Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)‑<i>s</i>‑triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Signaling Cascades by Ihab Shawish (13015516)

“…<i>N</i>-(4-Bromophenyl)-4-(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-6-morpholino-1,3,5-triazin-2-amine <b>4f</b>, <i>N</i>-(4-chlorophenyl)-4,6-bis­(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-1,3,5-triazin-2-amine <b>5c</b>, and 4,6-<i>bis</i>(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-<i>N</i>-(4-methoxyphenyl)-1,3,5-triazin-2-amine <b>5d</b> showed promising activity against these cancer cells: <b>4f</b> [(IC₅₀ = 4.53 ± 0.30 μM (MCF-7); 0.50 ± 0.080 μM (HCT-116); and 3.01 ± 0.49 μM (HepG2)]; <b>5d</b> [(IC₅₀ = 3.66 ± 0.96 μM (HCT-116); and 5.42 ± 0.82 μM (HepG2)]; and <b>5c</b> [(IC₅₀ = 2.29 ± 0.92 μM (MCF-7)]. …”

Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)‑<i>s</i>‑triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Signaling Cascades by Ihab Shawish (13015516)

“…<i>N</i>-(4-Bromophenyl)-4-(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-6-morpholino-1,3,5-triazin-2-amine <b>4f</b>, <i>N</i>-(4-chlorophenyl)-4,6-bis­(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-1,3,5-triazin-2-amine <b>5c</b>, and 4,6-<i>bis</i>(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-<i>N</i>-(4-methoxyphenyl)-1,3,5-triazin-2-amine <b>5d</b> showed promising activity against these cancer cells: <b>4f</b> [(IC₅₀ = 4.53 ± 0.30 μM (MCF-7); 0.50 ± 0.080 μM (HCT-116); and 3.01 ± 0.49 μM (HepG2)]; <b>5d</b> [(IC₅₀ = 3.66 ± 0.96 μM (HCT-116); and 5.42 ± 0.82 μM (HepG2)]; and <b>5c</b> [(IC₅₀ = 2.29 ± 0.92 μM (MCF-7)]. …”

First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation by Kairui Yue (11874403)

“…Representative inhibitor <b>35m</b> exhibits potent HDAC6 inhibitory activity with an IC₅₀ value of 0.019 μM. To our surprise, <b>35m</b> establishes significant improvement in the pharmacokinetic property with much higher AUC_0‑inf (10292 ng·h/mL) and oral bioavailability (93.4%) than hydroximic acid-based HDAC6 inhibitors Tubastatin A and ACY-1215. …”

First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation by Kairui Yue (11874403)

“…Representative inhibitor <b>35m</b> exhibits potent HDAC6 inhibitory activity with an IC₅₀ value of 0.019 μM. To our surprise, <b>35m</b> establishes significant improvement in the pharmacokinetic property with much higher AUC_0‑inf (10292 ng·h/mL) and oral bioavailability (93.4%) than hydroximic acid-based HDAC6 inhibitors Tubastatin A and ACY-1215. …”

<b>Diroximel fumarate acts through Nrf2 to attenuate methylglyoxal-induced nociception in mice and decrease ISR activation in DRG neurons</b> by Muhammad Saad Yousuf (20745168)

Effects of TGF-β1 on the expression of fibrosis indicators in HBdSMCs and the effects of MEL on the expression of fibrosis indicators in HBdSMCs induced by TGF-β1. by Yang Zhang (30734)

2‑Ethylhexyl Diphenyl Phosphate and Its Hydroxylated Metabolites are Anti-androgenic and Cause Adverse Reproductive Outcomes in Male Japanese Medaka (Oryzias latipes) by Yu Li (183836)

“…Although high concentrations of 2-ethylhexyl diphenyl phosphate (EHDPP) have been detected in wild fish, its reproductive toxicity in fish remains unclear. In this study, we for the first time observed that EHDPP elicited androgen receptor (AR) antagonistic activity with a 50% inhibitory concentration of 37.5 μM. 2-Ethyl-5-hydroxyhexyl diphenyl phosphate was proved to be the dominant metabolite of EHDPP in Japanese medaka and elicited 3.1-fold stronger AR antagonistic activity than that of EHDPP. …”

2‑Ethylhexyl Diphenyl Phosphate and Its Hydroxylated Metabolites are Anti-androgenic and Cause Adverse Reproductive Outcomes in Male Japanese Medaka (Oryzias latipes) by Yu Li (183836)

“…Although high concentrations of 2-ethylhexyl diphenyl phosphate (EHDPP) have been detected in wild fish, its reproductive toxicity in fish remains unclear. In this study, we for the first time observed that EHDPP elicited androgen receptor (AR) antagonistic activity with a 50% inhibitory concentration of 37.5 μM. 2-Ethyl-5-hydroxyhexyl diphenyl phosphate was proved to be the dominant metabolite of EHDPP in Japanese medaka and elicited 3.1-fold stronger AR antagonistic activity than that of EHDPP. …”

The pax7 probe set enables simultaneous detection of all three <i>pax7</i> genes. by Cécile Rallière (86527)

Antibodies used for flow cytometry experiments. by Joseph Rabin (7399436)

“…RA was devoid of serious side effects, and within 24 hours from the start of infusion was associated with increased oxygen saturation (93.8 ± 0.58 vs 96.6 ± 1.08%, P<0.05), decreased D-dimer (754 ± 17 vs 518 ± 98 ng/ml, P<0.05), and a trend toward decreased CRP (3.80 ± 1.40 vs 1.98 ± 0.74 mg/dL, P = 0.075). …”

Subject flow diagram. by Joseph Rabin (7399436)

“…RA was devoid of serious side effects, and within 24 hours from the start of infusion was associated with increased oxygen saturation (93.8 ± 0.58 vs 96.6 ± 1.08%, P<0.05), decreased D-dimer (754 ± 17 vs 518 ± 98 ng/ml, P<0.05), and a trend toward decreased CRP (3.80 ± 1.40 vs 1.98 ± 0.74 mg/dL, P = 0.075). …”

Inhibition of pan- and HDAC isoform activities. by Mira Jung (1277502)

“…Cellular growth inhibition studies show that SP-1-303 differentially inhibits growth of estrogen receptor positive breast cancer (ER+ BC) cells with effective growth inhibition concentrations (EC₅₀) for MCF-7 and T47D cells ranging from 0.32 to 0.34 μM, compared to 1.2–2.5 μM for triple negative breast cancer cells, and ~12 μM for normal breast epithelial cells. …”

Table_1_The Metabolic Changes and Immune Profiles in Patients With COVID-19.pdf by Bing He (135034)

“…Twenty-one severe patients had low PO₂ [57 mmHg (IQR, 50–73)] and SO₂ [90% (IQR, 86–93)] and high lactate dehydrogenase [580 U/L (IQR, 447–696)], cardiac troponin I [0.07 ng/mL (IQR, 0.02–0.30)], and pro-BNP [498 pg/mL (IQR, 241–1,726)]. …”

<i>S</i>. <i>pneumoniae</i> RNA regulators are ligand responsive and most designed mutations function as anticipated. by Indu Warrier (581139)

“…<p><b>(A)</b> β-galactosidase activity of RNA reporter strains grown in the absence and presence of ligand or ligand precursor (0.3 μg/mL thiamine, 140 ng/mL riboflavin, 20 μg/mL uracil, 75 μg/mL glycine, 204 μg/mL tryptophan, 50 μg/mL guanine) demonstrates regulation of gene expression with a significant difference between expression in the two conditions. …”

Image1_Ethyl 2-Succinate-Anthraquinone Attenuates Inflammatory Response and Oxidative Stress via Regulating NLRP3 Signaling Pathway.TIF by Burong Feng (11661529)

“…In vitro, a THP-1 macrophage inflammation model, made by 100 ng/ml phorbol-12-myristate-13-acetate (PMA) and 1 μg/ml LPS for 24 h, was constructed. …”

Image2_Ethyl 2-Succinate-Anthraquinone Attenuates Inflammatory Response and Oxidative Stress via Regulating NLRP3 Signaling Pathway.TIF by Burong Feng (11661529)

“…In vitro, a THP-1 macrophage inflammation model, made by 100 ng/ml phorbol-12-myristate-13-acetate (PMA) and 1 μg/ml LPS for 24 h, was constructed. …”

Image_1_RETRACTED: Modeling Cardiac Dysfunction Following Traumatic Hemorrhage Injury: Impact on Myocardial Integrity.tif by Johanna Wall (8088959)

I-R-Polar-Negative-0902 by Sheng-Yuan Ho (16909464)

“…All analyses were conducted with a lockspray to guarantee precision and reproducibility. As the lockmass, we utilized leucine-enkephalin (m/z = 556.2771) at a concentration of 1 ng/L and a flow rate of 5 L/min. …”

Data_Sheet_1_Identification of novel small molecule inhibitors of twin arginine translocation (Tat) pathway and their effect on the control of Campylobacter jejuni in chickens.pdf by Loïc Deblais (5620073)

“…These selected SMs were non-toxic to colon epithelial (Caco-2) cells when treated with 50 μg/mL for 24 h and completely cleared intracellular C. jejuni cells when treated with 0.63 μg/mL of SM for 24 h in the presence of 0.5 mM of CuSO₄. …”

Aucubin slows the development of osteoporosis by inhibiting osteoclast differentiation via the nuclear factor erythroid 2-related factor 2-mediated antioxidation pathway by Yongfeng Zhang (5963987)

“…Subsequently, 1, 2.5 and 5 µM AU were incubated with 50 ng/mL RANKL-induced RAW264.7 cells for 7 days to observe osteoclast differentiation. …”