Other grades of this product :
| trapoxin A Basic information |
| Product Name: | trapoxin A | | Synonyms: | trapoxin A;(4aR,7S,10S,13S)-10,13-Dibenzyl-7-[6-oxo-6-[(S)-oxiranyl]hexyl]-1,2,3,4,9,10-hexahydro-4aH-6,9,12,14a-tetraazabenzocyclododecene-5,8,11,14(6H,7H,12H,13H)-tetrone;Cyclo[L-Phe-L-Phe-D-Hpr-6-[2-[(S)-oxiranyl]-2-oxoethyl]-L-Nle-];RF-1023A;Cyclo((S)-phenylalanyl-(S)-phenylalanyl-(R)-pipecolinyl-(2S,9S)-2-amino-8-oxo-9,10-epoxydecanoyl);Cyclo[(aS,2S)-a-amino-h-oxo-2-oxiraneoctanoyl-L-phenylalanyl-L-phenylalanyl-(2R)-2-piperidinecarbonyl];Cyclo[(αS,2S)-α-amino-η-oxo-2-oxiraneoctanoyl-L-phenylalanyl-L-phenylalanyl-(2R)-2-piperidinecarbonyl] | | CAS: | 133155-89-2 | | MF: | C34H42N4O6 | | MW: | 602.72 | | EINECS: | | Product Categories: | | Mol File: | 133155-89-2.mol |
| trapoxin A Chemical Properties |
| storage temp. | -20°C | | solubility | DMSO: soluble0.9-1.10 mg/ml, clear, colorless to faintly yellow (may be further diluted 20 fold in H2O) | | form | solid |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 |
| trapoxin A Usage And Synthesis |
| Description | Trapoxin A is a cyclotetrapeptide histone deacetylase (HDAC) inhibitor. It inhibits HDAC activity in a concentration-dependent and irreversible manner. Trapoxin A inhibits proliferation of NIH3T3 cells transformed by the oncogene v-sis (sis/NIH3T3; IC50 = ~200 ng/ml) and has detransformation activity, flattening sis/NIH3T3 cells when used at a concentration of 1 ng/ml. It also halts the cell cycle at the G2 phase in 3Y1 fibroblasts when used at a concentration of 10 nM and inhibits growth of TR303 cells resistant to trichostatin A at a concentration of 50 ng/ml. | | Uses | Trapoxin A has been used:- to study its effects on the inhibition of histone deacetylase 11 (HDAC11)
- to study its effects on the inhibition of HDAC3 in human cell lines
- to study its effects on the inhibition of HDAC6 in rat pyramidal neurons
| | Definition | ChEBI: A homodetic cyclic tetrapeptide constructed from L-phenylalanyl (x2), D-pipecolinyl and L-2-amino-8-oxo-9,10-epoxydecanoyl residues. | | Biochem/physiol Actions | Trapoxin A is a cyclotetrapeptide and a histone deacetylase (HDAC) inhibitor. It increases the level of chromatin acetylation associated with histone H3 at low nanomolar concentrations. Unlike the reversible HDAC inhibition induced by TCA, Trapoxin A irreversibly inhibites HDAC activity in crude cell lysates, and induces the accumulation of hyperacetylated core histones in a number of mammalian cell lines and tissues. Histone acetylation and methylation have been studied extensively for their anti-tumor activities in carcinogenesis and Trapoxin has been suggested as a potential anticancer agent for pre-clinical trials. |
| trapoxin A Preparation Products And Raw materials |
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