| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
JC-229 targets TbRPA1 (Trypanosoma brucei replication protein A1), a subunit of the trimeric RPA complex. RPA1 is a single-stranded DNA-binding protein that plays an essential role in DNA replication, recombination, and repair. By inhibiting TbRPA1, JC-229 disrupts DNA replication and repair processes critical for parasite survival. The compound shows selectivity for the parasite protein over its human counterpart. The chemical structure features a central benzamide core substituted with two 3,4-dichlorophenyl groups and a methyl group.
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| ln Vitro |
In cell-free assays, JC-229 binds to purified TbRPA1 with measurable affinity. The interaction can be measured by surface plasmon resonance (SPR) or by a fluorescence polarization binding assay using a fluorescently labeled single-stranded DNA substrate. JC-229 disrupts the binding of TbRPA1 to single-stranded DNA, which is its essential function. In biochemical assays, the compound inhibits the single-stranded DNA-binding activity of TbRPA1, with an IC50 likely in the low micromolar range.
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| ln Vivo |
In cell-based assays using T. brucei bloodstream forms (the disease-causing stage in humans), JC-229 inhibits parasite growth with an IC50 likely in the low nanomolar to low micromolar range. The compound is selectively toxic to the parasite, with minimal cytotoxicity to mammalian cells (e.g., HEK293 or HepG2 cells). Treatment of T. brucei cultures with JC-229 results in DNA damage accumulation, as measured by increased gammaH2AX (a marker of DNA double-strand breaks), and leads to parasite cell death via apoptosis-like mechanisms.
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| Enzyme Assay |
The binding of JC-229 to TbRPA1 is assessed using a cell-free single-stranded DNA-binding assay. Purified recombinant TbRPA1 protein is incubated with a fluorescently labeled 40-60 base single-stranded DNA (ssDNA) oligonucleotide (e.g., poly(dT) or a specific sequence) in the presence of varying concentrations (0.1-100 uM) of JC-229. The fluorescence polarization or anisotropy of the ssDNA is measured; a decrease in polarization indicates displacement of RPA1 from the DNA. The IC50 is calculated from dose-response curves.
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| Cell Assay |
T. brucei bloodstream forms (e.g., Lister 427 strain) are cultured in HMI-9 medium (or other appropriate medium) supplemented with 10% FBS at 37degC with 5% CO2. Cells are seeded in 96-well plates (2×10⁴ cells/well) and treated with JC-229 (0.001-100 uM) for 48-72 hours. Cell viability is measured using the resazurin (Alamar Blue) reduction assay or CellTiter-Glo. Fluorescence (Ex 530/Em 590 nm) or luminescence is measured. The IC50 is calculated from dose-response curves. For DNA damage studies, cells are treated with JC-229 for 24 hours, and gammaH2AX levels are analyzed by Western blot.
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| Animal Protocol |
JC-229 can be evaluated in a mouse model of human African trypanosomiasis (HAT). Immunocompromised mice (e.g., SCID mice) are infected intraperitoneally with T. brucei bloodstream forms. JC-229 is administered orally or intraperitoneally at doses of 10-50 mg/kg, twice daily for 5-7 days. Parasitemia is monitored daily by tail blood smears under a microscope. Survival is recorded over 30-60 days. JC-229 treatment is expected to reduce parasitemia and prolong survival compared to vehicle controls. The standard drug pentamidine can be used as a positive control.
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| ADME/Pharmacokinetics |
JC-229 has a molecular formula of C20H14Cl4N2O3S and a molecular weight of 504.22 g/mol. The compound appears as a solid with purity >97%. For in vitro studies, it is dissolved in DMSO (10-50 mM stock). For in vivo administration, JC-229 can be formulated in a solution containing DMSO, PEG300, Tween 80, and saline, or in a suspension with carboxymethylcellulose and Tween 80. The compound is stable as a powder and should be stored at -20degC. Pharmacokinetic properties in rodents have not been reported but are being investigated.
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| Toxicity/Toxicokinetics |
JC-229 is a research compound; comprehensive toxicity data are not publicly available. In cell-based assays, JC-229 shows minimal cytotoxicity to mammalian cells (e.g., HEK293, HepG2) at concentrations that are effective against T. brucei, indicating a favorable selectivity index. In mouse xenograft studies (infection models), no significant body weight loss or signs of acute toxicity were observed at therapeutic doses. Standard laboratory safety precautions should be followed. Not for human use.
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| References | |
| Additional Infomation |
JC-229 is a research-use-only compound not approved for clinical use. It is an analog of previously reported compounds and was synthesized for its ease of accessibility. JC-229 represents a promising lead for the development of new anti-trypanosomal drugs targeting DNA replication and repair pathways. By targeting TbRPA1, it offers a novel mechanism of action that is distinct from current treatments for human African trypanosomiasis (e.g., pentamidine, suramin, melarsoprol). The central benzamide core with two 3,4-dichlorophenyl groups and a methyl group is characteristic of its structure.
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| Molecular Formula |
C20H14CL4N2O3S
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| Molecular Weight |
504.21
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| CAS # |
3026716-22-0
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| Appearance |
White to off-white solid powder
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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 :~40 mg/mL (~79.33 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 | 1.9833 mL | 9.9165 mL | 19.8330 mL | |
| 5 mM | 0.3967 mL | 1.9833 mL | 3.9666 mL | |
| 10 mM | 0.1983 mL | 0.9917 mL | 1.9833 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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