Molecular Formula | C17H22N2O3 |
Molar Mass | 302.37 |
Density | 1.139 |
Melting Point | 140-143℃ |
Specific Rotation(α) | D20.5 +62.8° ±1.1° (c = 1.007 in ethanol) |
Solubility | Soluble in water (Partly Miscible), ethanol (2 mg/mL), DMSO (20 mg/mL), acetonitrile, DM |
Appearance | Off-white lyophilized solid |
Color | Tan |
Merck | 14,9649 |
pKa | 8.93±0.23(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
Sensitive | Sensitive to heat |
Refractive Index | 136 ° (C=0.3, MeOH) |
MDL | MFCD03848392 |
Use | A potent and non-competitive reversible inhibitor of HDAC. |
In vitro study | Trichostatin A inhibits proliferation of eight breast cancer cell lines, including MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, and SK-BR-3, the mean IC50 was 124.4 nM (range 26.4-308.1 nM) and was more effective for cell lines expressing ERα than for cell lines expressing ERα negative. Trichostatin A inhibited HDAC activity in all breast cancer cell lines with A mean IC50 of 2.4 nM (range 0.6-2.6 nM), resulting in significant histone H4 hyperacetylation. Unlike Trapoxin (TPX) and Chlamydocin, which effectively inhibit HDAC1 or HDAC4 but not HDAC6, Trichostatin A inhibits these HDACs to A similar extent, with IC50 values of 6 nM, 38 nM, and 8.6 nM, respectively. Trichostatin A (100 ng/mL) acts on MIA PaCa-2 cells to induce the expression of transforming growth factor beta type II receptor (tβrii) by recruiting p300 and PCAF into the Sp1-NF-Y HDAC complex, the complex binds to the DNA fragment of the tβrii promoter, accompanied by Sp1 acetylation, and the HDAC associated with the complex is mathematically all reduced. |
In vivo study | Administration of Trichostatin A 0.5 mg/kg dose of N-methyl-N-nitrosourea carcinogen-induced rat breast cancer model for 4 weeks, with effective anticancer activity, even treatment at doses up to 5 mg/kg did not have any measurable toxicity. Intraperitoneal injection of Trichostatin A alone at A dose of 10 mg/kg in non-transgenic and spinal muscular atrophy (SMA) model mice resulted in increased levels of acetylated H3 and H4 histones, it also resulted in a slight increase in live motor neuron (SMN) gene expression. Trichostatin A daily treatment of SMA model mice at A dose of 10 mg/kg promoted survival, reduced weight loss, and enhanced locomotor activity. |
Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. R43 - May cause sensitization by skin contact |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
UN IDs | NA 1993 / PGIII |
WGK Germany | 3 |
RTECS | MI5215000 |
HS Code | 29280000 |
Reference Show more | 1. Zhao Zhengbin, Li Junfeng, Zhang Liting, etc. Effects of total saponins of astragalus on leptin-induced proliferation and TIMP-1 upregulation of HSC [J]. Journal of Xi'an Jiaotong University (Medical Sciences) 2012, Volume 33, Issue 5, 651-653, 3 pages, ISTIC PKU CSCD. |