化合物AS 602801 T2675

Product Introduction
Bioactivity


英文名: Bentamapimod

描述: Bentamapimod (AS 602801) 是一种ATP 竞争性的JNK 抑制剂，对JNK1、JNK2和JNK3的IC50分别为 80、90 和 230 nM。

细胞实验: AS 602801 (AS602801) is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media before use[2]. PANC-1, A2780, and A549 human cancer cells and IMR90 human normal fibroblasts are treated without (control) or with the indicated concentrations of AS 602801 (2.5, 5, and 7.5 μM) for 3 days. The number of viable cells (left panels) and the percentage of dead cells (right panels) are determined using trypan blue as a vital dye[2].

体外活性: AS 602801 (AS602801) treatment induces cell death and accordingly decreased the number of viable cells in all three cell lines in a dose-dependent manner, suggesting that AS 602801 may have selective cytotoxic activity against neoplastic cells. AS 602801 exhibits cytotoxicity against both serum-cultured non-stem cancer cells and cancer stem cells derived from human pancreatic cancer, non-small cell lung cancer, ovarian cancer and glioblastoma at concentrations that did not decrease the viability of normal human fibroblasts. AS 602801 also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving AS 602801 treatment[2].

体内活性: Treatment of nude mice bearing xenografts biopsied from women with endometriosis (BWE) with 30 mg/kg AS 602801 (AS602801) causes 29% regression of lesion. Medroxyprogesterone acetate (MPA) or progesterone (PR) alone did not cause regression of BWE lesions, but combining 10 mg/kg AS 602801 with MPA caused 38% lesion regression. In human endometrial organ cultures (from healthy women), treatment with AS 602801 or MPA reduced matrix metalloproteinase-3 (MMP-3) release into culture medium. In organ cultures established with BWE, PR or MPA failed to inhibit MMP-3 secretion, whereas AS 602801 alone or MPA + AS 602801 suppresses MMP-3 production. In an autologous rat endometriosis model, AS 602801 causes 48% regression of lesions compared to GnRH antagonist Antide (84%). AS 602801 reduces inflammatory cytokines in endometriotic lesions, while levels of cytokines in ipsilateral horns are unaffected. Furthermore, AS 602801 enhances natural killer cell activity, without apparent negative effects on uterus[3].

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

溶解度: DMSO : 4.57 mg/mL (9.98 mM)


关键字: inhibit | AS602801 | JNK | Inhibitor | Bentamapimod | AS-602801

相关产品: 15-Methoxypinusolidic acid | Vincristine | Juglanin | JNK-1-IN-2 | Guggulsterone | n-Butyl α-D-fructofuranoside | CC-401 Hydrochloride | JNK-IN-12 | Shizukaol B | Isoangustone A

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-COVID-19 Compound Library | Pyroptosis Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Apoptosis Compound Library | Anti-Pancreatic Cancer Compound Library

化合物AS 602801 T2675信息由TargetMol中国为您提供，如您想了解更多关于化合物AS 602801 T2675报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途