MA191

MA191 is a FLT3 PROTAC degrader. MA191 abrogates FLT3 inhibitor resistance from rebound activation of mitogen-activated kinases. MA191 mediates rapid FLT3-ITD degradation through a mechanism requiring VHL, neddylation, and BIM. MA191 reduces FLT3-ITD levels before inducing apoptosis. MA191 halts AML cell proliferation in Danio rerio. MA191 can be used for the study of acute myeloid leukemia (AML) (Pink: FLT3 ligand: (HY-175311), Blue: E3 ligase CRBN Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175312) ) [1].

Product Specifications

UNSPSC

12352005

Target

Akt; Apoptosis; ERK; FLT3; HSP; PROTACs; STAT

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; JAK/STAT Signaling; MAPK/ERK Pathway; Metabolic Enzyme/Protease; PI3K/Akt/mTOR; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer

Smiles

[H]N([C@@H](C)C1=CC=C(C2=C(C)N=CS2)C=C1)C([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC([C@@H]4CC[C@H](C(N5CCN(CCNC(C6=CC(OC7=CC=C(NC(NC8=NOC(C(C)(C)C)=C8)=O)C=C7)=CC=N6)=O)CC5)=O)CC4)=O)=O)=O

Molecular Formula

C57H73N11O9S

Molecular Weight

1088.32

References & Citations

[1]Melisa Halilovic, et al. Rapid proteasomal degradation of mutant feline McDonough sarcoma-like tyrosine 2 kinase-3 overcomes tyrosine kinase inhibitor resistance of acute myeloid leukemia 3 cells.