| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
CTX-012414 targets KAT6A (lysine acetyltransferase 6A), also known as MOZ (monocytic leukemia zinc finger protein), a histone acetyltransferase that acetylates histone H3 at lysine 9 (H3K9) and is involved in transcriptional regulation. CTX-012414 is a KAT6A inhibitor with an IC50 of 0.49 µM and a KD of 0.38 µM. It has a sulfonylhydrazide skeleton.
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| ln Vitro |
In vitro, CTX-012414 inhibits KAT6A with an IC50 of 0.49 µM and a KD of 0.38 µM. The compound is a KAT6A inhibitor with a sulfonylhydrazide skeleton. It is used in pharmacological research as a selective modulator.
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| ln Vivo |
In vivo activity data for CTX-012414 are not extensively detailed in the available sources. The compound is a research tool for studying KAT6A function. Specific in vivo efficacy data in animal models have not been reported.
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| Enzyme Assay |
The in vitro enzyme assay for CTX-012414 involves measuring the inhibition of KAT6A acetyltransferase activity. Recombinant KAT6A is incubated with a histone substrate and acetyl-CoA in the presence of varying compound concentrations. The IC50 of 0.49 µM is determined by quantifying the reduction in histone acetylation using radioactive or fluorescence-based assays. The KD of 0.38 µM is determined by binding assays such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC).
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| Cell Assay |
Cellular assays for CTX-012414 are performed using cells treated with the compound. Histone H3K9 acetylation is assessed by Western blotting. Gene expression changes are assessed by RT-qPCR or RNA-seq. Cell proliferation and viability are measured using standard assays.
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| Animal Protocol |
In vivo animal studies for CTX-012414 are not detailed in the available sources. The compound is a research tool for studying KAT6A function. Specific animal models, dosing regimens, and efficacy data have not been reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for CTX-012414 are not available in the provided sources. The compound has a molecular weight of 344.36 g/mol and a molecular formula of C17H13FN2O3S. It is soluble in DMSO. Powder formulations should be stored at -20°C for up to 2 years.
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| Toxicity/Toxicokinetics |
Toxicity data for CTX-012414 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. The compound has been evaluated in biochemical and cellular assays, but specific toxicological profiles have not been characterized.
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| Additional Infomation |
CTX-012414 is a research compound for studying KAT6A function in epigenetic regulation. It is a KAT6A inhibitor with an IC50 of 0.49 µM. The compound has a sulfonylhydrazide skeleton. It is available from commercial suppliers for research use only.
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| Molecular Formula |
C17H13FN2O3S
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|---|---|
| Molecular Weight |
344.360126256943
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| Exact Mass |
344.063
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| Elemental Analysis |
C, 59.29; H, 3.81; F, 5.52; N, 8.14; O, 13.94; S, 9.31
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| CAS # |
423731-64-0
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| PubChem CID |
877350
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| Appearance |
Solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.651
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| LogP |
2.85
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
549
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=CC2C=CC=CC=2C=1)(NNC(C1C=CC=CC=1F)=O)(=O)=O
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| InChi Key |
CMGWGSMHPCWLOH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H13FN2O3S/c18-16-8-4-3-7-15(16)17(21)19-20-24(22,23)14-10-9-12-5-1-2-6-13(12)11-14/h1-11,20H,(H,19,21)
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| Chemical Name |
2-fluoro-N'-naphthalen-2-ylsulfonylbenzohydrazide
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| Synonyms |
CTX-0124143; CTX 0124143; CTX0124143;
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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 : ~125 mg/mL (~362.99 mM)
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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 | 2.9039 mL | 14.5197 mL | 29.0394 mL | |
| 5 mM | 0.5808 mL | 2.9039 mL | 5.8079 mL | |
| 10 mM | 0.2904 mL | 1.4520 mL | 2.9039 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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