MAK683
Based on 5 publication(s) in Google Scholar
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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- Purity: 99.02%
- CAS No.: 1951408-58-4
- 화학식: C20H17FN6O
- 분자량:376.39
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MAK683
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
IC50: 59 nM (EED Alphascreen), 89 nM (LC-MS), 26 nM (ELISA)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-422 | GI50 |
4 μM
Compound: 22
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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
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[PMID: 35352560] |
| KARPAS-422 | GI50 |
6 nM
Compound: 1
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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
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[PMID: 34807608] |
| KARPAS-422 | IC50 |
0.003 μM
Compound: 44; MAK683
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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
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[PMID: 34351144] |
| KARPAS-422 | IC50 |
3 nM
Compound: 8; MAK683
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Antiproliferative activity against human KARPAS-422 cells
Antiproliferative activity against human KARPAS-422 cells
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[PMID: 35093670] |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1951408-58-4
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Appearance Solid
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분자량 376.39
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화학식 C20H17FN6O
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Color White to off-white
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SMILES
CC1=NC=CC=C1C2=CN=C(NCC3=C4CCOC4=CC=C3F)N5C2=NN=C5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Allosteric Inhibition of Polycomb Repressive Complex 2 by an EZH2-Selective Small Molecule Inhibitor. [Abstract]2026 Jun 18:e76025. PMID: 42314051 -
Cell Death Dis
Induction of senescence-associated secretory phenotype underlies the therapeutic efficacy of PRC2 inhibition in cancer. [Abstract]2022 Feb 15;13(2):155. PMID: 35169119 -
Commun Biol
2025 Feb 11;8(1):215. PMID: 39934221 -
J Biol Chem
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. [Abstract]2024 Oct;300(10):107765. PMID: 39276936 -
bioRxiv
Dual EZH1/2 inhibition enhances DNMT inhibitor efficacy in colon cancer through targeting H3K27me1. [Abstract]2025 Sep 18:2025.09.16.676613. PMID: 41000734
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
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 |
MAK683 Related Classifications
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