Name | trichostatin A |
---|---|
Synonyms |
Antibiotic A-300
2,4-Heptadienamide, 7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxo-, (2E,4E,6R)- (2E,4E,6R)-7-[4-(Dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide (R)-Trichostatin A 2,4-Heptadienamide, 7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxo-, (2E,4E,6R)- (9CI) TSA 2,4-Heptadienamide, 7-(4-(dimethylamino)phenyl)-N-hydroxy-4,6-dimethyl-7-oxo-, (2E,4E,6R)- 2,4-Heptadienamide, 7-(4-(dimethylamino)phenyl)-N-hydroxy-4,6-dimethyl-7-oxo- Trichostatin A 7-(4-(Dimethylamino)phenyl)-N-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide 7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6R-dimethyl-7-oxo-2E,4E-heptadienamide (2E,4E,6R)-7-[4-(Dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide |
Description | Trichostatin A is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC. |
---|---|
Related Catalog | |
Target |
HDAC:1.8 nM (IC50) |
In Vitro | Trichostatin A is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC. Trichostatin A (TSA) inhibits proliferation of eight breast carcinoma cell lines with mean±SD IC50 of 124.4±120.4 nM (range, 26.4-308.1 nM). HDAC inhibitory activity of Trichostatin A is similar in all cell lines with mean IC50 of 2.4±0.5 nM (range, 1.5-2.9 nM)[1]. Trichostatin A (330 nM) increases Gαs protein expression in human myometrial cells, but does not increase Gαs mRNA levels[2]. Trichostatin A (20-75 nM) induces minimal cytotoxicity to adipose-derived stem cells (ADSCs), and enhances the osteogenic differentiation capacity of ADSCs[3]. In addition, Trichostatin A (0, 10, 100, 500 nM) dose-dependently decreases HDAC class I/II activity[4]. |
In Vivo | Trichostatin A (500 μg/kg, s.c.) pronounces antitumor activity without causing any measurable toxicity in doses of up to 5 mg/kg by s.c. injection, in randomized controlled efficacy studies using the N-methyl-N-nitrosourea carcinogen-induced rat mammary carcinoma model[1]. |
Cell Assay | Cells are cultured in a 96-well plate at 1×103 cells per well with 100 μL complete DMEM in the presence or absence of a HDAC inhibitor Trichostatin A for 72 h. Cytotoxicity is measured by performing WST-8 assay using a CCK-8 cell proliferation kit. The 450 nm absorbance is measured with a microplate reader. All experiments are carried out in triplicate and 3 independent experiments are performed[3]. |
Animal Admin | Rats[1] Twelve rats are randomized to receive 500 μg/kg Trichostatin A in 50 μL DMSO, or 50 μL DMSO as vehicle control, by s.c. injection twice weekly for 4 weeks. In subsequent studies, 30 rats are randomized to receive Trichostatin A 500 μg/kg in 50 μL DMSO, or 50 μL DMSO as vehicle control, by s.c. injection daily for 4 weeks. Weekly tumor measurements, estimated tumor volumes, and body mass are recorded for each animal. Animals are sacrificed at the end of the 4-week study period; palpable tumors are resected and immediately snap-frozen in liquid nitrogen. Animals with tumors <2 cm in diameter or ulcerating tumors are withdrawn from study[1]. |
References |
Density | 1.1±0.1 g/cm3 |
---|---|
Melting Point | 141-143ºC |
Molecular Formula | C17H22N2O3 |
Molecular Weight | 302.368 |
Exact Mass | 302.163055 |
PSA | 69.64000 |
LogP | 2.77 |
Index of Refraction | 1.578 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATAMUTATION DATA
|
Symbol |
![]() GHS07 |
---|---|
Signal Word | Warning |
Hazard Statements | H302 + H312 + H332-H315-H317-H319-H335 |
Precautionary Statements | P261-P280-P302 + P352 + P312-P304 + P340 + P312-P333 + P313 |
Personal Protective Equipment | Eyeshields;Gloves;half-mask respirator (US);multi-purpose combination respirator cartridge (US) |
Hazard Codes | Xn: Harmful; |
Risk Phrases | R20/21/22 |
Safety Phrases | 26-36 |
RIDADR | NA 1993 / PGIII |
WGK Germany | 3 |
RTECS | MI5215000 |
HS Code | 2924299090 |
Precursor 9 | |
---|---|
DownStream 0 |
HS Code | 2924299090 |
---|---|
Summary | 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0% |