1. Epigenetics
  2. Histone Methyltransferase
  3. MM-102 TFA

MM-102 TFA (Synonyms: HMTase Inhibitor IX TFA)

Cat. No.: HY-12220A Purity: 99.77%
Handling Instructions

MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.

For research use only. We do not sell to patients.

MM-102 TFA Chemical Structure

MM-102 TFA Chemical Structure

CAS No. : 1883545-52-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 186 In-stock
Estimated Time of Arrival: December 31
2 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 912 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.

IC50 & Target

IC50: 2.4 nM (MLL)[1].

In Vitro

MM-102 (HMTase Inhibitor IX) inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins.
MM-102 (TFA), with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay withIC50=0.4-0.9 μM[1].
MM-102 (HMTase Inhibitor IX) dose-dependently inhibits cell growth in the MV4;11 and KOPN8 leukemia cell lines, which carry MLL1-AF4 and MLL1-ENL fusion proteins, respectively[1].
MM-102 (HMTase Inhibitor IX) has IC50=25 μM in both cell lines and completely inhibits cell growth in these cell lines at 75 μM[1].
MM-102 (HMTase Inhibitor IX) effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins and has minimal effect in leukemia cells with wild-type MLL1 protein[1].

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

Molecular Weight

783.83

Formula

C₃₇H₅₀F₅N₇O₆

CAS No.

1883545-52-5

SMILES

O=C(C1(NC([[email protected]@H](NC(C(NC(C(C)C)=O)(CC)CC)=O)CCCNC(N)=N)=O)CCCC1)NC(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3.FC(F)(F)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (127.58 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2758 mL 6.3789 mL 12.7579 mL
5 mM 0.2552 mL 1.2758 mL 2.5516 mL
10 mM 0.1276 mL 0.6379 mL 1.2758 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.19 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.19 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay

MV4;11, KOPN8, and K562 cells were cultured in RPMI 1640 medium (ATCC) supplemented with 10% fetal bovine serum and 100 U/L penicillinstreptomycin and incubated at 37°C under 5% CO2. Cells were seeded into 12-well plates for suspension at a density of 5 × 105 per well (1 mL) and treated with either vehicle control (DMSO, 0.2%) or MM-102 (HMTase Inhibitor IX) for 7 days. The medium was changed every 2 days, and compounds were resupplied. The CellTiter-Glo Luminescent Cell Viability Assay kit was used. First, 100 μL of the assay reagent was added into each well, and the content was mixed for 2 min on an orbital shaker to induce cell lysis. After 10 min incubation at room temperature, the luminescence was read on a microplate reader.

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

References

Purity: 99.77%

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Keywords:

MM-102HMTase Inhibitor IXMM102MM 102Histone MethyltransferaseInhibitorinhibitorinhibit

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MM-102 TFA
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