2097887-21-1

2097887-21-1 structure

Name: MM-589 TFA
Chemical Name: MM-589 TFA
CAS Number: 2097887-21-1
Molecular Formula: C₃₀H₄₅F₃N₈O₇
Molecular Weight: 686.72
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2019-06-16 22:57:24
Modify Date: 2024-01-12 07:57:55
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM[1].

Name	MM-589 TFA

Description	MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> Histone Methyltransferase
Target	IC50: 0.90 nM (WDR5), 12.7 nM (HMT)[1] Ki: <1 nM (WDR5)[1]
In Vitro	MM-589 (0.01-10 µM, 4 days or 7 days) potently and selectively inhibits cell growth in human leukemia cell lines harboring MLL translocations[1]. Cell Viability Assay[1] Cell Line: MV4-11 and MOLM-13 cells Concentration: 0.01, 0.1, 1, 10 μM Incubation Time: 4 days or 7 days Result: Potently inhibited MV4-11 and MOLM-13 cell growth with IC50s of 0.25 and 0.21 μM, respectively. Had much weaker activity in the inhibition of cell growth of the HL-60 cell line with an IC50 of 8.6 μM.
References	[1]. Karatas H, et al. Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)-Mixed Lineage Leukemia (MLL) Protein-Protein Interaction. J Med Chem. 2017 Jun 22;60(12):4818-4839.

Molecular Formula	C₃₀H₄₅F₃N₈O₇
Molecular Weight	686.72