1. Epigenetics
  2. Histone Methyltransferase
  3. MM-589 TFA

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.

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MM-589 TFA Chemical Structure

MM-589 TFA Chemical Structure

CAS No. : 2253167-09-6

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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target

IC50: 0.90 nM (WDR5), 12.7 nM (HMT)[1]

Ki: <1 nM (WDR5)[1]

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
8.56 μM
Compound: 18; MM-589
Cytotoxicity against human HL60 cells lacking MLL translocation assessed as cell growth inhibition after 4 days by WST8 assay
Cytotoxicity against human HL60 cells lacking MLL translocation assessed as cell growth inhibition after 4 days by WST8 assay
[PMID: 28603984]
MOLM-13 IC50
0.1 μM
Compound: 18; MM-589
Cytotoxicity against human MOLM13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition after 7 days by WST8 assay
Cytotoxicity against human MOLM13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition after 7 days by WST8 assay
[PMID: 28603984]
MOLM-13 IC50
0.21 μM
Compound: 18; MM-589
Cytotoxicity against human MOLM13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition after 4 days by WST8 assay
Cytotoxicity against human MOLM13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition after 4 days by WST8 assay
[PMID: 28603984]
MV4-11 IC50
0.25 μM
Compound: 18; MM-589
Cytotoxicity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition after 4 days by WST8 assay
Cytotoxicity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition after 4 days by WST8 assay
[PMID: 28603984]
MV4-11 IC50
0.29 μM
Compound: 18; MM-589
Cytotoxicity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition after 7 days by WST8 assay
Cytotoxicity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition after 7 days by WST8 assay
[PMID: 28603984]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

686.72

Formula

C30H45F3N8O7

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC[C@](NC(C(C)C)=O)(C)C1=O)[C@H](NC([C@@H](NC([C@H](CCCNC(NC)=N)N1)=O)CC)=O)C2=CC=CC=C2.FC(C(O)=O)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: 98.67%

References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MM-589 TFA
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HY-100869A
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