| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
PP5-IN-1 specifically targets the catalytic domain of serine/threonine protein phosphatase 5 (PP5). By competitively binding to the active site, the compound inhibits PP5's dephosphorylation activity, thereby modulating the activity of client proteins within Hsp90 chaperone complexes. This inhibition affects ATM/ATR-mediated DNA damage signaling pathways and influences cellular responses to DNA damage. PP5-IN-1 induces apoptosis in renal cancer cells, making it a valuable tool for studying PP5-related signaling pathways.
|
|---|---|
| ln Vitro |
In vitro, PP5-IN-1 demonstrates potent inhibition of PP5 phosphatase activity. The compound acts as a competitive inhibitor, binding to the catalytic domain of PP5 and preventing substrate dephosphorylation. PP5-IN-1 induces apoptosis in renal cancer cells, demonstrating its potential as an anticancer agent. The compound shows concentration-dependent inhibition of PP5 activity and cellular effects in various cancer cell models. Molecular weight is 342.41 and molecular formula is C₁₈H₁₈N₂O₃S.
|
| ln Vivo |
In vivo activity data for PP5-IN-1 are limited, as the compound is primarily studied in vitro. Based on its mechanism of PP5 inhibition and induction of apoptosis, the compound is expected to exhibit antitumor activity in animal models of cancer, particularly renal cancer. However, detailed efficacy studies in animal models have not been extensively reported. Further in vivo studies are needed to evaluate the compound's therapeutic potential and pharmacokinetic properties.
|
| Enzyme Assay |
The in vitro enzyme inhibition assay for PP5-IN-1 typically involves measuring the activity of recombinant human PP5 using a phosphopeptide substrate or p-nitrophenyl phosphate (pNPP). Purified PP5 enzyme is incubated with varying concentrations of PP5-IN-1 (0.01-100 µM) in assay buffer at 30°C for 15-30 minutes. The reaction is initiated by adding the substrate, and after incubation, the reaction is stopped. Phosphate release is quantified using colorimetric or fluorometric detection, and IC50 values are calculated.
|
| Cell Assay |
For in vitro cell-based assays, renal cancer cell lines or other cancer cell lines are cultured in appropriate medium and treated with PP5-IN-1 at concentrations ranging from 0.1-100 µM for 24-72 hours. Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is evaluated using Annexin V-FITC/PI double staining and caspase activity assays. PP5 activity is measured in cell lysates using a phosphatase activity assay kit. Hsp90 client protein levels and DNA damage markers are assessed by Western blot.
|
| Animal Protocol |
In vivo animal studies for PP5-IN-1 have not been extensively reported. Based on the compound's mechanism as a PP5 inhibitor and inducer of apoptosis, potential in vivo studies would involve administration to tumor-bearing mouse models, particularly renal cancer xenografts, via oral gavage, intraperitoneal injection, or intravenous injection at doses ranging from 1-50 mg/kg. Tumor growth would be monitored by caliper measurements. Apoptosis and PP5 activity would be assessed in tumor tissues.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of PP5-IN-1 have not been fully characterized. The compound is soluble in DMSO at 100 mg/mL (292.05 mM). Molecular weight is 342.41. Detailed pharmacokinetic parameters such as bioavailability, half-life, and protein binding have not been reported. Stability in solution may be limited and fresh solutions should be prepared for each experiment. The compound should be stored under recommended conditions.
|
| Toxicity/Toxicokinetics |
Toxicology data for PP5-IN-1 are limited. As a research compound, it has not been systematically evaluated for safety. The compound's mechanism of inducing apoptosis suggests potential cytotoxicity, which may be desirable for anticancer applications but requires careful safety assessment. Standard toxicological endpoints including cell viability, genotoxicity, and organ toxicity should be evaluated. The compound is intended for research use only and is not approved for human use.
|
| References | |
| Additional Infomation |
PP5-IN-1 is a potent and competitive inhibitor of serine/threonine protein phosphatase 5 (PP5) with potential anticancer activity. The compound induces apoptosis in renal cancer cells by inhibiting PP5 activity, making it a valuable tool for studying PP5-related signaling pathways, Hsp90 chaperone function, and DNA damage responses. PP5-IN-1 supports research into therapeutic strategies targeting PP5 and associated disorders. It is intended for research use only and is not approved for therapeutic use.
|
| CAS # |
1022417-69-1
|
|---|---|
| Appearance |
Yellow to orange solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (292.05 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
