mg-63 cells

PI-1840 是一种高效的、选择性的蛋白酶体chymotrypsin-like (CT-L)抑制剂，IC50=27nM。

Imatinib Mesylate (STI571 Mesylate) 是一种多靶点受体酪氨酸激酶抑制剂，可选择性抑制 BCR ABL、v-Abl、PDGFR、c-kit 等激酶活性，具有口服活性。Imatinib Mesylate 具有抗肿瘤活性，可用于治疗慢性粒细胞白血病。

Rifampicin (Rifamycin AMP) 是一种广谱抗生素。Rifampicin 对结核杆菌有较强抗菌作用，对革兰氏阳性或阴性细菌、病毒等也有疗效。

Tetracycline 是一种具有口服活性的广谱抗生素，对多种革兰氏阳性菌、革兰氏阴性菌、衣原体、支原体和立克次体具有抑制活性，常用于抗感染研究，也可用于诱导基于BCR-ABL基因沉默的肿瘤消退。

Imatinib (STI571) 是一种多靶点受体酪氨酸激酶抑制剂，可选择性抑制 BCR ABL、v-Abl、PDGFR、c-kit 等激酶活性，具有口服活性。Imatinib 具有抗肿瘤活性，可用于治疗慢性粒细胞白血病。

Ganoderic acid A 能够抑制 JAK-STAT3信号通路，也能抑制细胞增殖，存活率和 ROS。 它对人骨肉瘤 HOS 和MG-63细胞具有增殖抑制、凋亡和侵袭抑制作用。

Seocalcitol is an analog of vitamin D, binds vitamin D receptor protein from human osteosarcoma MG-63 cells(Kd : 0.27 nM).

Tubulin polymerization-IN-71 (Compound 4k) 是一种微管蛋白聚合抑制剂，其IC50为3.06 μM。该化合物能够抑制癌细胞MG-63和U2OS的增殖，IC50范围在0.08-0.14 μM。Tubulin polymerization-IN-71 可在G2 M期阻滞细胞周期，并在MG-63细胞中诱导细胞凋亡 (apoptosis)。

SHS4121705 is an orally bioavailable mitochondrial uncoupler.1It increases oxygen consumption rate in L6 rat myoblast cells with an EC50value of 4.3 μM. SHS4121705 (25 mg/kg per day in the diet) reduces hepatic steatosis, liver triglyceride levels, and plasma alanine aminotransferase (ALT) levels in Stelic animal model (STAM) mice, a model of non-alcoholic steatohepatitis (NASH). 1.Salamoun, J.M., Garcia, C.J., Hargett, S.R., et al.6-Amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol derivatives as efficacious mitochondrial uncouplers in STAM mouse model of nonalcoholic steatohepatitisJ. Med. Chem.63(11)6203-6224(2020)

CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β and the levels of chemokine (C-X-C motif) ligand 10 (CXCL10), and IL-6 in peripheral blood mononuclear cells (PBMCs) when used at a concentration of 10 μM. It also reduces tumor growth in a CT26 murine colon cancer model when administered at a dose of 0.15, but not 1.5, mg/kg. 1.Xi, Q., Wang, M., Jia, W., et al.Design, synthesis, and biological evaluation of amidobenzimidazole derivatives as stimulator of interferon genes (STING) receptor agonistsJ. Med. Chem.63(1)260-282(2019)

CAY10762 is an inhibitor of monoacylglycerol lipase (MAGL; IC50= 34.1 nM).1It reduces hydrogen peroxide-induced lactate dehydrogenase (LDH) release from Neuro2a cells when used at a concentration of 1 μM. CAY10762 (10 mg kg) increases levels of 2-arachidonoyl glycerol in mouse brain. 1.Castelli, R., Scalvini, L., Vacondio, F., et al.Benzisothiazolinone derivatives as potent allosteric monoacylglycerol lipase inhibitors that functionally mimic sulfenylation of regulatory cysteinesJ. Med. Chem.63(3)1261-1280(2020)

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16 F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

HSGN-218 is a gut-restrictive antibiotic.1It is active againstC. difficile(MIC = 0.007 μg/ml) and clinical isolates ofC. difficile(MICs = 0.003-0.03 μg/ml) and is not cytotoxic to Caco-2 cells when used at concentrations ranging from 4 to 64 μg/ml. HSGN-218 (50 mg/kg) increases survival and protects mice fromC. difficilerecurrence in mouse models ofC. difficileinfection. 1.Naclerio, G.A., Abutaleb, N.S., Li, D., et al.Ultrapotent inhibitor of Clostridioides difficile growth, which suppresses recurrence in vivoJ. Med. Chem.63(20)11934-11944(2020)

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).1It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 μM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 μM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day. 1.Wang, G., Zhao, Y., Liu, Y., et al.Discovery of a novel dual-target inhibitor of ERK1 and ERK5 that induces regulated cell death to overcome compensatory mechanism in specific tumor typesJ. Med. Chem.63(8)3976-3995(2020)

CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg. 1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020)

Sweroside 是分离自Lonicera japonica 中，具有细胞保护、抗骨质疏松和保护肝脏活性。

Antitumor agent-61 (Compound 9b)，Irinotecan (Ir)的衍生物，展现出对多种肿瘤细胞（包括SK-OV-3、SK-OV-3 CDDP、U2OS、MCF-7、A549与MG-63）具有显著的抑制效果，其IC50值分别为0.92、1.39、1.75、2.20、3.05和3.23 μM。该化合物主要通过线粒体途径引发SK-OV-3细胞的凋亡。

CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂（IC50分别为5.35、4.6、28、28和78 nM）。该化合物对这些激酶的选择性高于FGFR4（IC50 > 1,000 nM），但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体（IGF-1R；IC50分别为67、33、36和75 nM），以及EGFR、布鲁顿酪氨酸激酶（BTK）、细胞周期依赖性激酶4（Cdk4）/cyclin D3和MET（IC50分别为128、198、214和396 nM）。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖（IC50分别为0.84、0.76、1.36和0.72 µM）。在0.3和0.5 µM的浓度下，它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292（30 mg/kg）在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。

Tubulin polymerization-IN-67 (Compound 5h) 作为秋水仙碱结合位点的抑制剂,能够阻断微管蛋白聚合,其 IC50 值为 2.92 μM.在癌细胞系 HT29、A549、U2OS、MG-63 以及 HeLa 中,该化合物展现出显著的抑制增殖作用,IC50 范围为 0.12-4.13 μM.此外,Tubulin polymerization-IN-67 在 G2 M 期阻滞细胞周期,并在 U2OS 细胞中诱导细胞凋亡 (apoptosis),在 A549 细胞中抑制细胞迁移.该化合物还能够降低线粒体膜电位 (MMP),增加 ROS 水平,并在 HUVEC 细胞中抑制血管生成,显示出在小鼠体内的抗肿瘤活性.