[CAS NO. 1442106-11-7] MM-401 TFA
PRODUCTS SPECIFICATIONS [1442106-11-7]
DESCRIPTION [1442106-11-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 700.75 |
| Molecular Formula | C31H47F3N8O7 |
| SMILES | C[C@@](C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@@]1(C2=CC=CC=C2)[H])=O)CC)=O)=O)(NC(C(C)C)=O)CCCCNC1=O.O=C(O)C(F)(F)F |
Summary
IC50 & Target
Ki: < 1 nM (WDR5); IC50: 0.9 nM (WDR5-MLL1 interaction), 0.32 µM (MLL1) [1] .
In Vitro
MM-401 maintains high binding affinity to WDR5 with a K
i
value of < 1 nM and disrupts WDR5-MLL1 interaction with an IC
50
value of 0.9 nM
[1]
.
MM-401 is able to specifically inhibit MLL1 activity (IC
50
value of 0.32µM) by blocking MLL1-WDR5 interaction and thus the complex assembly
[1]
.
MM-401 (20 μM; 48 h) specifically inhibits MLL1-dependent H3K4 methylation in cells
[1]
.
MM-401 induces similar changes in MLL-AF9 transcriptome as the MLL1 deletion
[1]
.
MM-401 (10, 20, 40 μM; 48 h) specifically inhibits growth of MLL leukemia cells by inducing cell cycle arrest, apoptosis
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [1]
| Cell Line: | Murine MLL-AF9 and Hoxa9/Meis1 cells |
| Concentration: | 10, 20, 40 μM |
| Incubation Time: | 48 h |
| Result: | Specifically induced apoptosis of MLL-AF9 cells. |
Cell Cycle Analysis [1]
| Cell Line: | Murine MLL-AF9 and Hoxa9/Meis1 cells |
| Concentration: | 10, 20, 40 μM |
| Incubation Time: | 48 h |
| Result: | Induced prominent G1/S arrest in MLL-AF9 cells in a concentration dependent manner. |
RT-PCR [1]
| Cell Line: | MLL-AF9 cells |
| Concentration: | 20 μM |
| Incubation Time: | 48 h |
| Result: | Significantly decreased H3K4me, expression of 5 Hox A genes, especially Hoxa9 and Hoxa10. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL ( 142.70 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.4270 mL | 7.1352 mL | 14.2704 mL |
| 5 mM | 0.2854 mL | 1.4270 mL | 2.8541 mL |
| 10 mM | 0.1427 mL | 0.7135 mL | 1.4270 mL |