L-Penicillamine
CAS No. : 1113-41-3
Price and Availability of
CAS No. : 1113-41-3
| Size | Price | Stock |
|---|---|---|
| 1g | $50 | In-stock |
| 5g | $166 | In-stock |
| 25g | $576 | In-stock |
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| 100 g | Get quote | |
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| Cat. No. : | HY-116073 |
| M.Wt: | 149.22 |
| Formula: | C5H11NO2S |
| Purity: | >98 % |
| Solubility: | H2O : 33.33 mg/mL (ultrasonic) |
Introduction of
1113-41-3
:
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]. In Vivo:L-Penicillamine (100-125 mg/kg; p.o.; ad libitum daily; 14 days) produces 69% tumour inhibition in sarcoma-180-bearing CF1 mice on a complete diet and 71% tumour inhibition in those on a pyridoxine-deficient diet[3].
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].
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)[1][2][3].
In Vitro: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]. In Vivo:L-Penicillamine (100-125 mg/kg; p.o.; ad libitum daily; 14 days) produces 69% tumour inhibition in sarcoma-180-bearing CF1 mice on a complete diet and 71% tumour inhibition in those on a pyridoxine-deficient diet[3].
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].
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