ysl 109 | Cytotoxic evaluation of YSL ysl 109 YSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames .
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0 · Cytotoxic evaluation of YSL
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YSL-109 was synthesized in our laboratory following a previously reported method (Sixto-Lopez et al. 2020, 2021). Trichostatin A (TSA), a pan-HDAC inhibitor, was purchased from Enzo Life Sciences (Farmingdale, NY). See moreMDA-MB-231 and NIH-3T3 cell lines were cultured in 75 cm2 bottles in Dulbecco’s modified Eagle’s medium (DMEM Gibco, Life Technologies, . See moreAn in silico toxicological risk assessment was performed to predict the preclinical toxicological properties of YSL-109. To this end, ProTox-II (Banerjee et al. 2018), Lazar (lazy structure–activity relationships) (Maunz et al. 2013), T.E.S.T. (Toxicity Estimation Software . See moreFirst, cell lines were cultured in 75 cm2 bottles. Once the cells achieve an 80% of confluently, they were counted and 1 × 104 of cells were . See more
Six female CD-1 mice (20 ± 2 g) were obtained from the Facultad de Estudios Superiores Iztacala, UNAM (FES-Iztacala, UNAM). Animals were housed in a temperature and light . See moreYSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames .
YSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames test, whereas YSL-109 did not show in vivo genotoxicity and its oral acute toxicity (LD 50) in CD-1 female mice was higher than 2000 mg/kg, which is .YSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames test, whereas YSL-109 did not show in vivo genotoxicity and its oral acute toxicity (LD 50) in CD-1 female mice was higher than 2000 mg/kg, which is in agreement with our in silico predictions. YSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames test, whereas YSL-109 did not show in vivo genotoxicity and its oral acute toxicity (LD50) in CD-1.
3-(naphthalen-1-yl)-1-oxopropan-2-yl) benzamide (YSL-109), was assayed on TNBC cell line (MDA-MB231) showing an antiproliferative activity ( IC 50 = 50.34 ± 1.11 µM), whereas on broblast, it was lesser toxic. YSL-109 inhibited HDAC6 in a highly selective manner (0.537 nM) compared with HDAC8 and HDAC1, and showed 4000-fold selectivity (Table 4). Thus, YSL-109 is a highly selective HDAC6 inhibitor that is more potent than TSA (Fig. 6) or the other inhibitors that have been reported [7].
Therefore, in this work, an HDAC6 selective inhibitor, the (S)-4-butyl-N-(1-(hydroxyamino)-3-(naphthalen-1-yl)-1-oxopropan-2-yl) benzamide (YSL-109), was assayed on TNBC cell line (MDA-MB231) showing an antiproliferative activity (IC50 = 50.34 ± 1.11 µM), whereas on fibroblast, it was lesser toxic. Cytotoxic evaluation of YSL-109 in a triple negative breast cancer cell line and toxicological evaluations. Sixto-López Y1, Ordaz-Pichardo C2, Gómez-Vidal JA3, Rosales . Of all the compounds evaluated, YSL-109 showed the best activity against hepatocellular carcinoma (HepG2 cell line, IC 50 = 3.39 µM), breast cancer (MCF-7 cell line, IC 50 = 3.41 µM; HCC1954.
An HDAC6 selective inhibitor, the (S)-4-butyl-N-(1-(hydroxyamino)-3-(naphthalen-1-yl)-1-oxopropan-2-yl) benzamide (YSL-109), was assayed on TNBC cell line showing an antiproliferative activity and the toxicological profile was explored.Of all the compounds evaluated, YSL-109 showed the best activity against hepatocellular carcinoma (HepG2 cell line, IC50 cell line, IC50 = ic50 = 6.42 μM). 259.439 μM. = 3.41 μM) and. YSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames test, whereas YSL-109 did not show in vivo genotoxicity and its oral acute toxicity (LD 50) in CD-1 female mice was higher than 2000 mg/kg, which is .
YSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames test, whereas YSL-109 did not show in vivo genotoxicity and its oral acute toxicity (LD 50) in CD-1 female mice was higher than 2000 mg/kg, which is in agreement with our in silico predictions. YSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames test, whereas YSL-109 did not show in vivo genotoxicity and its oral acute toxicity (LD50) in CD-1.3-(naphthalen-1-yl)-1-oxopropan-2-yl) benzamide (YSL-109), was assayed on TNBC cell line (MDA-MB231) showing an antiproliferative activity ( IC 50 = 50.34 ± 1.11 µM), whereas on broblast, it was lesser toxic. YSL-109 inhibited HDAC6 in a highly selective manner (0.537 nM) compared with HDAC8 and HDAC1, and showed 4000-fold selectivity (Table 4). Thus, YSL-109 is a highly selective HDAC6 inhibitor that is more potent than TSA (Fig. 6) or the other inhibitors that have been reported [7].
Therefore, in this work, an HDAC6 selective inhibitor, the (S)-4-butyl-N-(1-(hydroxyamino)-3-(naphthalen-1-yl)-1-oxopropan-2-yl) benzamide (YSL-109), was assayed on TNBC cell line (MDA-MB231) showing an antiproliferative activity (IC50 = 50.34 ± 1.11 µM), whereas on fibroblast, it was lesser toxic.
Cytotoxic evaluation of YSL-109 in a triple negative breast cancer cell line and toxicological evaluations. Sixto-López Y1, Ordaz-Pichardo C2, Gómez-Vidal JA3, Rosales . Of all the compounds evaluated, YSL-109 showed the best activity against hepatocellular carcinoma (HepG2 cell line, IC 50 = 3.39 µM), breast cancer (MCF-7 cell line, IC 50 = 3.41 µM; HCC1954.
An HDAC6 selective inhibitor, the (S)-4-butyl-N-(1-(hydroxyamino)-3-(naphthalen-1-yl)-1-oxopropan-2-yl) benzamide (YSL-109), was assayed on TNBC cell line showing an antiproliferative activity and the toxicological profile was explored.
Cytotoxic evaluation of YSL
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ysl 109|Cytotoxic evaluation of YSL
