129431-12-5

Basic information

• Product Name: Mpa(Trt)-OSu
• Synonyms: Mpa(Trt)-OSu;2,5-Dioxopyrrolidin-1-yl 3-(tritylthio)propanoate
• CAS NO: 129431-12-5
• Molecular Formula: C₂₆H₂₃NO₄S
• Molecular Weight: 445.53012
• EINECS: -0
• Mol File: 129431-12-5.mol

Chemical Properties

• Boiling Point: 572.7±52.0 °C(Predicted)
• Appearance: /
• Density: 1.31±0.1 g/cm3(Predicted)
• Storage Temp.: 2-8°C
• CAS DataBase Reference: Mpa(Trt)-OSu(CAS DataBase Reference)
• NIST Chemistry Reference: Mpa(Trt)-OSu(129431-12-5)
• EPA Substance Registry System: Mpa(Trt)-OSu(129431-12-5)

Safety Data

• Hazardous Substances Data: 129431-12-5(Hazardous Substances Data)

Usage

Uses

Used in Bioconjugation:
Mpa(Trt)-OSu is used as a bioconjugation agent for the efficient labeling of proteins and other biomolecules. Its maleimide group reacts specifically with thiol groups on proteins, while the N-hydroxysuccinimide ester group reacts with primary amines, allowing for selective and site-specific conjugation.
Used in Pharmaceutical Industry:
Mpa(Trt)-OSu is used as a key component in the production of antibody-drug conjugates for targeted cancer therapies. Its ability to selectively conjugate drugs to antibodies enables the development of more effective and precise treatments.
Used in Diagnostics:
Mpa(Trt)-OSu is used as a labeling agent in the development of protein-based diagnostic tools. Its selective conjugation capabilities allow for the attachment of detection molecules to proteins, enhancing the sensitivity and specificity of diagnostic assays.
Used in Research and Development:
Mpa(Trt)-OSu is used as a valuable tool in chemical biology research and development. Its versatility and selectivity enable the exploration of novel protein-protein interactions, enzyme mechanisms, and other biological processes.

Upstream product

• 76-83-5 trityl chloride 
• 3695-77-0 triphenylmethanethiol 
• 76-84-6 triphenylmethyl alcohol 
• 6066-82-6 1-hydroxy-pyrrolidine-2,5-dione 
• 27144-18-9 3-(tritylthio) propanoic acid 

Downstream Products

• 1616776-08-9 Lys-boc octreotide 3-tritylmercaptopropionamide 
• 1313816-36-2 ((4aR,7S,7aR,12bS)-3-(3-(3-tritylthio)propanamido)butyl)-2,3,4,4a,7,7a-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diyl diacetate 
• 1037589-70-0 ^αN-(9-fluorenylmethoxycarbonyl)-^εN-[3-(triphenylmethylsulfanyl)propionyl]-L-lysine 
• 129431-13-6 N,N'-(propane-1,3-diyl)bis<3-(triphenylmethylthio)propanamide> 
• 1380245-39-5 N-(3-aminopropyl)-3-(tritylthio)propanamide 

Relevant articles and documents

Mitochondrial heat shock protein-guided photodynamic therapy

Mitochondria targeting sensitizers are continuing to gain importance in photodynamic therapy (PDT). Members of the 90 kDa heat shock protein (Hsp90) family, including TRAP1 (Hsp75), are overexpressed in cancer cells and help to control the antiapoptotic protein activity. The present work introduces an Hsp90 inhibitor-mitochondria targeting indocyanine dye conjugate (IR-PU) for high PDT efficacy.

Interrogating the Role of Receptor-Mediated Mechanisms: Biological Fate of Peptide-Functionalized Radiolabeled Gold Nanoparticles in Tumor Mice

(Graph Presented) To get a better insight on the transport mechanism of peptide-conjugated nanoparticles to tumors, we performed in vivo biological studies of bombesin (BBN) peptide functionalized gold nanoparticles (AuNPs) in human prostate tumor bearing mice. Initially, we sought to compare AuNPs with thiol derivatives of acyclic and macrocyclic chelators of DTPA and DOTA types. The DTPA derivatives were unable to provide a stable coordination of 67Ga, and therefore, the functionalization with the BBN analogues was pursued for the DOTA-containing AuNPs. The DOTA-coated AuNPs were functionalized with BBN[7-14] using a unidentate cysteine group or a bidentate thioctic group to attach the peptide. AuNPs functionalized with thioctic-BBN displayed the highest in vitro cellular internalization (≈ 25%, 15 min) in gastrin releasing peptide (GRP) receptor expressing cancer cells. However, these results fail to translate to in vivo tumor uptake. Biodistribution studies following intravenous (IV) and intraperitoneal (IP) administration of nanoconjugates in tumor bearing mice indicated that the presence of BBN influences to some degree the biological profile of the nanoconstructs. For IV administration, the receptor-mediated pathway appears to be outweighed by the EPR effect. By contrast, in IP administration, it is reasoned that the GRPr-mediated mechanism plays a role in pancreas uptake.

Novel mTOR inhibitor compounds and the use thereof

The novel mTOR inhibitor compounds of the present invention are capable of selective drug delivery to bone and released slowly in bone for a long period of time. The present invention relates to a targeted compound linked to a mTOR inhibitory bone disease therapeutic agent.

Novel mTOR inhibitor compounds and the use thereof

The novel mTOR inhibitor compounds of the present invention are capable of selective drug delivery to bone and released slowly in bone for a long period of time. The present invention relates to a targeted compound linked to a mTOR inhibitory bone disease therapeutic agent.

Compound comprising Hsp90 inhibitor targeting mitochondria and pharmaceutical composition for photodynamic therapy comprising the compound

The present invention relates to mitochondrial target Hsp90 inhibitor-based compounds and pharmaceutical compositions for photodynamic therapy comprising the same. According to the present invention, provided are compounds obtained by conjugating an indocyanine derivative and a purine derivative, a diastereomer thereof, or a pharmaceutically acceptable salt thereof. The present invention relates to compositions for photodynamic diagnosis, treatment or cancer treatment comprising the above compounds, diastereomer, and salt as active ingredients.

Degradable hydrogel under physiological conditions

The present invention discloses a hydrogel that can be degraded under physiological conditions. The hydrogel includes at least one backbone moiety and an optional crosslinking moiety, and biodegradable linkers connecting backbone moieties and crosslinking moieties can be degraded by intramolecular cyclization.

Design, Synthesis, and Evaluation of Lipopeptide Conjugates of Mercaptoundecahydrododecaborate for Boron Neutron Capture Therapy

We developed new 10B carriers for boron neutron capture therapy (BNCT) that can effectively transport and accumulate boron clusters into cells. These carriers consist of a lipopeptide, mercaptoundecahydrododecaborate (BSH), and a disulfide linker. The carriers were conceived according to the structure of pepducin, a membrane-penetrating lipopeptide targeting protease-activated receptor 1 (PAR1). To improve the membrane permeability of BSH, the structure was optimized using various lipopeptides possessing different peptides and lipid moieties. These synthesized lipopeptides were conjugated with BSH and evaluated for intracellular uptake using T98G glioblastoma cells. Among them, the most effectively incorporated and accumulated in the cells was compound 5 a, which contains a peptide of 13 residues derived from the intracellular third loop of PAR1 and a palmitoyl group. For further improvement of 10B accumulation in cells, the introduction of an amine linker was investigated; intracellular uptake similar to that of 5 a was observed for compound 14, which has a piperazine linker. Both compounds 5 a and 14 showed a stronger radiosensitizing effect than BSH along on T98G cells under mixed-neutron beam irradiation. The results demonstrate that lipopeptide conjugation is effective for enhancing intracellular delivery and accumulation of BSH and improving the cytotoxic effect of BNCT.

INSULIN ANALOG DIMERS

Disclosed herein are insulin analog dimers having unique insulin receptor agonist activity based on insulin polypeptide sequences, the site of dimerization and the length of the dimerization linker that connects the two insulin polypeptides. In accordance with one embodiment the first and second insulin polypeptide are independently a two chain insulin analog or a single chain analog and the first and second insulin polypeptides are linked to one another via a B29-B29′, B1-C8, B1-B1 or C8-C8 linkage.

FRET-based imaging of transbilayer movement of pepducin in living cells by novel intracellular bioreductively activatable fluorescent probes

To elucidate the mechanisms of direct transmembrane penetration of pepducins, which are artificial lipopeptide G protein-coupled receptor (GPCR) modulators, we developed two types of FRET-based probes, Pep13-FL-SS-Dab (13) targeting the inner leaflet of the lipid bilayer and Pep13-Dab-SS-FL (14) targeting the cytosol, respectively. They are composed of a pepducin moiety and a fluorescent switch component consisting of 5(6)-carboxyfluorescein (FAM) as a fluorophore and dabcyl as a quencher connected through disulfide bond linkage. When they are internalized into the cytosol, intracellular glutathione can cleave the disulfide bond to release the quencher, which results in a turn-on fluorescence signal. Using these probes, we performed live cell imaging of transbilayer movements of pepducins on MCF-7 cells for the first time. The results suggested that the lipid moiety of the probes facilitated pepducin flipping across and tethering to the membrane. The present study raises the possibility of applying the probe architecture for direct intracellular drug delivery. The Royal Society of Chemistry 2013.

Access to biomolecular assemblies through one-pot triple orthogonal chemoselective ligations

Three into one will go: The consecutive combination of three orthogonal chemoselective reactions (oxime ligation, thioether addition, and copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC)) in a sequential one-pot approach allows the syntheses of highly sophisticated biomolecular compounds without intervening isolations and protection schemes (see picture; ODN=oligodeoxynucleotide).