| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
Pentachloropseudilin targets myosin motor proteins, particularly class I myosins (Myo1), as a reversible allosteric inhibitor. It also inhibits class 5 myosins. The compound inhibits TGF-β-stimulated signaling with an IC₅₀ of 0.1-0.2 µM by accelerating cell-surface type II TGF-β receptor turnover. It also exhibits antimicrobial and antifungal activity.
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| ln Vitro |
In target cells (A549, HepG2, and Mv1Lu cells), pentachloropsin (PClP) inhibits TGF-β-stimulated Smad2/3 phosphorylation and plasminogen activator inhibitor-1 (PAI-1) promoter activation; the IC50 value is 0.1 μM [1]. Pentachloropseudoprotein inhibited vimentin, N-cadherin, and fibronectin expression in response to TGF-β, preventing TGF-β-induced epithelial-mesenchymal transition (EMT) in these cells. The TGF-β-mediated (50 or 100 pM) increase in p-Smad2/3 expression was inhibited by pretreatment with pentachloropsin (0.05 to 1 μM; 0–6 hours) by 47% (Mv1Lu) and 79% (A549)[1]. By reducing the expression of type II TGF-β receptors on the cell surface and speeding up caveolae-mediated internalization, which is mainly followed by lysosome-dependent receptor degradation, pentachloropsin (0.2 μM) inhibits TGF-β. Sucrose density gradient analysis and immunofluorescence staining were used to examine cellular responses to stimulation [1]. In HUVEC, pentachloropsin (200 μM; 24 hours) shows and modifies cell viability [2].
In vitro, pentachloropseudilin inhibits myosin ATPase activity. It impairs actin-based motility and intracellular trafficking. The compound inhibits TGF-β-stimulated signaling with an IC₅₀ of 0.1-0.2 µM. It blocks Trypanosoma cruzi invasion of host cells and impairs angiogenesis by disrupting the actin cytoskeleton, integrin trafficking, and the cell cycle. |
| ln Vivo |
In vivo, pentachloropseudilin is used as a chemical probe to study myosin-dependent cellular processes, vesicle transport, and cytoskeletal regulation. It provides insights into mechanisms of cell motility, endocytosis, and related disease pathways. The compound has been studied for its anti-angiogenic activity.
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| Enzyme Assay |
Myosin ATPase assays: Purified myosin (class I or class V) is incubated with ATP in the presence of pentachloropseudilin at various concentrations (typically 0.1-100 µM). ATPase activity is measured by detecting released phosphate using colorimetric or fluorometric methods. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
TGF-β signaling assays: Cells expressing TGF-β receptors are treated with pentachloropseudilin at various concentrations (0.01-10 µM) and stimulated with TGF-β. SMAD2/3 phosphorylation and downstream gene expression are measured by Western blot and qRT-PCR. Receptor turnover is assessed by cell surface biotinylation and internalization assays.
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| Animal Protocol |
In vivo studies are conducted in animal models of angiogenesis, infection, or motility-related diseases. Pentachloropseudilin is administered via intraperitoneal, intravenous, or other routes at specified doses. Tumor growth, angiogenesis, and metastasis are assessed. Tissue samples are analyzed for myosin and TGF-β pathway markers.
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| ADME/Pharmacokinetics |
Pentachloropseudilin has molecular weight 331.41 and formula C₁₀H₄Cl₅NO. It is soluble in DMSO. Purity is ≥95%. The compound is a reversible allosteric inhibitor of myosin motor proteins with antimicrobial and antifungal activity.
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| References |
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| Additional Infomation |
Pentachloropseudilin is a marine-derived antibiotic that functions as a reversible allosteric inhibitor of myosin motor proteins, particularly class I myosins. It also inhibits class 5 myosins and TGF-β activity. The compound is widely used as a chemical probe to study myosin-dependent cellular processes, vesicle transport, and cytoskeletal regulation. It has anti-angiogenic activity and blocks Trypanosoma cruzi invasion.
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| Molecular Formula |
C10H4CL5NO
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|---|---|
| Molecular Weight |
331.39
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| Exact Mass |
328.874
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| CAS # |
69640-38-6
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| PubChem CID |
3053233
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| Appearance |
Off-white to gray solid powder
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| Density |
1.733g/cm3
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| Boiling Point |
445.9ºC at 760 mmHg
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| Flash Point |
223.5ºC
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| Index of Refraction |
1.672
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| LogP |
5.654
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
281
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FBRLLYYPGGXCKT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H4Cl5NO/c11-3-1-4(9(17)5(12)2-3)8-6(13)7(14)10(15)16-8/h1-2,16-17H
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| Chemical Name |
2,4-dichloro-6-(3,4,5-trichloro-1H-pyrrol-2-yl)phenol
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| Synonyms |
PClP Pentachloropseudilin
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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 (~301.74 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0176 mL | 15.0880 mL | 30.1759 mL | |
| 5 mM | 0.6035 mL | 3.0176 mL | 6.0352 mL | |
| 10 mM | 0.3018 mL | 1.5088 mL | 3.0176 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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