| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
YUKA1 targets Lysine demethylase 5A (KDM5A/RBP2/JARID1A), a histone demethylase that removes methyl groups from histone H3 lysine 4 (H3K4me3). It is a potent and cell-permeable inhibitor of KDM5A. YUKA1 has less inhibitory activity on KDM5C and is inactive on KDM5B, KDM6A, or KDM6B.
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| ln Vitro |
YUKA1 is a potent inhibitor of KDM5A with an IC50 of 2.66 μM. It has less inhibitory activity on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A, or KDM6B. YUKA1 increases H3K4me3 levels in human cells and selectively inhibits the proliferation of cancer cells associated with KDM5A. It inhibits drug resistance and cancer cell growth in HeLa cervical cancer cells and ZR-75-1 breast cancer cells.
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| ln Vivo |
Specific in vivo activity data for YUKA1 are not extensively reported in the available literature. As a KDM5A inhibitor with anticancer activity, it is expected to exhibit efficacy in preclinical models of cancer. YUKA1 inhibits drug resistance and cancer cell growth in HeLa cervical cancer cells and ZR-75-1 breast cancer cells. Further research is needed to characterize its pharmacokinetic and pharmacodynamic profiles in animal models.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for YUKA1 typically involves measuring its inhibitory activity against KDM5A using a standard demethylase assay. The compound is incubated with the enzyme and a histone H3 peptide substrate, and the demethylation activity is measured. The IC50 value is determined from the dose-response curve.
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| Cell Assay |
The in vitro cellular assay for YUKA1 typically involves culturing cancer cell lines such as HeLa or ZR-75-1 in appropriate growth media. Cells are treated with varying concentrations of the compound, and H3K4me3 levels are measured using Western blotting or ELISA. Cell proliferation, viability, and apoptosis are assessed using standard assays such as MTT or flow cytometry.
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| Animal Protocol |
In vivo animal studies for YUKA1 would typically involve the use of mouse xenograft models bearing human tumors. Tumor-bearing mice would be administered the compound via appropriate routes (e.g., oral gavage or intraperitoneal injection) at various dose levels. Tumor growth inhibition would be monitored over several weeks, and endpoints would include tumor volume measurements, body weight changes, and histopathological analysis of tumor tissues.
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| ADME/Pharmacokinetics |
YUKA1 has a molecular weight of 264.30 g/mol and a molecular formula of C11H12N4O2S. The IUPAC name is 4-[(3-methoxy-2-prop-2-enoxyphenyl)methylamino]-1H-1,2,4-triazole-5-thione. The compound is soluble in DMSO and other organic solvents. Further detailed physicochemical properties are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Specific toxicology data for YUKA1 are not available in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application. Researchers should consult the safety data sheet for detailed handling and disposal information.
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| References | |
| Additional Infomation |
YUKA1 is a potent and cell-permeable Lysine demethylase 5A (KDM5A) inhibitor with an IC50 of 2.66 μM. It has less inhibitory activity on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A, or KDM6B. YUKA1 increases H3K4me3 levels in human cells and selectively inhibits the proliferation of cancer cells associated with KDM5A. It has not yet entered clinical trials and is strictly for preclinical research purposes.
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| Molecular Formula |
C13H16N4O2S
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|---|---|
| Molecular Weight |
292.356740951538
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| Exact Mass |
292.099
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| CAS # |
708991-09-7
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| PubChem CID |
2215170
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| Appearance |
White to off-white solid powder
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| LogP |
1.8
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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 |
7
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| Heavy Atom Count |
20
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| Complexity |
377
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=CN(NCC2=CC=CC(OC)=C2OCC=C)C(=S)N1
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| InChi Key |
NHJCZZWENDYDEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H16N4O2S/c1-3-7-19-12-10(5-4-6-11(12)18-2)8-15-17-9-14-16-13(17)20/h3-6,9,15H,1,7-8H2,2H3,(H,16,20)
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| Chemical Name |
4-[(3-methoxy-2-prop-2-enoxyphenyl)methylamino]-1H-1,2,4-triazole-5-thione
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| Synonyms |
YUKA1; YUKA 1; YUKA-1
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~342.04 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 | 3.4204 mL | 17.1022 mL | 34.2044 mL | |
| 5 mM | 0.6841 mL | 3.4204 mL | 6.8409 mL | |
| 10 mM | 0.3420 mL | 1.7102 mL | 3.4204 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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