2. Epigenetics
  3. WDR5
  4. MM-102 TFA

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

製品番号: HY-12220A 純度: 99.68%
COA 取扱説明書 Technical Support

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.

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MM-102 TFA

MM-102 TFA 構造式

CAS 番号 : 1883545-52-5

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 228 在庫あり
Solution
10 mM * 1 mL in DMSO USD 228 在庫あり
Solid
2 mg $60 在庫あり
5 mg $132 在庫あり
10 mg $216 在庫あり
50 mg $912 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of MM-102 TFA:

MM-102 TFA 関連抗体

Top Publications Citing Use of Products

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製品説明

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].
体外実験

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].

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

MM-102 TFA 関連抗体
分子量

783.83

分子式

C37H50F5N7O6
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1(NC([C@@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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

DMSO : ≥ 100 mg/mL (127.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.68%

COA (251 KB) HNMR (325 KB) LCMS (90 KB) Elemental Analysis Report (110 KB)

取扱説明書 (2659 KB)
参考文献
細胞実験

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.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2758 mL 6.3789 mL 12.7579 mL 31.8947 mL
5 mM 0.2552 mL 1.2758 mL 2.5516 mL 6.3789 mL
10 mM 0.1276 mL 0.6379 mL 1.2758 mL 3.1895 mL
15 mM 0.0851 mL 0.4253 mL 0.8505 mL 2.1263 mL
20 mM 0.0638 mL 0.3189 mL 0.6379 mL 1.5947 mL
25 mM 0.0510 mL 0.2552 mL 0.5103 mL 1.2758 mL
30 mM 0.0425 mL 0.2126 mL 0.4253 mL 1.0632 mL
40 mM 0.0319 mL 0.1595 mL 0.3189 mL 0.7974 mL
50 mM 0.0255 mL 0.1276 mL 0.2552 mL 0.6379 mL
60 mM 0.0213 mL 0.1063 mL 0.2126 mL 0.5316 mL
80 mM 0.0159 mL 0.0797 mL 0.1595 mL 0.3987 mL
100 mM 0.0128 mL 0.0638 mL 0.1276 mL 0.3189 mL
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MM-102 TFA Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

Keywords:

MM-1021883545-52-5HMTase Inhibitor IXMM102MM 102WDR5WD repeat protein-5WD40 repeat domain protein 5Inhibitorinhibitorinhibit

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