| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
KAT6A (lysine acetyltransferase 6A, also known as MOZ) and KAT6B (lysine acetyltransferase 6B, also known as MYST4 or MORF). WM-2474 is an inactive analog of the KAT6A/KAT6B inhibitor WM-1119, with an IC50 value >125 μM against KAT6B, confirming its lack of inhibitory activity at relevant concentrations.
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| ln Vitro |
In vitro, WM-2474 shows no inhibitory activity against KAT6A or KAT6B, with an IC50 value >125 μM for KAT6B. It does not affect cell proliferation, confirming its suitability as a negative control for WM-1119 and related KAT6A/B inhibitors. This inactivity allows researchers to distinguish between on-target effects of active inhibitors and non-specific cellular responses.
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| ln Vivo |
In vivo activity data for WM-2474 are not applicable as the compound is specifically designed as an inactive control. It is not expected to produce any pharmacological effects in animal models. Its primary use is as a negative control in in vitro and in vivo studies to validate that observed effects are specifically attributable to KAT6A/B inhibition by the active compound WM-1119.
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| Enzyme Assay |
KAT6A and KAT6B inhibitory activity is measured using a histone acetyltransferase (HAT) activity assay. Recombinant KAT6A or KAT6B enzymes are incubated with acetyl-CoA and a histone peptide substrate in the presence of varying concentrations of WM-2474 or WM-1119. The incorporation of acetyl groups is detected by scintillation counting or fluorescence, and IC50 values are calculated. WM-2474 shows IC50 >125 μM.
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| Cell Assay |
Cells are treated with WM-2474 at concentrations matching those used for WM-1119 (typically up to 10-50 µM) for 48-72 hours. Cell proliferation is assessed using CellTiter-Glo, MTT, or BrdU incorporation assays. The lack of effect on cell proliferation confirms that WM-2474 serves as an appropriate negative control, and any antiproliferative effects observed with WM-1119 are attributable to KAT6A/B inhibition.
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| Animal Protocol |
Not applicable for WM-2474 as it is an inactive control compound. In studies evaluating WM-1119 in vivo, WM-2474 may be administered as a negative control at equivalent doses to confirm that any antitumor effects observed with WM-1119 are specifically due to KAT6A/B inhibition rather than off-target effects or vehicle-related artifacts.
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| ADME/Pharmacokinetics |
WM-2474 has molecular formula C17H13FN4O3S and molecular weight 372.07. It is soluble in DMSO (>128.8 mg/mL) but insoluble in ethanol and water. The compound is supplied as a powder and should be stored at 2-8°C or -20°C. As an inactive control, pharmacokinetic parameters are not typically characterized since the compound is not intended for therapeutic use.
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| Toxicity/Toxicokinetics |
No toxicity data are specifically reported for WM-2474 as it is an inactive control compound. The compound is classified as Eye Irritant Category 2 and Skin Irritant Category 2 (Hazard Classifications). Standard laboratory safety precautions should be followed when handling. It is not intended for human or veterinary use.
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| References |
[1]. Inhibitors of histone
acetyltransferases KAT6A/B induce senescence and arrest tumour growth.
Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub
2018 Aug 1.
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| Additional Infomation |
WM-2474 (also known as MOZ-IN-2) is an acylsulfonohydrazide derivative and an inactive analog of WM-8014/WM-1119. It is used as a negative control compound in studies of MYST family histone acetyltransferases KAT6A and KAT6B. The compound has CAS number 2055397-88-9 (not to be confused with the alternative CAS mentioned in some sources). It is for research use only, with no clinical or FDA approval.
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| Appearance |
Typically exists as solid 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
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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