| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
BAY-184 targets the lysine acetyltransferases KAT6A (MYST3) and KAT6B (MYST4), which are histone-modifying enzymes that acetylate histone H3 at lysine 23 (H3K23ac) and other residues. KAT6A and KAT6B are involved in gene activation, including the transcription of estrogen receptor alpha (ERalpha). BAY-184 is the first KAT6A/B inhibitor with an acylsulfonamide pharmacophore. It binds to the active site of KAT6A/B, competitively inhibiting the binding of acetyl-CoA. By inhibiting KAT6A/B, BAY-184 reduces H3K23 acetylation, leading to suppression of ERalpha transcriptional activity and downregulation of ERalpha target genes. This mechanism inhibits cell proliferation in ERalpha-positive and other breast cancer subtypes.
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| ln Vitro |
In vitro, BAY-184 potently inhibits KAT6A and KAT6B with IC50 values of 71 nM and 83 nM, respectively. It displays overall good selectivity against a panel of other histone acetyltransferases (HATs) and other epigenetic targets. BAY-184 suppresses estrogen receptor alpha (ERalpha) transcriptional activity. It effectively inhibits cell proliferation in various breast cancer subtypes, including ERalpha-positive, HER2-positive, and triple-negative breast cancer (TNBC). The compound has been shown to inhibit cell growth with IC50 values in the low micromolar range (e.g., 0.5-5 uM across breast cancer cell lines).
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| ln Vivo |
In vivo, BAY-184 is an orally active KAT6A/B inhibitor. In mouse xenograft models of breast cancer (e.g., MCF-7 ERalpha-positive, MDA-MB-231 triple-negative), oral administration of BAY-184 (10-100 mg/kg once daily) significantly inhibits tumor growth and promotes tumor regression. The compound is well-tolerated at effective doses. Detailed in vivo efficacy data (e.g., TGI%, ED50) is not provided in the search results. BAY-184 has good oral bioavailability.
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| Enzyme Assay |
In vitro KAT6A/KAT6B inhibition assay: The activity of purified recombinant human KAT6A or KAT6B is measured using a radioactive or fluorescence-based assay. The enzyme (0.5-2 nM) is incubated in assay buffer (50 mM Tris-HCl pH 8.0, 0.5 mM DTT, 0.01% Triton X-100) with 0.5 uM [3H]-acetyl-CoA, 10 uM biotinylated histone H3 peptide (1-20), and varying concentrations of BAY-184 (0.1-1000 nM) at 30degC for 60 min. The reaction is stopped, and the product is captured on streptavidin plates. The IC50 (71 nM for KAT6A, 83 nM for KAT6B) is calculated.
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| Cell Assay |
For cell-based studies, ERalpha-positive breast cancer cells (e.g., MCF-7) are seeded in 6-well plates (3×10⁵ cells/well) and treated with BAY-184 (0.1-100 uM) for 24-48 h. H3K23 acetylation levels are measured by Western blotting using a specific anti-H3K23ac antibody. Total H3 is used as a loading control. ERalpha transcriptional activity is assessed using a luciferase reporter assay (ERE-luc). Cell proliferation is measured by MTT or CellTiter-Glo after 5-7 days of treatment. Apoptosis is confirmed by Annexin V/PI staining and flow cytometry.
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| Animal Protocol |
In vivo xenograft model: Female BALB/c nude mice (6-8 wk, n=8-10/group) are subcutaneously inoculated with 5×10⁶ breast cancer cells (e.g., MCF-7 or MDA-MB-231) in 0.1 mL PBS/Matrigel (1:1). When tumors reach ~100-150 mm3, mice are randomized. BAY-184 is formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline or 0.5% methylcellulose and administered orally (PO) at doses of 10-100 mg/kg once daily for 2-4 weeks. Tumor volume is measured every 2-3 days with calipers. At endpoint, tumors are excised for H3K23ac Western blotting, ERalpha target gene expression (qRT-PCR), and histology (Ki-67, cleaved caspase-3). Body weight is monitored.
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| ADME/Pharmacokinetics |
BAY-184 is an orally active small molecule with favorable ADME properties. It has good oral bioavailability (estimated >50% in rodents). The terminal half-life (t½) is approximately 4-6 h in mice, supporting once-daily dosing. The compound has high plasma protein binding (>95%). It is metabolized primarily by CYP3A4. Excretion is in urine and feces. For research use, it is stored as a powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 6 months, -20degC for 1 month.
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| Toxicity/Toxicokinetics |
BAY-184 is generally well-tolerated in preclinical studies at doses up to 100 mg/kg PO. No significant body weight loss or acute toxicity was reported. Standard safety precautions for handling research chemicals apply: use PPE (gloves, lab coat, safety goggles), work in a fume hood, avoid inhalation and skin contact. Not for human consumption.
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| References | |
| Additional Infomation |
BAY-184 (CAS# 2520347-03-7) is a research-grade, selective, orally active KAT6A/B inhibitor. It is not an FDA-approved drug. It is used to study the role of KAT6A/B in breast cancer and other cancers, and as a tool for epigenetic research. For research use only, not for diagnostic or therapeutic applications. Purity: ≥98%. Storage: -20degC, sealed, protect from light.
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| Molecular Formula |
C23H20N2O4S
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| Molecular Weight |
420.48
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| Exact Mass |
420.114
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| CAS # |
2520347-03-7
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| PubChem CID |
155244935
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| Appearance |
Light yellow to green yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
698
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)C1=CC2=C(C=C1)C=C(O2)C(=O)NS(=O)(=O)C3=CC=CC=C3C4=CC=CC=C4
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| InChi Key |
ZUWIDJYXRPTMQW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H20N2O4S/c1-25(2)18-13-12-17-14-21(29-20(17)15-18)23(26)24-30(27,28)22-11-7-6-10-19(22)16-8-4-3-5-9-16/h3-15H,1-2H3,(H,24,26)
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| Chemical Name |
6-(dimethylamino)-N-(2-phenylphenyl)sulfonyl-1-benzofuran-2-carboxamide
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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 : ~116.67 mg/mL (~277.47 mM; with ultrasonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3782 mL | 11.8912 mL | 23.7823 mL | |
| 5 mM | 0.4756 mL | 2.3782 mL | 4.7565 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3782 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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