| 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 |
PU 23 targets multidrug resistance protein 4 (MRP4), an efflux transporter that pumps anticancer drugs out of cells. By inhibiting MRP4, PU 23 reduces the efflux of 6-mercaptopurine and other anticancer agents, thereby overcoming drug resistance. It also targets heat shock protein 90 (Hsp90).
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| ln Vitro |
6-Mercaptopurine (6-MP) has an IC50 of 2.81 μM and inhibits HEK293 and HEK293/MRP4 cells, respectively. HEK293 and HEK293/MRP4 cells are inhibited by the combination of PU 23 (Cpd23) and 6-Mercaptopurine (6-MP), with IC50 values of 1.84 and 6.06 μM, respectively[1]. The amount of 6-MP in HEK293/MRP4 cells is also markedly increased by preincubating them with PU 23 (50 μM) for two hours[1].
In vitro, PU 23 inhibits MRP4-mediated drug efflux. It reduces resistance to 6-mercaptopurine in HEK293 cells expressing MRP4. The compound's activity as an MRP4 inhibitor makes it a valuable tool for studying drug resistance mechanisms in cancer. |
| ln Vivo |
Specific in vivo activity data for PU 23 are not available in the consulted sources. As an MRP4 inhibitor, it may have potential in vivo efficacy in combination with anticancer agents to overcome drug resistance. However, no systematic in vivo studies have been reported.
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| Enzyme Assay |
Typical in vitro assays for PU 23 involve measuring MRP4-mediated drug efflux. Cells expressing MRP4 are treated with the compound and a fluorescent substrate or radiolabeled drug. Intracellular accumulation of the substrate is measured by fluorescence or scintillation counting. Cytotoxicity assays are performed in the presence and absence of the compound to assess its ability to overcome drug resistance.
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| Cell Assay |
Cellular assays for PU 23 typically involve treating HEK293 or other cells expressing MRP4 with the compound at concentrations ranging from 1-100 µM. The compound's ability to increase intracellular accumulation of anticancer drugs such as 6-mercaptopurine is assessed. Cell viability is assessed by MTT assay.
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| Animal Protocol |
In vivo animal experiments for PU 23 are not detailed in the available literature. For studying MRP4 inhibition and drug resistance, typical animal models include xenograft mouse models where drug-resistant tumors are implanted. The compound would be administered in combination with anticancer agents, and tumor growth inhibition would be assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for PU 23 are not available. As a small molecule with a molecular weight of 425.52 g/mol, it would be expected to have reasonable oral bioavailability. Detailed ADME parameters have not been characterized.
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| Toxicity/Toxicokinetics |
No toxicological data are available for PU 23 in the consulted sources. As a research compound, comprehensive toxicological studies have not been reported. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Ya Chen, et al. Discovery of novel multidrug resistance protein 4 (MRP4) inhibitors as active agents reducing resistance to anticancer drug 6-Mercaptopurine (6-MP) by structure and ligand-based virtual screening. PLoS One. 2018 Oct 15;13(10):e0205175.
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| Additional Infomation |
PU 23 is a non-carboxylic multidrug resistance protein 4 (MRP4) inhibitor that reduces resistance to anticancer agents such as 6-mercaptopurine. It is used in cancer research to study drug resistance mechanisms. The compound also targets Hsp90. It is a research compound and is not approved for any clinical indication.
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| Molecular Formula |
C21H19N3O3S2
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|---|---|
| Molecular Weight |
425.523862123489
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| Exact Mass |
425.086
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| CAS # |
817635-93-1
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| PubChem CID |
4779049
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| Appearance |
Off-white to yellow solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
643
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)CNS(=O)(=O)C2=CC=C(C=C2)NC(=S)NC(=O)C3=CC=CC=C3
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| InChi Key |
RYIRRFWVFHEXTH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19N3O3S2/c25-20(17-9-5-2-6-10-17)24-21(28)23-18-11-13-19(14-12-18)29(26,27)22-15-16-7-3-1-4-8-16/h1-14,22H,15H2,(H2,23,24,25,28)
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| Chemical Name |
N-[[4-(benzylsulfamoyl)phenyl]carbamothioyl]benzamide
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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 (293.76 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 | 2.3501 mL | 11.7503 mL | 23.5007 mL | |
| 5 mM | 0.4700 mL | 2.3501 mL | 4.7001 mL | |
| 10 mM | 0.2350 mL | 1.1750 mL | 2.3501 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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