| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
12.1μM (lysine acetyltransferase 8, KAT8)[1]
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| ln Vitro |
In HT29 cells, MC4033 (25, 50, 100, and 200 μM, for 72 hours) decreased the expression level of H4K16Ac, suggesting that it can suppress the expression level of KAT8 in cells [1]. The IC50 values of MC4033 in HCT116, H1299, A549, and U937 cells were found to be 39.4 μM, 52.1 μM, 41 μM, and 30.1 μM, in that order[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HT29, HCT116, HeLa, H1299, A549, H460, MCF7, U937, and U251 cells Tested Concentrations: 10, 25, 50, and 100 μM Incubation Duration: 72 h Experimental Results: Displayed dose-dependent antiproliferative effects in HCT116, H1299, A549, and U937 cell lines. The inhibition rate of cell proliferation was 70% at 50 μM and >80 % at 100 μM in U937 cells. Cell Cycle Analysis[1] Cell Types: HT29, HCT116, and HeLa cells Tested Concentrations: 50 μM and 100 μM Incubation Duration: 72 h Experimental Results: Propidium iodide (PI) staining demonstrated a slight increase in the percentage of cells with DNA hypodiploid peak, indicative of apoptosis. RT-PCR[1] Cell Types: HCT116 cells Tested Concentrations: 100 μM Incubation Duration: 48h Experimental Results: decreased the mRNA levels of oncogenes UCP2. Immunofluorescence[1] Cell Types: HT29 cells Tested Concentrations: 50 μM Incubation Duration: 24 h Experimental Results: decreased H4K16Ac signal intensity by 80%. Western Blot Analysis[1] Cell Types: HCT116 cells Tested Concentrations: 0,10, 25, 50,100 μM Incubation Duration: 48 h Experimental Results: demonstrated that the altered ratio of LC3-II/-I and the regulation of p62 autophagy markers indicated the activation of autophagy in HCT116 cells. Apoptosis Analysis[1] Cell Types: HCT116 cells Tested Concentrations: 100 μM or 10 μM (MC4033/CQ) Incubation Duration: 72 h Experimental Results: demonstrated that exposure of HCT116 cells to CQ increased the apoptotic effect of KAT8i. |
| References |
[1]. Fiorentino F, et al. First-in-Class Selective Inhibitors of the Lysine Acetyltransferase KAT8. J Med Chem. 2023 May 25;66(10):6591-6616
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| Molecular Formula |
C16H13N3O3
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|---|---|
| Molecular Weight |
295.29
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| CAS # |
28532-21-0
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~338.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3865 mL | 16.9325 mL | 33.8650 mL | |
| 5 mM | 0.6773 mL | 3.3865 mL | 6.7730 mL | |
| 10 mM | 0.3387 mL | 1.6933 mL | 3.3865 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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