MOZ-IN-3
Based on 1 Customer Validation
MOZ-IN-3 is an orally active KAT6A (MOZ) inhibitor with an IC50 of 0.03 μM against human targets, and it exhibits high selectivity over other MYST family histone acetyltransferases. MOZ-IN-3 modulates monocyte function, exerts anti-tumor effects, increases the nucleocytoplasmic ratio, and enhances cellular resistance to chemotherapeutic drug-induced cell death. MOZ-IN-3 is applicable to leukemia-related research.
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- Pureté: 98.75%
- CAS No.: 3059058-07-7
- Formule: C17H13FN2O3S
- Masse moléculaire:344.36
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
MOZ/MORF 0.03 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
0.197 μM
Compound: 6j
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Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 37651878] |
| K562 | IC50 |
0.082 μM
Compound: 6j
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Cytotoxicity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 37651878] |
| U-937 | IC50 |
0.162 μM
Compound: 6j
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Cytotoxicity against human U-937 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human U-937 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 37651878] |
In Vitro
MOZ-IN-3 (compound 6j) (2-fold serial dilutions starting at 10 μM; 20 min pre-incubation, 4 h total reaction) potently inhibits recombinant human KAT6A catalytic domain activity with an IC50 of 0.03 μM[1].
MOZ-IN-3 (compound 6j) (0.05-0.8 μM for HL-60, U937, K562; 0.2-3.2 μM for SKNO-1; 48 h) exhibits potent cytotoxicity against HL-60, U937, SKNO-1, and K562 human leukemia cell lines, with the strongest activity in K562 cells (IC50 = 0.082 μM) after 48 h of treatment[1].
MOZ-IN-3 (3 μM; 15 days pretreatment) blocks phorbol myristate acetate/1,25(OH)2-VitD3-induced differentiation and enhances chemoresistance in U937 monocytic acute myeloid leukemia cells[2].
MOZ-IN-3 (3 μM; 0-14 days) treatment increases miR-223 and MOZ expression in U937 monocytic acute myeloid leukemia cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human leukemia cell lines HL-60, U937, SKNO-1, K562
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Concentration:0.05, 0.1, 0.2, 0.4, 0.8 μM (HL-60, U937, K562); 0.2, 0.4, 0.8, 1.6, 3.2 μM (SKNO-1)
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Incubation Time:48 h
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Result:Demonstrated potent anti-leukemia cytotoxicity with IC50 values of 0.197 μM (HL-60), 0.162 μM (U937), 1.846 μM (SKNO-1), and 0.082 μM (K562).
Showed the lowest IC50 in K562 cells.
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Cell Line:U937 monocytic acute myeloid leukemia cells
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Concentration:3 μM
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Incubation Time:0, 1, 2, 4, 7, 14 days
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Result:Increased miR-223 expression over time.
Showed a corresponding increase in MOZ expression over the same time period.
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Cell Line:MCF-7 breast cancer cells
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Concentration:0.1, 1, 10, 30 μM
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Incubation Time:24 h
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Result:Showed no measurable effects on MYST-dependent histone acetylation biomarkers, including H3K23Ac (KAT6A/B), H3K14Ac (KAT7), and H4K16Ac (KAT8), at any tested concentration.
Parmacokinetics
In Vivo
MOZ-IN-3 (10-20 mg/kg; p.o., i.v.; single dose) exhibits favorable pharmacokinetic properties in male SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:embryos (4 nL of cells suspension containing 400 labeled cells was microinjected into the yolk of anesthetized embryos)[1]
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Dosage:1 μM; 5 μM; 10 μM
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Administration:exposure via aquatic media
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Result:Decreased tumor area compared to the control group.
Showed the greatest reduction in tumor area at 10 μM dose.
Demonstrated dose-dependent suppression of K562 cell proliferation in zebrafish xenografts.
Chemical Information
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CAS No. 3059058-07-7
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Appearance Solid
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Masse moléculaire 344.36
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Formule C17H13FN2O3S
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Color White to off-white
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SMILES
FC1=C(C(CNS(=O)(C2=CC=CC3=C2N=CC=C3)=O)=O)C=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : ≥ 200 mg/mL (580.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 20 mg/mL (58.08 mM); Clear solution
This protocol yields a clear solution of ≥ 20 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (200.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 20 mg/mL (58.08 mM); Clear solution
This protocol yields a clear solution of ≥ 20 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (200.0 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:
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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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Duan Y, et al. Discovery of N-(2-oxoethyl) sulfanilamide-derived inhibitors of KAT6A (MOZ) against leukemia by an isostere strategy. European journal of medicinal chemistry. 2023 Nov 15;260:115770. [Content Brief]
[2]. Jiang M, et al. MOZ Forms an Autoregulatory Feedback Loop with miR-223 in AML and Monocyte/Macrophage Development. iScience. 2019 Jan 25;11:189-204. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9039 mL | 14.5197 mL | 29.0394 mL | 72.5984 mL |
| 5 mM | 0.5808 mL | 2.9039 mL | 5.8079 mL | 14.5197 mL | |
| 10 mM | 0.2904 mL | 1.4520 mL | 2.9039 mL | 7.2598 mL | |
| 15 mM | 0.1936 mL | 0.9680 mL | 1.9360 mL | 4.8399 mL | |
| 20 mM | 0.1452 mL | 0.7260 mL | 1.4520 mL | 3.6299 mL | |
| 25 mM | 0.1162 mL | 0.5808 mL | 1.1616 mL | 2.9039 mL | |
| 30 mM | 0.0968 mL | 0.4840 mL | 0.9680 mL | 2.4199 mL | |
| 40 mM | 0.0726 mL | 0.3630 mL | 0.7260 mL | 1.8150 mL | |
| 50 mM | 0.0581 mL | 0.2904 mL | 0.5808 mL | 1.4520 mL | |
| 60 mM | 0.0484 mL | 0.2420 mL | 0.4840 mL | 1.2100 mL | |
| 80 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL | 0.9075 mL | |
| 100 mM | 0.0290 mL | 0.1452 mL | 0.2904 mL | 0.7260 mL |
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