L-Penicillamine
Based on 1 Customer Validation
L-Penicillamine is an orally active serine palmitoyltransferase (SPT) inhibitor. L-Penicillamine inactivates the PLP cofactor by forming adducts, thereby inhibiting SPT activity and reducing sphingolipid biosynthesis. L-Penicillamine not only blocks tumor access to vitamin B6, but also stabilizes the human papillomavirus 16 E6 oncoprotein monomer and inhibits its polymerization, exhibiting a unique anticancer mechanism. L-Penicillamine effectively delays the growth of Sarcoma-180, induces tumor necrosis and prolongs survival (though long-term use may lead to Pyridoxine (HY-B1328) deficiency and weight loss).
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- Pureté: 99.71%
- CAS No.: 1113-41-3
- Formule: C5H11NO2S
- Masse moléculaire:149.22
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Stockage:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
L-Penicillamine (5 mM; 30 min; 25 °C) potently inhibits purified Sphingomonas paucimobilis serine palmitoyltransferase, reducing activity to 3% at 5 mM after 30 minutes at 25 °C, and this inhibition is reversible via dialysis against PLP-containing buffer to restore ~80% enzyme activity[1].
L-Penicillamine (10 mM; 30 min) forms a PLP-thiazolidine adduct with purified Sphingomonas paucimobilis serine palmitoyltransferase, detected via a 333 nm UV-visible peak that forms completely within 30 minutes of 10 mM L-Penicillamine addition, and this adduct is removable by dialysis to regenerate holo-enzyme[1].
L-Penicillamine (2 mM; 12 days; 4 °C) stabilizes monomeric, soluble HPV16 S-E6 fusion protein in dialysis buffer containing 20 μM ZnCl2 and 2 mM DTT, with a zinc-to-protein stoichiometric ratio of ~1:1[2].
L-Penicillamine functions as a weak zinc chelator, with a chelating strength ~100 times weaker than EGTA (HY-D0861) and ~1000 times weaker than EDTA[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
L-Penicillamine (100 mg/kg; p.o.; daily; 7 days via drinking water) produces marked ascitic tumour inhibition in sarcoma-180-bearing CF1 mice on a pyridoxine-deficient diet, with no significant prolongation of median survival time[3].
L-Penicillamine (25-100 mg/kg; s.c., i.p., p.o. intubation, p.o. drinking water; daily; 7 days) produces 21-60% tumour inhibition in sarcoma-180-bearing CF1 mice, while 200 mg/kg daily via subcutaneous injection or stomach intubation is 100% lethal[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CF1 white Swiss male mice (initial weight 20 g; subcutaneous implantation of 1×106 ascitic sarcoma-180 cells)[3]
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Dosage:100 mg/kg
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Administration:p.o.; ad libitum daily via drinking water
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Result:Achieved 8-week survival rates of 60%, 80%, 40%, and 40% across four separate experiments.
Resulted in 74% 30-day survival in the first experiment, with 11 of 20 mice experiencing complete tumour regression with no recurrence 342 days after treatment cessation.
Observed incomplete tumour regression in an additional 3 of 20 mice.
Caused significantly smaller tumours, with many becoming necrotic, decreasing in size, and being extruded by day 43.
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Animal Model:CF1 white Swiss mice (initial weight 20 g; intraperitoneal injection of 1×106 ascitic sarcoma-180 cells)[3]
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Dosage:100 mg/kg
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Administration:p.o.; daily; 7 days via drinking water
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Result:Caused minimal ascitic tumour inhibition and a median survival time of 12.5 days in mice on complete diet.
Caused marked ascitic tumour inhibition and a median survival time of 11 days in mice on pyridoxine-deficient diet.
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Animal Model:CF1 white Swiss male mice (initial weight 20 g; subcutaneous implantation of 1×106 ascitic sarcoma-180 cells)[3]
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Dosage:25, 50, 100 mg/kg (s.c.); 100 mg/kg (i.p.); 25, 50, 100 mg/kg (p.o. stomach intubation); 25, 50, 100, 200 mg/kg (p.o. drinking water)
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Administration:s.c.; daily; 7 days;
i.p.; daily; 7 days;
p.o. (stomach intubation); daily; 7 days;
p.o. (drinking water); ad libitum daily; 7 days -
Result:Caused 21% tumour inhibition at 25 mg/kg, 24% at 50 mg/kg, 60% at 100 mg/kg via subcutaneous administration; 200 mg/kg daily was 100% lethal.
Caused 39% tumour inhibition at 100 mg/kg via intraperitoneal administration.
Caused 24% tumour inhibition at 25 mg/kg, 42% at 50 mg/kg, 47% at 100 mg/kg via stomach intubation; 200 mg/kg daily was 100% lethal.
Caused 26% tumour inhibition at 25 mg/kg, 35% at 50 mg/kg, 46% at 100 mg/kg, 44% at 200 mg/kg via oral drinking water with 0 mortality.
Chemical Information
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CAS No. 1113-41-3
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Appearance Solid
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Masse moléculaire 149.22
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Formule C5H11NO2S
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Color White to off-white
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
H2O : 33.33 mg/mL (223.36 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (278 KB)
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SDS (761 KB)
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- Portuguese - PT (761 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 6.7015 mL | 33.5076 mL | 67.0151 mL | 167.5379 mL |
| 5 mM | 1.3403 mL | 6.7015 mL | 13.4030 mL | 33.5076 mL | |
| 10 mM | 0.6702 mL | 3.3508 mL | 6.7015 mL | 16.7538 mL | |
| 15 mM | 0.4468 mL | 2.2338 mL | 4.4677 mL | 11.1692 mL | |
| 20 mM | 0.3351 mL | 1.6754 mL | 3.3508 mL | 8.3769 mL | |
| 25 mM | 0.2681 mL | 1.3403 mL | 2.6806 mL | 6.7015 mL | |
| 30 mM | 0.2234 mL | 1.1169 mL | 2.2338 mL | 5.5846 mL | |
| 40 mM | 0.1675 mL | 0.8377 mL | 1.6754 mL | 4.1884 mL | |
| 50 mM | 0.1340 mL | 0.6702 mL | 1.3403 mL | 3.3508 mL | |
| 60 mM | 0.1117 mL | 0.5585 mL | 1.1169 mL | 2.7923 mL | |
| 80 mM | 0.0838 mL | 0.4188 mL | 0.8377 mL | 2.0942 mL | |
| 100 mM | 0.0670 mL | 0.3351 mL | 0.6702 mL | 1.6754 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
L-Penicillamine Related Classifications
HY-116073 Related Classifications
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