目录号 | 产品详情 | 靶点 | |
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T83898 | |||
S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine (SFN-Cys) 是一种异硫氰酸酯衍生物及第一类和第二类组蛋白去乙酰化酶(HDAC)抑制剂和抗癌剂硫代硫酸烯醇醚的活性代谢产物。它通过巯基乙酸途径酶从硫代硫酸烯醇醚经DL-硫代硫酸烯醇醚谷胱甘肽和硫代硫酸烯醇醚半胱氨酸甘肽中间体形成。SFN-Cys (20 µM) 通过创伤愈合和腔室分析实验,分别减少了U87MG和U373 MG胶质母细胞瘤细胞的侵袭和迁移。在45 µM的浓度下,它降低了对紫杉醇耐药的A549肺癌细胞(A549/T)中的α-微管蛋白、βIII-微管蛋白、司他敏1和X连锁抑制剂的凋亡(XIAP)的水平,并减少了细胞密度。使用30 µM浓度的SFN-Cys诱导U87MG和U373 MG细胞凋亡和G2/M期细胞周期停滞。 | |||
T73550 | |||
CUR5g 是一种有效的自噬 (autophagy) 抑制剂。CUR5g 通过阻断自噬体-溶酶体融合选择性地抑制癌细胞中的自噬体降解。CUR5g 通过依赖 UVRAG 的机制阻止 STX17 募集到自噬体,导致自噬体无法与溶酶体融合。CUR5g 可提高顺铂 (Cisplatin) 在体外和体内对 A549 细胞的抗癌作用。 | |||
T61823 | |||
Anticancer agent 63 (compound 3h) exhibits significant cytotoxic activity against multiple cancer cell lines, including SW480, HeLa, A549, and MCF-7, with IC 50 values of 4.9, 11.5, 9.4, and 3.4 μM, respectively, after 24 hours of treatment. In particular, Anticancer agent 63 induces apoptosis in MCF-7 cells by down-regulating Bcl-2 expression and up-regulating IL-2 and Caspase-3 expression. Additionally, Anticancer agent 63 demonstrates antioxidative properties [1]. | |||
T60793 | |||
Tubulin inhibitor 26 (compound 3c) 是一种吲唑衍生物,是微管蛋白抑制剂,对 HepG2、HCT116、SW620、HT29 和 A549 癌细胞系具有显著的低纳摩尔效力。Tubulin inhibitor 26 抑制G2/M 期肿瘤细胞,并且诱导细胞凋亡。Tubulin inhibitor 26 在体内抑制肿瘤生长,并且不影响小鼠体重。 | |||
T72475 | |||
Anticancer agent 58 对多种癌细胞具有抑制活性,特别是在 A549 和 T24 细胞中,IC50分别为 0.6 μM 和 0.7 μM。Anticancer agent 58 通过激活 caspase3/8/9活性诱导细胞凋亡 (apoptosis),也诱导 Ca2+和 ROS 水平升高。Anticancer agent 58 在 T24 异种移植小鼠模型中能显著抑制肿瘤生长。 | |||
T63676 | |||
Bcl-2-IN-6 是 Bcl-2 (b 细胞淋巴瘤-2) 的有效抑制剂,可下调 Bcl-2 的表达,并提高 p53、Bax、caspase-7 mRNA 的表达。Bcl-2-IN-7 能够诱导乳腺癌 MCF-7 细胞周期阻滞和凋亡。Bcl-2-IN-7 能够作用于 MCF-7 细胞 (IC50: 20.91 μM)、LoVo 细胞 (IC50: 22.30 μM)、HepG2 细胞 (IC50: 42.29 μM) 和 A549 细胞 (IC50: 48.00 μM) 均显示出良好的抗肿瘤效果。 | |||
T79275 | Histone Methyltransferase | ||
Antiproliferative agent-25 (Compound 3s4)作为一种选择性PRMT5抑制剂(IC50: 0.11 μM),能够上调hnRNP E1蛋白水平,并通过与SAM及PRMT5的E444残基形成氢键相互作用。该化合物通过促进apoptosis和抑制细胞迁移,有效抑制A549细胞的增殖。此外,Antiproliferative agent-25在人和大鼠肝微粒体中的高清除率表明,其T1/2分别为21.8和4.7分钟。 | |||
T79274 | Histone Methyltransferase | ||
PRMT5-IN-31(Compound 3m)作为一种高选择性PRMT5抑制剂,其IC50为0.31 μM。它能够通过占据PRMT5的底物位点以及与氨基酸残基形成必要相互作用来上调hnRNP E1蛋白水平。此外,PRMT5-IN-31能有效抑制A549细胞增殖,其机制涉及诱导apoptosis和阻碍细胞迁移。该化合物在人肝微粒体中表现出较高的代谢稳定性,半衰期为132.4分钟。 | |||
TN3009 | Others | ||
6-Prenylapigenin(4',5,7-Trihydroxy-6-prenylflavone) shows potent inhibitory activity on melanin formation, it may be potential sources for skin whitening agents. It also shows moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarci | |||
T63494 | |||
Antitumor agent-60 是有效的抗肿瘤药物,靶向RAS-RAF 信号通路,可与CRAF 结合 (Kd: 721.3 nM)。Antitumor agent-60 能增加癌细胞中p53和ROS 水平,使细胞核呈椭圆形和不规则形态。Antitumor agent-60 够将细胞的细胞周期阻滞在 G2/M 期,并诱导细胞凋亡 (apoptosis)。在 A549 肿瘤移植模型中,Antitumor agent-60 具有一定的抑制肿瘤生长能力。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPK-00305 | TGFBR1 Protein, Human, Recombinant (mFc & Avi) | Human | HEK293 Cells | ||
transforming growth factor beta receptor 1 (TGFBR1), a key stimulator of tumor proliferation and metastasis, was a direct target of miR‑98‑5p. miR‑98‑5p overexpression resulted in the downregulation of TGFBR1 and the suppression of the viability, proliferation, migration and invasion of A549 and H1299 cells. TGFBR1 Protein, Human, Recombinant (mFc & Avi) is expressed in HEK293 mammalian cells with C-mFc-Avi tag. The predicted molecular weight is 38.2 kDa and the accession number is P36897-1.
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TMPK-00306 | TGFBR1 Protein, Human, Recombinant (mFc & Avi), Biotinylated | Human | HEK293 Cells | ||
transforming growth factor beta receptor 1 (TGFBR1), a key stimulator of tumor proliferation and metastasis, was a direct target of miR‑98‑5p. miR‑98‑5p overexpression resulted in the downregulation of TGFBR1 and the suppression of the viability, proliferation, migration and invasion of A549 and H1299 cells. TGFBR1 Protein, Human, Recombinant (mFc & Avi), Biotinylated is expressed in HEK293 mammalian cells with C-mFc-Avi tag. The predicted molecular weight is 38.2 kDa and the accession number is P36897-1.
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