TCS 21311

Potent JAK3 inhibitor (IC₅₀ = 8 nM). Selective for JAK3 over JAK1, JAK2 and TYK2 (IC₅₀ values are 1017, 2550 and 8055 nM respectively). Also inhibits GSK-3β, PKCα and PKCθ (IC₅₀ values are 3, 13 and 68 nM respectively).

Rhamnolipid-enhanced aerobic biodegradation of triclosan (TCS) by indigenous microorganisms in water-sediment systems.[Pubmed:27476727]

Sci Total Environ. 2016 Nov 15;571:1304-11.

Bioremediation of triclosan (TCS) is a challenge because of its low bioavailability, persistence in the environment and recalcitrance to remediation efforts. Rhamnolipid (RL) was used to enhance TCS biodegradation by indigenous microbes in an aerobic water-sediment system. However, knowledge of the effects of TCS on the bacterial community and environmental factors in an RL-enhanced, TCS-degrading system are lacking. Therefore, in this study, the influence of environmental factors on RL-enhanced biodegradation of TCS was investigated by single factor experiments, and shifts in aerobic TCS-degrading bacterial populations, with and without RL, were analyzed by high-throughput sequencing technology. The results showed that aerobic biodegradation of TCS was significantly promoted by the addition of RL. Environmental conditions, which included RL addition (0.125-0.5g/L), medium concentrations of TCS (<90mug/g), water disturbance, elevated temperature, ionic strength (0.001-0.1mol/L NaCl) and weak alkaline environments (pH8-9), were monitored. High concentrations of TCS had a remarkable influence on the bacterial community structure, and this influence on the distribution proportion of the main microorganisms was strengthened by RL addition. Alpha-proteobacteria (e.g., Sphingomonadaceae and Caulobacteraceae) might be resistant to TCS or even capable of TCS biodegradation, while Sphingobacteria, Beta- and Delta-proteobacteria were sensitive to TCS toxicity. This research provides ecological information on the degradation efficiency and bacterial community stability in RL-enhanced bioremediation of TCS-polluted aquatic environments.

Commonality between BCS and TCS.[Pubmed:27208656]

Int J Pharm. 2016 Jul 25;509(1-2):35-40.

Both biopharmaceutics classification system (BCS) and topical drug classification system (TCS) are based on sound scientific principles with the aim of providing biowaiver and reducing regulatory burden without lowering the quality requirements and standards of approval for the drug products. BCS is based on the solubility and permeability properties of the active pharmaceutical ingredient (API, or drug substance) whereas the TCS is based on the qualitative and quantitative composition of the dosage form and the in vitro release rate of the active ingredient as key decision tools. Both BCS and TCS take drug release and dissolution as their guiding principle for providing biowaiver, increasing the availability and affordability of safe and effective medicines to the consumers and at the same time maintaining the drug product quality.

Uncertainties in calculated correction factors for true coincidence-summing (TCS).[Pubmed:28161650]

Appl Radiat Isot. 2017 Apr;122:174-179.

The aim of this work was to estimate the uncertainties in Monte Carlo calculated correction factors for true coincidence summing (TCS). In this work TCS-factors and their uncertainties were calculated for (134)Cs and then the corrected activities compared to empirical data. The study was carried out using a close-end coaxial p-type detector (O80mmx54.5mm, 80% relative efficiency) and a cylindrical glass fiber sample (O60mmx14mm). It was shown that the uncertainty in the calculated correction factor for the primary gamma ray was below 0.5%, which means it will not contribute significantly to the combined uncertainty in an activity measurement for e.g. environmental monitoring.

Different culture conditions affect the growth of human tendon stem/progenitor cells (TSPCs) within a mixed tendon cells (TCs) population.[Pubmed:28244027]

J Exp Orthop. 2017 Dec;4(1):8.

BACKGROUND: Tendon resident cells (TCs) are a mixed population made of terminally differentiated tenocytes and tendon stem/progenitor cells (TSPCs). Since the enrichment of progenitors proportion could enhance the effectiveness of treatments based on these cell populations, the interest on the effect of culture conditions on the TSPCs is growing. In this study the clonal selection and the culture in presence or absence of basic fibroblast growth factor (bFGF) were used to assess their influences on the stemness properties and phenotype specific features of tendon cells. METHODS: Cells cultured with the different methods were analyzed in terms of clonogenic and differentiation abilities, stem and tendon specific genes expression and immunophenotype at passage 2 and passage 4. RESULTS: The clonal selection allowed to isolate cells with a higher multi-differentiation potential, but at the same time a lower proliferation rate in comparison to the whole population. Moreover, the clones express a higher amounts of stemness marker OCT4 and tendon specific transcription factor Scleraxis (SCX) mRNA, but a lower level of decorin (DCN). On the other hand, the number of cells obtained by clonal selection was extremely low and most of the clones were unable to reach a high number of passages in cultures. The presence of bFGF influences TCs morphology, enhance their proliferation rate and reduce their clonogenic ability. Interestingly, the expression of CD54, a known mesenchymal stem cell marker, is reduced in presence of bFGF at early passages. Nevertheless, bFGF does not affect the chondrogenic and osteogenic potential of TCs and the expression of tendon specific markers, while it was able to downregulate the OCT4 expression. CONCLUSION: This study showed that clonal selection enhance progenitors content in TCs populations, but the extremely low number of cells produced with this method could represent an insurmountable obstacle to its application in clinical approaches. We observed that the addition of bFGF to the culture medium promotes the maintenance of a higher number of differentiated cells, reducing the proportion of progenitors within the whole population. Overall our findings demonstrated the importance of the use of specific culture protocols to obtain tendon cells for possible clinical applications.

TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.

TCS 21311,1260181-14-3,Natural Products,JAK, buy TCS 21311 , TCS 21311 supplier , purchase TCS 21311 , TCS 21311 cost , TCS 21311 manufacturer , order TCS 21311 , high purity TCS 21311