Thiostrepton , ≥98%(HPLC) , 1393-48-2
Synonym(s):
Bryamycin;FOXM1 Inhibitor I;Thiactin;Thiostreptin A
CAS NO.:1393-48-2
Empirical Formula: C72H85N19O18S5
Molecular Weight: 1664.89
MDL number: MFCD00135828
EINECS: 215-734-9
Pack Size | Price | Stock | Quantity |
250MG | RMB559.20 | In Stock |
|
1G | RMB1599.20 | In Stock |
|
others | Enquire |
PRODUCT Properties
Melting point: | 248-257°C (dec.) |
alpha | D23 -98.5° (glacial acetic acid); -61° (dioxane); -20° (pyridine) |
Density | 1.0824 (rough estimate) |
refractive index | 1.6700 (estimate) |
storage temp. | Sealed in dry,Store in freezer, under -20°C |
solubility | Soluble in DMSO or chloroform |
form | Off-white powder |
pka | 10.43±0.46(Predicted) |
color | Off-white |
Water Solubility | 0.24g/L(28 ºC) |
Merck | 13,9440 |
Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week. |
Description and Uses
The mammalian transcription factor forkhead box M1 (FoxM1) is induced during G1 phase, with expression continuing through S phase and mitosis. Thiostrepton is a natural peptide thiazole antibiotic that inhibits FoxM1 in mammalian cells, preventing the expression of FoxM1-regulated genes, which includes FoxM1 itself. Through this mechanism, thiostrepton prevents proliferation and induces apoptosis in human cancer cells. These effects correlate with the ability of thiostrepton to act as a proteasome inhibitor.
Thiostrepton is a macrocyclic antibiotic incorporating thiazoles and other atypical amino acids. Patented in 1961, thiostrepton has been used as an antibiotic and acts by binding to ribosomes to prevent the binding of the EF-G elongation factor and GTP to the 50S ribosomal subunit. Thiostrepton is an inducer of tipA, a gene that controls the bacterial transcription regulators, TipAL and TipAS, that are central regulators in multidrug resistance. Thiostrepton is closely related to siomycin, a recently discovered inhibitor of oncogenic transcription factor, FoxM1.
Safety
Symbol(GHS) | GHS07 |
Signal word | Warning |
Hazard statements | H302+H312+H332 |
Precautionary statements | P271-P261-P280 |
Hazard Codes | Xn |
Risk Statements | 22 |
Safety Statements | 22-24/25 |
WGK Germany | 3 |
RTECS | XN6300100 |
F | 10-21 |
HS Code | 29419090 |
Toxicity | LD50 oral in mouse: > 1gm/kg |