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Search Results for " u87mg "

13

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6303L	CCT128930 hydrochloride CCT128930 hydrochloride(885499-61-6 Free base)	Apoptosis; Akt; PKA; mTOR; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	CCT128930 hydrochloride (CCT128930 hydrochloride) 是一种选择性 AKT 抑制剂，具有抗肿瘤活性。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173)，对 PKA 激酶具有 28 倍的选择性，对 p70S6K 具有 20 倍的选择性。
T6303	CCT128930	Akt; PKA; S6 Kinase; Autophagy	Autophagy; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	CCT128930 是一种 ATP 竞争性，选择性 AKT 抑制剂。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173)，对 PKA 激酶具有 28 倍的选择性，对 p70S6K 具有 20 倍的选择性，具有抗肿瘤活性。
T72726	3-epi-Vitamin D3 Epicholecalciferol
	3-epi-Vitamin D3 (Epicholecalciferol) 是维生素 D3 类似物，是一种Hedgehogpathway 抑制剂，在U87MG 细胞中测定的IC50为 39.2 μM。
T83513	(αR)-Cyclopropaneacetamide-Exatecan
	(αR)-Cyclopropaneacetamide-Exatecan (化合物2-A)作为一种Exenotecan衍生物，具有细胞毒性。该化合物在抑制U87MG和SK-BR-3细胞株的增殖方面表现出显著效力，其IC50值分别为8.11 μM和2.31 μM。
T83898	S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine SFN-Cys,D,L-Sulforaphane-L-cysteine
	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。
T41151	K34c
	K34c is a potent and selective α5β1 integrin inhibitor (IC50 = 3.1 nM). K34c inhibits cell survival and migration, inhibits p53-dependent senescence induced by Temozolomide or Ellipticine and promotes apoptosis in U87MG cells. K34c also prevents TGFβ-induced infiltrationin vivoand reduces cell adhesion on fibronectin.
T63957	PI3K-IN-29
	PI3K-IN-29 是一种有效的 PI3K 抑制剂。PI3K-IN-29 对 U87MG、HeLa 和 HL60 细胞具有较好的抑制作用，IC50值分别为 0.264、2.04 和 1.14 µM。PI3K-IN-29 通过抑制PI3K 催化的Akt 的磷酸化来抑制PI3K/Akt 通路。
T70890	ML309
	ML309 is a potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. ML309 is capable of potent and selective inhibition of mutant IDH1 and effectively lowers cell-based production of 2-HG in a U87MG mutant glioblastoma cell line.
T36035	CAY10784
	CAY10784 is a STAT3 inhibitor (IC50= 0.74 μM in a reporter assay) and a derivative of WP1066 .1It inhibits proliferation of HeLa, Caco-2, A549, A375, U87MG, and HL-60 cancer cells (IC50s = 1.8, 1.8, 3, 2.8, 2.3, and 1.2 μM, respectively) but not PC3 or HT-29 cancer cells (IC50s = >10 μM for both). CAY10784 is also active againstH. pyloriandC. jejuni(MICs = 1.6 and 4.7 μM, respectively).2 1.Lü, Z., Li, X., Li, K., et al.Structure-activity study of nitazoxanide derivatives as novel STAT3 pathway i...
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T83911	CYY292
	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。
T83777	LAU-0901
	LAU-0901是一种血小板活化因子(PAF)受体拮抗剂。在体内，LAU-0901（30、60及90 mg/kg）通过减少梗塞体积和改善大鼠由中脑动脉阻塞(MCAO)引起的脑缺血模型中的神经功能来发挥作用。它还能减少同一模型中的小胶质细胞浸润，并增加星形胶质细胞和神经元的存活率。单独使用LAU-0901（30 mg/kg）或与阿托伐他汀联合使用，能减少U87MG胶质母细胞瘤小鼠原位肿瘤模型中的肿瘤生长。
T35491	3,5-dimethyl PIT-1
	PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorab...

化合物

CCT128930 hydrochloride

Cat.No: T6303L

Synonym: CCT128930 hydrochloride(885499-61-6 Free base)

Target: Apoptosis, Akt, PKA, mTOR, Autophagy

Cat.No: T6303

Target: Akt, PKA, S6 Kinase, Autophagy

3-epi-Vitamin D3

Cat.No: T72726

Synonym: Epicholecalciferol

(αR)-Cyclopropaneacetamide-Exatecan

Cat.No: T83513

S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine

Cat.No: T83898

Synonym: SFN-Cys,D,L-Sulforaphane-L-cysteine

Cat.No: T41151

Cat.No: T63957

Cat.No: T70890

Cat.No: T36035

Reduced Haloperidol

Cat.No: T37167

Cat.No: T83911

Cat.No: T83777

3,5-dimethyl PIT-1

Cat.No: T35491

Cat. No.	Product Name	Target	Signaling Pathways
T21523	β-Tocotrienol Beta-Tocotrienol	Caspase	Apoptosis; Proteases/Proteasome
	Beta-Tocotrienol to serve as a new anticancer agent for treating human lung and brain cancers. It inhibits the growth of both A549 (GI50=1.38±0.334μM) and U87MG (GI50=2.53±0.604μM) cells at rather low concentrations.
T36430	Pheophorbide a
	Pheophorbide a is a product of chlorophyll breakdown that has been used as a photosensitizer in photodynamic therapy for the treatment of cancer. It has been reported to inhibit U87MG cells with an IC50 value of 2.8 μg/ml and demonstrates cytostatic activity specifically against glioblastoma cells without affecting normal cells. It also displays antiproliferative activity against melanoma, breast, and lung cancer cells in vitro at 100 μg/ml.

天然产物

Cat.No: T21523

Synonym: Beta-Tocotrienol

Target: Caspase

Cat.No: T36430

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