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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
12.1μM (lysine acetyltransferase 8, KAT8)[1]
MC4033 targets lysine acetyltransferase 8 (KAT8), also known as MYST1. KAT8 is a histone acetyltransferase that acetylates histone H4 at lysine 16 (H4K16Ac). By inhibiting KAT8 with an IC50 of 12.1 μM, MC4033 reduces the level of H4K16Ac in cells, thereby modulating gene expression and inducing apoptosis in cancer cells. |
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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].
In vitro, MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells. It shows significant biological activity in various cancer cell lines. MC4033 induces apoptosis and has anticancer effects. It is a selective and reversible inhibitor of KAT8. |
| ln Vivo |
In vivo data for MC4033 is not extensively reported in publicly available sources. As a selective KAT8 inhibitor with anticancer effects in vitro, the compound has potential applications in animal models of non-small cell lung cancer and other cancers. However, specific published in vivo efficacy studies are not detailed in the current literature. MC4033 is primarily used as a research tool for studying KAT8 biology and cancer.
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| Enzyme Assay |
The in vitro KAT8 inhibition assay for MC4033 uses recombinant KAT8 enzyme and a histone H4 peptide substrate. Enzyme activity is measured by quantifying the acetylation of the substrate using radioactive or fluorescence-based methods. The compound is added at various concentrations, and IC50 values are calculated from dose-response curves. Selectivity profiling against other histone acetyltransferases is performed to confirm specificity.
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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. Cellular assays for MC4033 are conducted in cancer cell lines such as HT29, HCT116, H1299, A549, and U937 cells. Cells are treated with varying concentrations of MC4033 (e.g., 25, 50, 100, and 200 μM) for up to 72 hours. H4K16Ac levels are measured by Western blotting. Cell viability and proliferation are measured using standard assays such as MTT or CellTiter-Glo. Apoptosis is assessed by flow cytometry using Annexin V/PI staining. |
| Animal Protocol |
In vivo studies for MC4033 would typically involve xenograft mouse models of non-small cell lung cancer or other cancers. The compound would be administered via oral or intraperitoneal routes. Efficacy would be assessed by measuring tumor growth inhibition. Pharmacodynamic markers such as H4K16Ac levels in tumor tissues would be evaluated to confirm target engagement. However, specific published in vivo protocols for MC4033 are not available.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MC4033 is not extensively reported in publicly available sources. The compound has a molecular weight of 295.29 and a molecular formula of C16H13N3O3. It has a CAS number of 28532-21-0. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for MC4033 is limited. As with all research compounds, MC4033 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
MC4033 (CAS 28532-21-0) is a selective and reversible inhibitor of lysine acetyltransferase 8 (KAT8) with an IC50 of 12.1 μM. It has anticancer effects and induces apoptosis. MC4033 can be used for the study of non-small cell lung cancer. It has a molecular formula of C16H13N3O3 and a molecular weight of 295.29. It is for research use only.
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| Molecular Formula |
C16H13N3O3
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|---|---|
| Molecular Weight |
295.292723417282
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| Exact Mass |
295.095
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| CAS # |
28532-21-0
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| PubChem CID |
169492942
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
533
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC\1=NN(C(=O)/C1=C\C2=CC=CN2)C3=CC=C(C=C3)C(=O)O
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| InChi Key |
WBHVGUYXAZIVHV-ZROIWOOFSA-N
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| InChi Code |
InChI=1S/C16H13N3O3/c1-10-14(9-12-3-2-8-17-12)15(20)19(18-10)13-6-4-11(5-7-13)16(21)22/h2-9,17H,1H3,(H,21,22)/b14-9-
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| Chemical Name |
4-[(4Z)-3-methyl-5-oxo-4-(1H-pyrrol-2-ylmethylidene)pyrazol-1-yl]benzoic acid
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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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