2. Epigenetics
  3. Histone Methyltransferase
  4. MAK683

MAK683 is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.

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MAK683

MAK683 構造式

CAS 番号 : 1951408-58-4

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 157 在庫あり
Solution
10 mM * 1 mL in DMSO USD 157 在庫あり
Solid
5 mg $143 在庫あり
10 mg $264 在庫あり
25 mg $583 在庫あり
50 mg $869 在庫あり
100 mg $1265 在庫あり
200 mg   お問い合わせ  
500 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 MAK683:

MAK683 関連抗体

Top Publications Citing Use of Products

Histone Methyltransferase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

MAK683 is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay[1][2].

IC50 & Target

IC50: 59 nM (EED Alphascreen), 89 nM (LC-MS), 26 nM (ELISA)[1]
Cellular Effect
Cell Line Type Value Description References
KARPAS-422 GI50
4 3
Compound: 22
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
[PMID: 35352560]
KARPAS-422 IC50
3 1
Compound: 8; MAK683
Antiproliferative activity against human KARPAS-422 cells
Antiproliferative activity against human KARPAS-422 cells
[PMID: 35093670]
KARPAS-422 GI50
6 1
Compound: 1
Antiproliferative activity against human KARPAS-422 cells assessed as growth inhibition after 14 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human KARPAS-422 cells assessed as growth inhibition after 14 days by CellTiter-Glo luminescent cell viability assay
[PMID: 34807608]
KARPAS-422 GI50
6 1
Compound: 1
Antiproliferative activity against human KARPAS-422 cells assessed as growth inhibition after 14 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human KARPAS-422 cells assessed as growth inhibition after 14 days by CellTiter-Glo luminescent cell viability assay
[PMID: 34807608]
KARPAS-422 GI50
4 3
Compound: 22
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
[PMID: 35352560]
KARPAS-422 IC50
0.003 3
Compound: 44; MAK683
Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth incubated upto 14 days
Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth incubated upto 14 days
[PMID: 34351144]
KARPAS-422 GI50
4 3
Compound: 22
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
[PMID: 35352560]
KARPAS-422 GI50
6 1
Compound: 1
Antiproliferative activity against human KARPAS-422 cells assessed as growth inhibition after 14 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human KARPAS-422 cells assessed as growth inhibition after 14 days by CellTiter-Glo luminescent cell viability assay
[PMID: 34807608]
KARPAS-422 IC50
0.003 3
Compound: 44; MAK683
Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth incubated upto 14 days
Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth incubated upto 14 days
[PMID: 34351144]
KARPAS-422 IC50
3 1
Compound: 8; MAK683
Antiproliferative activity against human KARPAS-422 cells
Antiproliferative activity against human KARPAS-422 cells
[PMID: 35093670]
体外実験

MAK683 has antiproliferative activities in B cell lymphoma cell KARPAS422 after 14 days of treatment with an IC50 of 30 nM[1].

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

MAK683 関連抗体
臨床実験
分子量

376.39

分子式

C20H17FN6O
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC1=NC=CC=C1C2=CN=C(NCC3=C4CCOC4=CC=C3F)N5C2=NN=C5
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 40 mg/mL (106.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6568 mL 13.2841 mL 26.5682 mL
5 mM 0.5314 mL 2.6568 mL 5.3136 mL
10 mM 0.2657 mL 1.3284 mL 2.6568 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. 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: 2.17 mg/mL (5.77 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.17 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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% Corn Oil

    Solubility: ≥ 2.17 mg/mL (5.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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
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. 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 2.6568 mL 13.2841 mL 26.5682 mL 66.4205 mL
5 mM 0.5314 mL 2.6568 mL 5.3136 mL 13.2841 mL
10 mM 0.2657 mL 1.3284 mL 2.6568 mL 6.6420 mL
15 mM 0.1771 mL 0.8856 mL 1.7712 mL 4.4280 mL
20 mM 0.1328 mL 0.6642 mL 1.3284 mL 3.3210 mL
25 mM 0.1063 mL 0.5314 mL 1.0627 mL 2.6568 mL
30 mM 0.0886 mL 0.4428 mL 0.8856 mL 2.2140 mL
40 mM 0.0664 mL 0.3321 mL 0.6642 mL 1.6605 mL
50 mM 0.0531 mL 0.2657 mL 0.5314 mL 1.3284 mL
60 mM 0.0443 mL 0.2214 mL 0.4428 mL 1.1070 mL
80 mM 0.0332 mL 0.1661 mL 0.3321 mL 0.8303 mL
100 mM 0.0266 mL 0.1328 mL 0.2657 mL 0.6642 mL
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MAK683 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:

MAK6831951408-58-4MAK 683MAK-683Histone MethyltransferaseInhibitorinhibitorinhibit

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製品名:
MAK683
製品番号:
HY-103663
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