| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
PS432 targets the atypical Protein Kinase C (PKC) isoforms, specifically PKCι and PKCζ. It is an allosteric inhibitor that binds to the PIF-pocket, a regulatory site present in the kinase domain of these enzymes. The IC50 values for PS432 are 16.9 µM for PKCι and 18.5 µM for PKCζ. By binding to this allosteric site, it inhibits the kinase activity of these PKC isoforms, which are known to play critical roles in cell proliferation and survival, particularly in cancer.
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| ln Vitro |
PS432 (25 μM; 24 h) suppresses cell division, which in turn suppresses A549 and A427, with IC50 values of 14.8 μM and 10.4 μM, respectively [1]. PS432 (50 μM; 12, 24, 36 h) arrests A549 lung cancer cells in the G0/G1 phase of the cell cycle [1].
In vitro, PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs). Its activity is demonstrated by the dose-dependent reduction in cell viability and growth in cultured NSCLC cell lines. The specific IC50 values for its anti-proliferative effect on different cell lines are not detailed in the available summaries, but the compound is described as a potent inhibitor of NSCLC cell growth. This in vitro activity is the basis for its observed in vivo anti-tumor efficacy. |
| ln Vivo |
In a transplant model for heterogeneous lung cancer, PS432 (2.5 mg/kg; intraperitoneal injection; once daily for 14 days) suppresses tumor growth [1].
In vivo, PS432 has been shown to significantly reduce tumor growth in mouse xenograft models without causing side effects. In these models, human NSCLC cells are implanted into immunodeficient mice, and the mice are treated with PS432. The treatment leads to a significant reduction in tumor growth compared to control groups. A key finding is the absence of observable side effects, suggesting that the compound has a favorable therapeutic index and selectively targets cancer cells. |
| Enzyme Assay |
Cell-free assays for PS432 focus on its ability to inhibit the enzymatic activity of its targets, PKCι and PKCζ. A common method is a kinase activity assay. In this assay, the recombinant PKCι or PKCζ enzyme is incubated with a substrate peptide and ATP in the presence of varying concentrations of PS432. The amount of phosphorylated substrate is then measured, often using a radioactive (e.g., 32P-ATP) or a fluorescent/luminescent detection system. The concentration of PS432 required to inhibit 50% of the kinase activity (IC50) is calculated. The IC50 for PS432 against PKCι and PKCζ are reported as 16.9 µM and 18.5 µM, respectively.
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| Cell Assay |
In vitro cell-based assays for PS432 are performed to evaluate its anti-proliferative effects. Non-small cell lung cancer (NSCLC) cell lines, such as A549 or H1299, are cultured and treated with increasing concentrations of PS432 for a defined period (e.g., 48-72 hours). Cell viability is then measured using standard assays like MTT, CellTiter-Glo, or by counting the number of viable cells. The compound's ability to induce apoptosis can also be assessed by staining cells with Annexin V and propidium iodide, followed by flow cytometry. These assays confirm the compound's ability to inhibit cancer cell growth in a cellular context.
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| Animal Protocol |
In vivo animal experiments for PS432 are conducted using mouse xenograft models to assess its anti-tumor efficacy. In a typical study, human NSCLC cells are subcutaneously injected into immunodeficient mice to establish tumors. Once the tumors reach a certain size, the mice are randomized into treatment and control groups. PS432 is administered, often via intraperitoneal (IP) injection, at a specific dose and schedule. Tumor growth is monitored by caliper measurements, and endpoints include tumor volume, tumor weight, and survival. The study also assesses the compound's toxicity by monitoring body weight and overall health of the animals.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for PS432 is not detailed in the available literature. Its properties, such as oral bioavailability, half-life, and tissue distribution, would be important for its development as a therapeutic agent. Given its in vivo efficacy, it is assumed to have reasonable pharmacokinetic properties. However, no specific PK parameters (e.g., Cmax, Tmax, AUC) are provided. The compound is typically stored as a powder at -20°C for up to three years.
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| Toxicity/Toxicokinetics |
Toxicological data for PS432 is limited. A key finding from in vivo studies is that PS432 significantly reduces tumor growth without side effects in mouse xenograft models. This suggests a favorable safety profile, at least in the short term. However, comprehensive toxicology studies, such as those measuring LD50, organ toxicity, and genotoxicity, have not been reported in the public domain. Its use is restricted to laboratory research, and it is not approved for human use.
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| References | |
| Additional Infomation |
PS432 is a research-grade compound developed as a potent and selective inhibitor of atypical PKCs, specifically targeting the PIF-pocket. It is a valuable tool for studying the role of PKCι and PKCζ in cancer biology and for validating these kinases as therapeutic targets. Its ability to inhibit tumor growth without side effects in preclinical models makes it a promising candidate for further development. It has not yet progressed to clinical trials. All information is for research reference and not for diagnostic or clinical use.
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| Molecular Formula |
C25H19CLN2O5S
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|---|---|
| Molecular Weight |
494.94
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| Exact Mass |
494.07
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| CAS # |
2083630-26-4
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| PubChem CID |
124222222
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
662.5±65.0 °C at 760 mmHg
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| Flash Point |
354.5±34.3 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.686
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| LogP |
5.81
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
832
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(=O)C1=C(C(=O)N(C1C2=CC=C(O2)C3=CC=C(C=C3)Cl)C4=NC5=C(S4)C=C(C=C5)C)O
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| InChi Key |
NBZPOMWJBSLLCT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H19ClN2O5S/c1-3-32-24(31)20-21(18-11-10-17(33-18)14-5-7-15(26)8-6-14)28(23(30)22(20)29)25-27-16-9-4-13(2)12-19(16)34-25/h4-12,21,29H,3H2,1-2H3
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| Chemical Name |
ethyl 2-[5-(4-chlorophenyl)furan-2-yl]-4-hydroxy-1-(6-methyl-1,3-benzothiazol-2-yl)-5-oxo-2H-pyrrole-3-carboxylate
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| Synonyms |
PS 432; PS-432; PS432
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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 : ~100 mg/mL (~202.04 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 | 2.0204 mL | 10.1022 mL | 20.2045 mL | |
| 5 mM | 0.4041 mL | 2.0204 mL | 4.0409 mL | |
| 10 mM | 0.2020 mL | 1.0102 mL | 2.0204 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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