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Search Results for " fibrosarcoma "

13

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2168	2-(1,8-naphthyridin-2-yl)phenol	STAT	JAK/STAT signaling; Stem Cells
	2-NP 是选择性的STAT1转录增强剂。它能够增强 IFN-γ 的功能，提高对人乳腺癌和纤维肉瘤细胞增殖的抑制能力。
T17044	Tesaglitazar	PPAR	DNA Damage/DNA Repair; Metabolism
	Tesaglitazar 是一种有效且具有选择性的过氧化物 PPAR α / γ受体双重激动剂，对 PPARγ的亲和力比 PPARα更有效，对大鼠PPARα和人PPARα的EC50分别为13.4 μM 和3.6 μM,对大鼠PPARγ和人类 PPARγ的EC50都是0.2 μM。Tesaglitazar 诱导大鼠皮下组织间质间充质细胞DNA 合成和纤维肉瘤形成。
T36466	Chlorin E6 Ce6,Chlorin e6,CE6	Parasite	Microbiology/Virology
	Chlorin E6 (CE6) 是一种第二代光敏剂，在与辐照结合使用时具有抗肿瘤活性。在植入性纤维肉瘤的小鼠模型中，Chlorin E6（2.5-10 毫克/千克，静脉注射，50-200 焦耳/平方厘米的辐照）在不同程度的辐照后会导致肿瘤完全消失。在一项针对支气管源性早期浅表鳞状细胞癌患者的 I 期临床研究中，对包括 Chlorin E6 在内的制剂进行了测试，结果良好（40 毫克/平方米，静脉注射，100 焦耳/平方厘米的激光辐照）。在一项针对早期肺癌患者的二期临床试验中，同样的给药模式使 82.9% 的患者获得了完全应答。Chlorin E6 已被研究为一种纳米技术给药工具。
T38101	Bisucaberin
	Bisucaberin is a siderophore and bacterial metabolite that has been found inA. haloplanktisand has anticancer activity.1,2It inhibits the growth of L1210 and 1MC carcinoma cells (IC50s = 9.7 and 12.7 μM, respectively) and sensitizes fibrosarcoma 1023 cells to macrophage-mediated cytolysis. 1.Hou, Z., Raymond, K.N., O’Sullivan, B., et al.A preorganized siderophore: Thermodynamic and structural characterization of alcaligin and bisucaberin, microbial macrocyclic dihydroxamate chelating agentsInorg...
T64194	Belvarafenib TFA
	Belvarafenib TFA (HM95573 TFA) 是一种有效的、广泛的迅速加速纤维肉瘤激酶(RAF)的抑制剂，能够作用于 B-RAF (IC50: 56 nM)、B-RAFv600E (IC50: 7 nM) 和 C-RAF (IC50: 5 nM)。
T83692	EGFR Peptide (human, mouse) (myristoylated) TFA Myr-Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH,Epidermal Growth Factor Receptor Peptide,N-myristoyl-RKRTLRRL
	EGFR peptide (myristoylated) 是一种合成的肽类PKC抑制剂，其IC50值为5µM，与EGFR内部区域的氨基酸序列相对应。当浓度为1µM时，可以逆转紫外线-2237M (UV-2237M-ADRR) 成纤维细胞瘤细胞对多柔比星的抗药性。
T35613	Cytostatin (sodium salt)
	Cytostatin (sodium salt) is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin (sodium salt) potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect agai...
T36748	Heliquinomycin
	Heliquinomycin is a bacterial metabolite originally isolated fromStreptomycesthat has diverse biological activities.1It is active against a variety of Gram-positive bacteria, including strains ofB. anthracis, B. subtilis, and methicillin-sensitive or -resistantS. aureus(MICs = <0.05-0.39 μg/ml). Heliquinomycin inhibits the activity of DNA helicase with a Kivalue of 6.8 μM. It reduces the growth of L1210 leukemia, B16 melanoma, and FS-3 fibrosarcoma cells (IC50s = 0.97, 0.89, and 0.83 μg/ml, resp...
T70527	DAT-230
	DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated ...
T83780	GPX4 24 Phospholipid Hydroperoxide Glutathione Peroxidase 24,PHGPx 24,Glutathione Peroxidase 4 24
	GPX4 24是(1S,3R)-RSL3的衍生物，具有抑制谷胱甘肽过氧化物酶4（GPX4）的作用。它能够在浓度依赖的方式中与4T1小鼠乳腺癌细胞中的GPX4形成共价结合。在GPX4依赖的HT-1080成纤维细胞中，GPX4 24诱导铁死亡（EC50 = 0.16 µM）。当以200 mg/kg剂量给予小鼠时，它能够增加小鼠肾脏和血浆中丙二醛（MDA）的水平。
T36404	PRLX-93936
	PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM...
T83886	icFSP1 TFA
	icFSP1是一种抑制剂，针对的是铁死亡抑制蛋白1（FSP1）。在2.5 µM的浓度下使用时，能够引发FSP1在细胞中的凝聚和相分离，但在无细胞测试中并不抑制FSP1的酶活性（IC50 = > 30 µM）。icFSP1以浓度依赖的方式诱导HT-1080纤维肉瘤细胞的铁死亡。在体内，icFSP1（50 mg/kg）通过使用人类过表达FSP1，Gpx4-/-Fsp1-/-的B16/F10细胞，在B16/F10鼠黑色素瘤模型中减少肿瘤体积和重量。
T37861	Talabostat
	Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...

化合物

2-(1,8-naphthyridin-2-yl)phenol

Cat.No: T2168

Target: STAT

Cat.No: T17044

Target: PPAR

Cat.No: T36466

Synonym: Ce6,Chlorin e6,CE6

Target: Parasite

Cat.No: T38101

Belvarafenib TFA

Cat.No: T64194

EGFR Peptide (human, mouse) (myristoylated) TFA

Cat.No: T83692

Synonym: Myr-Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH,Epidermal Growth Factor Receptor Peptide,N-myristoyl-RKRTLRRL

Cytostatin (sodium salt)

Cat.No: T35613

Cat.No: T36748

Cat.No: T70527

Cat.No: T83780

Synonym: Phospholipid Hydroperoxide Glutathione Peroxidase 24,PHGPx 24,Glutathione Peroxidase 4 24

Cat.No: T36404

Cat.No: T83886

Cat.No: T37861

Cat. No.	Product Name	Target	Signaling Pathways
T2S2215	Crebanine	Apoptosis; Others; Akt	Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
	Crebanine 是来自于韦诺萨千金藤的一种生物碱，通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性，还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。
TN3854	Dihydroniloticin	Others	Others
	Dihydroniloticin shows cytotoxic activity against a HT-1080 human fibrosarcoma cell line( IC50 = 8.2 microM).
TN3307	9,10-Dimethoxycanthin-6-one	Others	Others
	9,10-Dimethoxycanthin-6-one shows cytotoxic activity against a HT-1080 human fibrosarcoma cell line( IC50 = 5.0 microM).
TN3571	Calyxin B	Others	Others
	Calyxin B exhibits potent activity against human HT-1080 fibrosarcoma cells with an ED50 value of 0.69 microM. A methylated product of calyxin A and an epimeric mixture of Calyxin B, showed greatly reduced activity suggesting that phenolic hydroxyl groups
TN4623	Nagilactone C	Antifection	Microbiology/Virology
	Nagilactone C and phyllanthoside are novel protein synthesis inhibitors, they are specific for the eukaryotic translation apparatus, function in vivo and in vitro, and interfere with translation elongation. Nagilactone C shows high insecticidal activity against second-instar nymphs of Eocanthecona furcellata. Nagilactone C possesses potent antiproliferative activity against human fibrosarcoma and murine colon carcinoma tumor cell lines exhibiting ED50 values of 2.3 and 1.2 microg/ml, respectivel...
TN2029	p-Hydroxy-5,6-dehydrokawain 4'-Hydroxydehydrokawain,4'-羟基-5,6-脱氢醉椒素	Others	Others
	p-Hydroxy-5,6-dehydrokawain (4'-Hydroxydehydrokawain) 是一种分离自 Kawain 的天然产物。
T37055	Cytostatin
	Cytostatin is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.

天然产物

Cat.No: T2S2215

Target: Apoptosis, Others, Akt

Dihydroniloticin

Cat.No: TN3854

Target: Others

9,10-Dimethoxycanthin-6-one

Cat.No: TN3307

Target: Others

Cat.No: TN3571

Target: Others

Cat.No: TN4623

Target: Antifection

p-Hydroxy-5,6-dehydrokawain

Cat.No: TN2029

Synonym: 4'-Hydroxydehydrokawain,4'-羟基-5,6-脱氢醉椒素

Target: Others

Cat.No: T37055

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