderia infection and cystic fibrosis-associated bacterial infections. | |||||||||||||||||||||
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References
- [1]. Li D, et al. Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic. Oncogene. 2022 Jun;41(24):3328-3340. [Content Brief]
- [2]. Maydaniuk D, et al. New Auranofin Analogs with Antibacterial Properties against Burkholderia Clinical Isolates. Antibiotics (Basel). 2021 Nov 24;10(12):1443.
