Design,Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders

Lysine demethylase 5 C (KDM5C) controls epigenetic gene expression and is attracting great interest in the field of chemical epigenetics. KDM5C has emerged as a therapeutic target for anti-prostate cancer agents, and recently we identified triazole 1 as an inhibitor of KDM5C. Compound 1 exhibited highly potent KDM5C-inhibitory activity in in vitro enzyme assays, but did not show strong anticancer effects. Therefore, a different approach is needed for the development of anticancer agents targeting KDM5C. Here, we attempted to identify KDM5C degraders by focusing on a protein-knockdown strategy. Compound 3 b , which was designed based on compound 1 , degraded KDM5C and inhibited the growth of prostate cancer PC-3 cells more strongly than compound 1 . These findings suggest that KDM5C degraders are more effective as anticancer agents than compounds that only inhibit the catalytic activity of KDM5C.     

Ramp‐setup design technique in three‐electrode surface‐discharge ACPDPs

Abstract— A simple model to calculate changes in wall voltage during weak discharge in three‐electrode ACPDPs was developed. A change in the wall voltage vector has an intrinsic direction for each discharge, which not only reveals the basis of problems in the ramp setup but also simplifies the analysis of cell operation during setup. New ramp‐setup waveforms designed for this model widened the operating margin.     

Comparison of MTBF in the parallel string configuration and the quad configuration systems

In this study, four redundant systems having the parallel string configuration and the quad configuration consisting of 2n identical units are considered and the reliability of each system and MTBF (Mean Time Between Failures) are evaluated. Next, as the special case of the systems in this study, the case of four units corresponds to the Keene's system and MTBF of each system agreed with his results. Further, as the results evaluated MTBF relating to each system consisting of 6, 8 and 10 units, the large and small relations of the MTBF between systems are made clear.     

Dependence of strength and fracture behaviour on chemical compositions in spot-welded L-type joints

In order to achieve lighter and stronger car bodies by applying high strength steel sheets, one of the key technologies is enhancement of joint strength. In this study, we investigated dependence of strength and fracture behaviour on chemical compositions of steels in spot-welded L-type joints in detail. Consequently, the following experimental results were obtained. (1) Maximum load of the joint decreased with increase of carbon (C) and phosphorous (P). The maximum load was decreased by 0.4–0.7 kN with increase of 0.1% in C, with C content ranging from 0.03 to 0.5%, and 0.5 kN with increase of 0.01% in P, with P content ranging from 0 to 0.03%. (2) Fracture portion changed from the outside to the inside of weld metal with increase of C and P. (3) The fracture path was estimated to accord with the solidification segregation site in the weld metal in the case of a steel of 0.2% C, 0.03% P. (4) By implementation of an appropriate post heat during spot welding process for the steel of 0.2% C, 0.03% P, the degree of solidification segregation was clearly reduced and the maximum load of the joints was improved by 70%.     

Performance and internal flow of sirocco fan using contra-rotating rotors

A sirocco fan using contra-rotating rotors in which an inner rotor is settled inside the sirocco fan rotor and each rotor rotates in an opposite direction was proposed for the purpose of getting the higher pressure and making the structure of a sirocco fan more compact. If the high discharge pressure is obtained with the adoption of the contra-rotating rotors, it could be used for various purposes. Pressure coefficient of a sirocco fan with contra-rotating rotors is 2.5 times as high as the conventional sirocco fan and the maximum efficiency point of contra-rotating rotors shifts to larger flow rate than a conventional sirocco fan. On the other hand, it was clarified from the flow measurement results that circumferential velocity component at the outlet of the outer rotor of contra-rotating ro- tors becomes larger than a conventional one. In the present paper, the performance of a conventional sirocco fan and a sirocco fan with contra-rotating rotors are shown and the internal flow field at the outlet of outer rotor of both cases is clarified. Then, the effect of different kind of contra-rotating rotors on the performance and internal flow field is investigated and the rotor design with higher performance would be discussed.     

Epitaxial growth of lithium niobate film using metalorganic chemical vapor deposition

Lithium niobate films grown epitaxially on sapphire substrate were prepared using a thermal chemical vapor deposition method from the metalorganic compounds Li(C₁₁H₁₉O₂) and Nb(OC₂H₅)₅. The range of operating conditions for obtaining pure epitaxially grown LiNbO₃ without other oxides is within that for obtaining pure polycrystalline LiNbO₃ grown on silicon substrate. On analyzing the composition of the epitaxially grown LiNbO₃ film, the composition of the film was similar to that of the LiNbO₃ solid solution in the phase diagram of the Li-Nb composite oxide obtained for crystal growth from a molten solution.     

Joint strength and behaviour of coated aluminium in laser lap welding of steel sheets

When galvanized steel sheets are closely overlapped and welded by laser lap welding, a large amount of molten metal spatters, resulting in a poor surface appearance of the weld and weakened strength of the welded joint, as compared with that of cold-rolled steel sheets. Whereas in the case of aluminium-coated steel sheets, even when they are closely overlapped and welded by laser lap welding, no spattering occurs. Thus, a good surface appearance of the weld is obtained, but the welded joint has lower strength. In both the mentioned cases, it is known that if a clearance of about 0.1 mm is provided between the steel sheets, laser lap welding produces a good surface appearance of the weld and the welded joint strength equal to that of the cold-rolled steel sheets. This report discusses specifically how, in laser lap welding of overlapped Al-coated steel sheets, Al of the coated layer comes to enter the weld metal, also specifically how to reduce the joint strength, as well as what behaviours of Al are present when a clearance is provided between the steel sheets. When the steel sheets are closely overlapped and welded, Al becoming molten on the base metal side of the bond of the overlapped face becomes swallowed up by the bath streams of the molten pool, flowing into the molten pool, then forming the Fe–Al intermetallic compound, while not being sufficiently stirred. It is considered that when subjected to the tensile shear test, the Fe–Al intermetallic compound starts to fracture, thereby causing a partial loss of the weld metal and a reduction in the joint strength. On the other hand, when a clearance is provided between the steel sheets, it may be inferred that the fusion Al on the base metal side of the bond stays in place without flowing into the molten pool, consequently not forming the Fe–Al intermetallic compounds within the weld metal.     

Power attenuation and focus shift of solid state laser beam caused by laser-induced plume

Currently, remote laser welding using solid-sate lasers is widespread in industry. Meanwhile, it is well known that the laser-induced plume blown up from the processing point affects penetration in laser welding, through the attenuation and the refraction of the laser beam. These phenomena in carbon dioxide laser welding have been investigated well and it is widely recognized that using the shielding gas flow to blow away the laser-induced plume is very important. However, in remote laser welding it is not easy to maintain the shielding gas flow to the processing point. By the way, these phenomena depend on the wavelength of the laser. So, quantitative knowledge of the attenuation and refraction of the solid state laser beam are necessary in achieving stable penetration in remote laser welding with this laser. This study was made to determine the attenuation coefficient and the amount of the effective focus shift caused by refraction of the laser beam in the plume, through melt run experiments with a YAG laser. The attenuation coefficient of the laser beam was estimated to be 0.00090 mm^?1 from the dependence of the cross-sectional area of weld metal on the laser power and the plume length. This value is about one twentieth of the attenuation coefficient of a carbon dioxide laser beam at welding found in the literature. The amount of focus shift was estimated to be 0.67 mm per 100 mm plume length, from the dependency of penetration depth on the defocusing distance and the plume length. Comparing the 3 mm of plume length, this value is centesimal of the estimated value by Beck et al. [The effect of plasma formation on beam focusing in deep penetration welding with CO₂ lasers. J. Phys. D: Appl. Phys. 1995;28:2430–2442] in CO₂ laser welding. Therefore, a solid-state laser such as a YAG laser is considered to be a suitable laser source for remote laser welding.     

Spin-current-driven thermoelectric coating

Energy harvesting technologies, which generate electricity from environmental energy, have been attracting great interest because of their potential to power ubiquitously deployed sensor networks and mobile electronics. Of these technologies, thermoelectric (TE) conversion is a particularly promising candidate, because it can directly generate electricity from the thermal energy that is available in various places. Here we show a novel TE concept based on the spin Seebeck effect, called 'spin-thermoelectric (STE) coating', which is characterized by a simple film structure, convenient scaling capability, and easy fabrication. The STE coating, with a 60-nm-thick bismuth-substituted yttrium iron garnet (Bi:YIG) film, is applied by means of a highly efficient process on a non-magnetic substrate. Notably, spin-current-driven TE conversion is successfully demonstrated under a temperature gradient perpendicular to such an ultrathin STE-coating layer (amounting to only 0.01% of the total sample thickness). We also show that the STE coating is applicable even on glass surfaces with amorphous structures. Such a versatile implementation of the TE function may pave the way for novel applications making full use of omnipresent heat.     

Effect of magnetic field strength and admixture gas on current interrupting capability of a CO2 rotary‐arc load‐break switch

First, current interrupting experiments were performed for a rotary‐arc type of load‐break switch filled with pure CO₂ at a total pressure of 0.1 MPa. Increase in the coil turns for generating magnetic field from 1 to 1.8, 2.5, and 3.6 (arbitrary unit) raised the current interrupting capability from 2.6 kA to 3.2, 3.5, and 4.1 kA. Second, experiments were performed for CO₂ gas mixture under the condition of 3.6 coil turns. Gases of He, O₂, N₂, and air were admixted to CO₂. Adding either He or O₂ to CO₂ at a concentration of 30% allows the switch to have higher interrupting capability than using pure CO₂. © 2009 Wiley Periodicals, Inc. Electr Eng Jpn, 167(2): 21–27, 2009; Published online in Wiley InterScience ( www.interscience.wiley.com ). DOI 10.1002/eej.20742