化合物HMN176 T3643

Product Introduction
Bioactivity


英文名: HMN-176

描述: HMN176 是一种二苯乙烯衍生物，可抑制有丝分裂，干扰 polo 样激酶-1 (PLK1)

细胞实验: Cells to be tested are seeded into a 96-well microplate at a density of 3 ×103-1×104 cells/well. Drugs are added the next day and the plate is incubated for 72 h at 37 °C in a humidified incubator (5% CO2, 95% air). The inhibition of growth is measuredby the MTT assay, and the concentration required to produce 50% inhibition of growth (IC50) calculated by the Scansoft 96 software program. The IC50 values for HMN-176 andreference agents are presented. Briefly, for each compound the mean IC50 value for all cell lines tested is calculated and the difference between the individual IC50 values and the mean IC50 value (log10) displayed by a bar projecting to the right or left of the mean. The resistance index is calculated as (IC50 value for drug-resistant cell line)/(IC50 for parent cell line).

体外活性: HMN-176 (2.5 μM) significantly increases the duration of mitosis in hTERT-RPE1 and CFPAC-1 Cell lines. The effect of HMN-176 on spindle morphology does not appear to be related to effects on microtubule polymerization. HMN-176 (2.5, 0.25, and 0.025 μM) inhibits aster formation in a concentration dependent manner[1]. HMN-176 (0.1, 1.0, or 10.0 µg/mL) demonstrates inhibitory effects in multiple tumors, with notable activity seen in breast, nonsmall-cell lung, and ovarian cancer specimens. HMN-176 demonstrates activity towards 63% of the breast (5/8), 67% of the non-small cell lung (4/6), and 57% of the ovarian (4/7) tumor specimens treated with 10.0 µg/mL[2]. HMN-176 shows potent cytotoxicity, with a mean IC50 value of 118 nM. HMN-176 displays similar cytotoxicity against tumors with various characteristics from different organs[3]. Treatment with 3 μM HMN-176 suppresses the expression of MDR1 mRNA by 56%. HMN-176 has no significant effect on the residual promoter activity[4].

体内活性: HMN-176 prevents spindle assembly and meiosis in Spisula oocytes by inhibiting centrosome-dependent MT nucleation, i.e., aster formation. Oocytes treated with 0.25 μM HMN-176 undergoes GVBD, but asters or spindles fails to form, even after prolonged periods[1]. After p.o. of HMN-214 to male rats, the prodrug is not detected in the plasma, while plasma levels of HMN-176 peaks at 2 h and gradually decreases thereafter[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (130.74 mM)


关键字: HMN 176 | HMN-176 | Polo-like Kinase (PLK) | HMN176 | Inhibitor | inhibit

相关产品: Poloxime | Rigosertib sodium | MLN0905 | Onvansertib | Ro3280 | ON1231320 | Poloxin | BI 2536 | TC-S 7005 | Wortmannin

相关库: Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Preclinical Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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