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Search Results for " 4t1 "

15

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T31101	CRT0273750 CRT 0273750,CRT-0273750	PDE	Metabolism
	CRT0273750 是一种 ATX 抑制剂的先导化合物，可调节血浆中 LPA 水平，用于 ATX/LPA 依赖性癌症模型。
T5208	BAY-8002 BAY8002,BAY 8002	Monocarboxylate transporter	Membrane transporter/Ion channel
	BAY-8002 是一种可口服的单羧酸转运蛋白第 1 亚型 MCT1 选择性抑制剂，在表达 MCT1 的 DLD-1 细胞中，IC50值为 85 nM，具有抗肿瘤活性。
T79395	CBP/p300-IN-21	Epigenetic Reader Domain	Chromatin/Epigenetic
	CBP/p300-IN-21 (Compound 5d) 作为一种选择性CBP/p300抑制剂，展现出对p300和CBP具有差异性的IC50值，分别为0.07 μM和1.755 μM。该化合物能有效降低H3K18Ac的水平，并抑制小鼠4T1肿瘤的生长。
T79580	Antitumor agent-115	Apoptosis	Apoptosis
	Antitumor agent-115 (SS-12)是一种在体外展现出显著抗肿瘤活性的化合物，针对小鼠乳腺癌细胞系4T1的IC50值介于0.34 μM至24.14 μM。该化合物能够阻断4T1细胞周期、降低其线粒体膜电位并诱导凋亡，其对4T1细胞抑制活性的IC50值在8-25 μmol/L之间，适用于乳腺癌研究领域。
T83078	Anticancer agent 33
	Anticanceragent 33 (compound 3) 为Squamocin与Bullatacin衍生物，展现出有效的抗癌特性。本化合物对4T1乳腺癌细胞系（包括A549、HeLa、HepG2和MCF-7细胞）的生长抑制作用显著，其IC50范围为1.9-5.4 µM。
T83889	C-02
	C-02是一种由巨噬细胞抑制剂Lonidamine和Cereblon配体Thalidomide组成的蛋白酶体靶向嵌合体（PROTAC）。在20 µM浓度下使用时，可诱导786-O和PANC-1细胞中的Hexokinase 2降解。C-02对786-O、4T1、PANC-1、HGC-27和MCF-7癌细胞具有细胞毒性（IC50分别为34.07、5.08、31.53、6.11和21.65 µM）。同时，20 µM浓度下减少4T1细胞的细胞外酸化率（ECAR）和氧气消耗率（OCR），表明其抑制糖酵解和引起线粒体损伤。在体内，C-02（50 mg/kg）能减少4T1小鼠乳腺癌模型的肿瘤体积，并诱导肿瘤内细胞因子积累和细胞焦亡。
T71293	Nifuroxazide-d4
	Nifuroxazide-d4 is intended for use as an internal standard for the quantification of nifuroxazide by GC- or LC-MS. Nifuroxazide is a nitrofuran antibiotic. It is active against strains of the enteropathogenic bacteria C. jejuni, Salmonella, Y. enterocolitica, Shigella, and E. coli. It inhibits quorum sensing and virulence factor production in P. aeruginosa. Nifuroxazide inhibits STAT3 activity in a reporter assay and decreases viability of U266 and INA-6 myeloma cells, which have constitutive S...
T79723	PDK-IN-2
	PDK-IN-2（Compound 1F）是一种具有IC50为68 nM的PDK抑制剂。该化合物能够抑制PDK1和PDK4在细胞内的表达，增强线粒体生物能并降低糖酵解表型，同时诱导细胞走向线粒体途径的apoptosis。此外，PDK-IN-2在4T1同基因小鼠模型中能够有效抑制肿瘤生长。
T82758	CDK9-Cyclin T1 PPI-IN-1	CDK	Cell Cycle/Checkpoint
	CDK9-Cyclin T1 PPI-IN-1 (Compound B19) 是CDK9-Cyclin T1蛋白-蛋白相互作用的选择性抑制剂。该化合物能够有效抑制TNBC MDA-MB-231细胞系的细胞增殖(IC50: 0.044 μM)，诱导细胞凋亡，同时降低CDK9的转录活性并减少RNA Pol II CTD ser2的磷酸化，有效地抑制了4T1移植瘤模型小鼠中肿瘤的生长。
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。
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...
T35616	Migrastatin
	Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mam...
T83871	Ferroptocide
	Ferroptocide是一种抑制剂，可抑制硫氧还蛋白(Trx)活性，并且是pleuromutilin的衍生物。在20 µM的浓度下，Ferroptocide能够抑制ES-2卵巢癌细胞中的Trx活性，并对ES-2细胞具有细胞毒性(IC50 = 1.6 µM)。5 µM的Ferroptocide能够诱导ES-2细胞发生铁死亡，这一效应可以通过铁螯合剂去铁胺(DFO)、抗氧化剂Trolox或铁死亡抑制剂ferrostatin-1来阻断。在使用免疫完整但非免疫缺陷小鼠的4T1小鼠乳腺癌模型中，每周两次以50 mg/kg剂量给药时，Ferroptocide能够减少肿瘤体积。
T79714	HDAC3-IN-2	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	HDAC3-IN-2 (compound 4i) 是一种具有纳摩尔级效力的吡嗪酰肼基HDAC3抑制剂，IC50值为14 nM，针对三阴性乳腺癌细胞表现出高效抑制作用。该化合物在细胞内毒性测定中显示，对4T1细胞株的IC50为0.55 μM，对MDA-MB-231细胞株的IC50为0.74 μM。HDAC3-IN-2通过增加乙酰化水平（如H3K9、H3K27和H4K12），促进细胞凋亡（涉及caspase-3、caspase-7和细胞色素c的水平提升），并抑制细胞增殖相关蛋白（如Bcl-2、CD44、EGFR和Ki-67）的表达，从而在荷瘤小鼠模型中表现出显著的体内抗肿瘤作用。
T35672	SMU127
	SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer.1It induces NF-κB signaling in cells expressing human TLR2 (EC50= 0.55 μM) but not cells expressing human TLR3, -4, -5, -7, or -8 when used at concentrations ranging from 0.1 to 100 μM. SMU127 induces the production of TNF-α in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 0.01 to 1 μM.In vivo, SMU127 (0.1 mg/animal) reduces tumor volume in a 4T1 murine mammary carcinoma m...

化合物

Cat.No: T31101

Synonym: CRT 0273750,CRT-0273750

Target: PDE

Cat.No: T5208

Synonym: BAY8002,BAY 8002

Target: Monocarboxylate transporter

Cat.No: T79395

Target: Epigenetic Reader Domain

Antitumor agent-115

Cat.No: T79580

Target: Apoptosis

Anticancer agent 33

Cat.No: T83078

Cat.No: T83889

Nifuroxazide-d4

Cat.No: T71293

Cat.No: T79723

CDK9-Cyclin T1 PPI-IN-1

Cat.No: T82758

Target: CDK

Cat.No: T83780

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

3,5-dimethyl PIT-1

Cat.No: T35491

Cat.No: T35616

Cat.No: T83871

Cat.No: T79714

Target: HDAC

Cat.No: T35672

Cat. No.	Product Name	Target	Signaling Pathways
TN4801	Piscidinol A	Others	Others
	Piscidinol A is toxic against the 4T1 and HEp2 cancer cell lines, the IC50 of 8.0 ± 0.03 and 8.4 ± 0.01 uM, respectively. It can inhibit NO production in mouse peritoneal macrophages with inhibitory ratios ranging from 39.8±7.7 to 68.2±4.5%.
TN4263	Isoangustone A	MMP; GSK-3; NF-κB; ROS; Akt; PI3K; CDK; JNK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
	Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Isoangustone A dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-ÎºB signaling. Isoangustone A also shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.

天然产物

Cat.No: TN4801

Target: Others

Cat.No: TN4263

Target: MMP, GSK-3, NF-κB, ROS, Akt, PI3K, CDK, JNK

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