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3
Cat. No. | Product Name | Target | Signaling Pathways |
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T6941 |
PI-1840
PI 1840 |
PARP; Proteasome | Chromatin/Epigenetic; DNA Damage/DNA Repair; Proteases/Proteasome; Ubiquitination |
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。 | |||
T19559 |
Seocalcitol
EB 1089 |
Others | Others |
Seocalcitol is an analog of vitamin D, binds vitamin D receptor protein from human osteosarcoma MG-63 cells(Kd : 0.27 nM). | |||
T35762 | MC1742 | ||
MC1742 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.1, 0.11, 0.02, and 0.61 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 7 and 40 nM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb over class IIa HDACs (IC50s = >50 μM for HDAC4, -5, -7, and -9). MC1742 reduces proliferation of HOS, MG-63, RD, A204, SK-ES-1, and A673 sarcoma cancer stem cells (CSCs). It increases levels of acetylated histone H3 and acetylated tubulin... | |||
T74491 | Antitumor agent-61 | ||
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。 | |||
T36498 |
CAY10762
CAY10762 |
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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(... | |||
T38072 | HSGN-218 | ||
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 rec... | |||
T83911 |
CYY292
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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。 | |||
T35636 |
SHS4121705
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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 effic... | |||
T38377 |
ADTL-EI1712
ADTL-EI1712 |
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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 do... | |||
T36645 |
CAY10763
CAY10763 |
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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... | |||
T36461 |
CAY10748
CAY10748 |
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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 an... | |||
T38381 |
CAY17c
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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,... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T6S2252 |
Sweroside
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Others | Others |
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。 | |||
T6S1141 |
Ganoderic acid A
灵芝酸 A,灵芝酸A |
Apoptosis; NF-κB; Endogenous Metabolite; Autophagy | Apoptosis; Autophagy; Metabolism; NF-κB |
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。 | |||
T35779 |
Oosporein
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Oosporein is a mycotoxin that has been found inBeauveriaand has diverse biological activities.1,2It is cytotoxic to Sf9 and Sf21 insect cells with 50% cytotoxic concentration (CC50) values of 4.23 and 10.43 μM, respectively.3Oosporin induces lethality in day-old cockerels (LD50= 6.12 mg/kg).4It inhibits Na+/K+-, Ca2+-, and Mg2+-ATPase activities by 27, 52, and 100%, respectively, in equine erythrocyte ghosts when used at a concentration of 200 μg/ml.2Oosporein inhibits herpes simplex 1 (HSV-1), ... |