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Search Results for " epithelial-mesenchymal "

27

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21981	Phthalazinone pyrazole	Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	Phthalazinone pyrazole 是强效、选择性和口服生物可利用的 Aurora-A 激酶抑制剂，IC50值为 0.031 μM。它抑制人胚胎干细胞向肝细胞样细胞分化过程中的上皮间质转化。它还可阻止有丝分裂并随后通过增殖细胞的凋亡抑制肿瘤生长。
T0459	Sulindac Arthrocine,MK-231,舒林酸,Clinoril,Sulindac sulfoxide	COX; Autophagy	Autophagy; Immunology/Inflammation; Neuroscience
	Sulindac (Sulindac sulfoxide) 是一种非甾体类抗炎剂，可抑制COX-2的活性，也可抑制 COX-2 的过表达。它是一种亚磺酰基茚衍生物前药，具有潜在的抗肿瘤活性。
T1725	Y-27632 dihydrochloride 反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐,Y-27632 2HCl	ROCK; Apoptosis	Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	Y-27632 dihydrochloride (Y-27632 2HCl) 是一种 ROCK-I 和 ROCK-II 抑制剂，具有口服有效性、ATP 竞争性。Y-27632 dihydrochloride 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡。
T4252	ML327	c-Myc; Autophagy	Autophagy; Cell Cycle/Checkpoint
	ML327 是 MYC 的阻断剂，还可抑制 E-钙粘蛋白转录和逆转上皮间质转化。
T9601	Tepotinib hydrochloride(1 : x)	c-Met/HGFR; P-gp; ABC	Membrane transporter/Ion channel; Neuroscience; Tyrosine Kinase/Adaptors
	Tepotinib hydrochloride(1 : x) 是一种口服生物可利用的间充质-上皮转化 (MET) TKI，主要针对具有 METex14 跳跃突变的特定 NSCLC 患者开发。
T38752	EW-7195	ALK; TGF-beta/Smad	Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
	EW-7195 是一种具有选择性和高效性的 ALK5 (TGFβR1) 抑制剂，IC50 值为 4.83 nM。EW-7195 对 ALK5 的亲和力是 p38α 的 300 多倍。EW-7195 对 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移有抑制作用。
T73300	AXL-IN-13	FLT; TAM Receptor; PDGFR; TGF-beta/Smad	Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
	AXL-IN-13 是一种有效且具有口服活性的 AXL 抑制剂，其IC50值为 1.6 nM，Kd 值为0.26 nM。AXL-IN-13 具有抗癌活性，可逆转 TGF-β1 诱导的上皮间质转化 (EMT)，并抑制癌细胞迁移和侵袭。
T11793	KY-05009	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	KY-05009 是 ATP 竞争性的、有效的 TNIK 抑制剂，Ki 为 100 nM。KY-05009抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制TNIK 的蛋白表达和Wnt 靶基因的转录活性，并诱导癌细胞凋亡，显示抗癌活性。
T77701	FL118 FL 118,FL-118,10,11-(Methylenedioxy)-20(S)-camptothecin	Survivin	Apoptosis
	FL118是一种新型存活素抑制剂，可抑制癌症干细胞样特性。FL118 是一种新型喜树碱类似物，具有抗癌活性，通过 Wnt/β-catenin 信号通路抑制上皮-间充质转化，从而抑制人乳腺癌细胞的迁移和侵袭。
T36696	DMBA
	7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase...
T11187	EMT inhibitor-2	Others	Others
	EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively. EMT inhibitor-2 inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes.
T79789	DT-6	TGF-beta/Smad	Stem Cells
	DT-6为一有效TGF-β1抑制剂，能够抑制M2巨噬细胞诱导的上皮至间质转化(Epithelial-Mesenchymal Transition, EMT)及癌细胞侵袭性迁移，可用于癌症相关疾病研究。
T76994	Sotevtamab
	Sotevtamab (16B5) 是一种抗clusterin 单克隆抗体 (mAb)。Sotevtamab 是上皮间充质转化的抑制剂。Sotevtamab 可用于癌症研究。
T72880	PI3K/AKT-IN-2
	PI3K/AKT-IN-2 是一种 PI3K 和 AKT 抑制剂。PI3K/AKT-IN-2 阻断上皮-间质转化 (EMT)，诱导细胞凋亡 (apoptosis)。PI3K/AKT-IN-2 抑制微管蛋白 (tubulin) 的聚合。
T83075	Anticancer agent 94
	Anticanceragent 94, 一种4-羟基香豆素衍生物，能抑制肺癌细胞的侵袭和迁移，其机制为调节(EMT)效应子表达。
T83076	Anticancer agent 93
	Anticanceragent 93, 一种4-羟基香豆素衍生物，能够抑制肺癌细胞的侵袭与迁移，其机制为调节上皮间质转化（EMT）效应子的表达。
T82673	CPF-7 Caerulein precursor fragment
	CPF-7（Caerulein precursor fragment）是一种促进胰岛素释放的肽，可以通过增加PANC-1导管细胞中Snai1表达来引导上皮-间质转换（EMT），并且CPF-7还能通过提高Ngn3表达以诱导外分泌细胞可塑性。此外，CPF-7适用于2型糖尿病的相关研究。
T73035	STAT3-IN-15
	STAT3-IN-15是一款有效、具口服活性的STAT3抑制剂，用于对抗特发性肺纤维化（IPF）。该化合物阻止STAT3磷酸化，同时抑制TGF-β1引起的上皮细胞迁移及变形，并防止上皮间质转化（EMT）。
T73547	CPUL1
	CPUL1 是一种TrxR 抑制剂，对 A549 细胞显示出增殖抑制和抗转移活性。CPUL1 通过抑制TrxR1酶活性来诱导 ROS 介导的ERK/JNK 信号传导从而影响上皮-间质转化 (EMT)。CPUL1 与α-Lipoic Acid 或Dithiodipropionic acid 联合使用效果更好。
T61852	hCAIX-IN-8
	hCAIX-IN-8 (compound 7i) is a highly potent and selective inhibitor of hCAIX, demonstrating potent inhibitory activity against CAIX with an IC50 value of 0.024 μM. It also exhibits inhibitory activity against CAII and CAVA with IC50 values of 1.99 μM and 1.10 μM, respectively. Furthermore, hCAIX-IN-8 exhibits anti-proliferative effects and low toxicity. It effectively reduces the occurrence of epithelial-to-mesenchymal transitions and promotes apoptosis. Additionally, hCAIX-IN-8 effectively inhi...
T71884	ß-Carboline-1-carboxylic acid
	β-Carboline-1-carboxylic acid is an alkaloid that has been found in P. quassioides and has diverse biological activities. It reduces LPS-induced increases in MCP-1, TNF-α, IL-6, and IL-1β levels in RAW 264.7 cells when used at a concentration of 15 µg/ml and inhibits the epithelial-to-mesenchymal transition (EMT) induced by TGF-β1 in A549 cells. β-Carboline-1-carboxylic acid induces cytotoxicity in CT26.WT, K562, and SGC-7901 cells (IC50s = 14.96, 22.11, and 19.7 µg/ml, respectively) but not Hep...
T62814	Antitumor agent-77
	Antitumor agent-77 对癌细胞的生长和迁移具有抑制作用，具有抗癌作用。Antitumor agent-77 能够抑制 GPx-4 和提高 COX2 引发铁下垂。Antitumor agent-77 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，阻碍肿瘤细胞上皮间质转化 (EMT) 过程。
T36460	CAY10736 CAY10736
	CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a ...
T63768	Antitumor agent-78
	Antitumor agent-78 能够抑制 GPx-4 和升高 COX2 ，进而导致铁下垂 (ferroptosis)。Antitumor agent-78 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，抑制肿瘤细胞上皮间质转化 (EMT) 过程。Antitumor agent-78 表现出抗肿瘤效果，并能够抑制癌细胞的生长和迁移。
T62822	CT1-3
	CT1-3 是一种有效的抗癌剂。CT1-3 能够调控 JNK/Bcl-2/Bax/XIAP 通路，进而诱导线粒体介导的细胞凋亡 (apoptosis)。CT1-3 可以调控 E-cadherin/Snail 轴抑制人癌细胞 (HCCs) 的上皮间充质转化 (EMT) 电位，并抑制肿瘤发生。CT1-3 在小鼠模型中具有抗肿瘤作用，且没有表现出明显的肝、肾毒性。
T36497	CAY10735 CAY10735
	CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells ...
T61585	Sulindac sodium
	Sulindac (sodium) (MK-231) 是一种非甾体抗炎剂，具有口服活性。Sulindac (sodium) 用于减轻疼痛，肿胀和关节僵硬的关节炎。Sulindac 还用于脊柱关节炎、痛风性关节炎的研究。Sulindac (sodium) 作为一种免疫调节剂，可通过阻断 NF-κB 信号通路下调 PD-L1，调节 pMMR CRC 对抗 PD-L1 免疫治疗的应答，抑制结直肠癌 CRC 的发生发展。 Sulindac 还可通过下调 SIRT1 抑制 TGF-β1-诱导的 EMT，抑制肺癌细胞的迁移和侵袭。

化合物

Phthalazinone pyrazole

Cat.No: T21981

Target: Aurora Kinase

Cat.No: T0459

Synonym: Arthrocine,MK-231,舒林酸,Clinoril,Sulindac sulfoxide

Target: COX, Autophagy

Y-27632 dihydrochloride

Cat.No: T1725

Synonym: 反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐,Y-27632 2HCl

Target: ROCK, Apoptosis

Cat.No: T4252

Target: c-Myc, Autophagy

Tepotinib hydrochloride(1 : x)

Cat.No: T9601

Target: c-Met/HGFR, P-gp, ABC

Cat.No: T38752

Target: ALK, TGF-beta/Smad

Cat.No: T73300

Target: FLT, TAM Receptor, PDGFR, TGF-beta/Smad

Cat.No: T11793

Target: Wnt/beta-catenin

Cat.No: T77701

Synonym: FL 118,FL-118,10,11-(Methylenedioxy)-20(S)-camptothecin

Target: Survivin

Cat.No: T36696

EMT inhibitor-2

Cat.No: T11187

Target: Others

Cat.No: T79789

Target: TGF-beta/Smad

Cat.No: T76994

Cat.No: T72880

Anticancer agent 94

Cat.No: T83075

Anticancer agent 93

Cat.No: T83076

Cat.No: T82673

Synonym: Caerulein precursor fragment

Cat.No: T73035

Cat.No: T73547

Cat.No: T61852

ß-Carboline-1-carboxylic acid

Cat.No: T71884

Antitumor agent-77

Cat.No: T62814

Cat.No: T36460

Synonym: CAY10736

Antitumor agent-78

Cat.No: T63768

Cat.No: T62822

Cat.No: T36497

Synonym: CAY10735

Sulindac sodium

Cat.No: T61585

Cat. No.	Product Name	Target	Signaling Pathways
T3862	Irigenin	NF-κB; Integrin	Cytoskeletal Signaling; NF-κB
	Irigenin 可通过特异性和选择性地阻断 Extra Domain A 域的 C-C 环上α9β1和α4β1整合素结合位点，介导其抗转移作用。可通过增强胃癌细胞中促凋亡分子的表达来敏化 TRAIL 诱导的凋亡，具有抗癌作用。
T0518	Methacycline hydrochloride Rondomycin,盐酸甲烯土霉素,盐酸美他环素,Methacycline HCl	ribosome; Antibacterial; Antibiotic	Microbiology/Virology
	Methacycline hydrochloride (Rondomycin) 是四环素抗生素，可抑制细菌蛋白质的合成。它是上皮-间质转化 (EMT) 抑制剂。它在体外可阻断 EMT，体内抑制纤维发生，不会直接影响 TGF-β1 Smad 信号传导。它是抗菌剂，有潜力研究肺纤维化。
TN1198	19-Hydroxybufalin	Others	Others
	19-Hydroxybufalin 是蟾二烯羟酸内酯，能够阻碍上皮间质转化，抑制 PC3 细胞的迁移和侵袭。
T2S0690	Ecliptasaponin A 早莲苷 A,旱莲苷A,Echinocystic acid-3-o-glucoside	Others	Others
	Ecliptasaponin A (Echinocystic acid-3-o-glucoside) 是一种墨旱莲 (Eclipta prostrate) 中分离得到的五环三萜皂苷。其中墨旱莲是一种具有多效作用的滋补草药，如抗炎、保肝、抗氧化和免疫调节。
T3330	trans-Trimethoxyresveratrol trans-trismethoxy Resveratrol,E-Resveratrol Trimethyl Ether,MR-3,Tri-O-methylresveratrol,白藜芦醇三甲醚,3,4',5-Trimethoxy-trans-stilbene,Trimethoxystilbene	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	trans-Trimethoxyresveratrol (MR-3) 是一种 Resveratrol(RSV) 的衍生物，与Resveratrol(RSV)相比，它可能是一个更有效的抗炎、抗血管新生的化合物。
T7982	3,6-Dihydroxyflavone	Others	Others
	3,6-Dihydroxyflavone 是一种抗癌剂。它能够提高细胞内氧化应激和脂质过氧化。它是能够根据剂量和时间依赖性地降低细胞活力，并活化半胱天冬酶级联、切割聚 (ADP-核糖) 聚合酶 (PARP) 诱导细胞凋亡。
T4S1383	Escin IA Aescin IA,Escin IA;Aescin IA,Escin IA	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Escin IA (Escin IA;Aescin IA);Aescin IA 是从马蹄中七叶树分离出的一种三萜皂苷，抑制HIV-1蛋白酶，IC50值为 35 μM。它具有抗 TNBC 转移活性，其作用机制涉及通过下调 LOXL2 表达抑制上皮-间质转化过程。
TN1433	Batatasin III	FAK; Others; Akt	Angiogenesis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	Batatasin III 通过抑制上皮间质转化和 FAK-AKT 信号来抑制癌症迁移和侵袭，并具有抗癌活性。 Batatasin III 对整株生长有长期抑制作用，显示出抑制萌发活性。
T6S1315	Oroxylin A 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether	Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy	Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

天然产物

Cat.No: T3862

Target: NF-κB, Integrin

Methacycline hydrochloride

Cat.No: T0518

Synonym: Rondomycin,盐酸甲烯土霉素,盐酸美他环素,Methacycline HCl

Target: ribosome, Antibacterial, Antibiotic

19-Hydroxybufalin

Cat.No: TN1198

Target: Others

Ecliptasaponin A

Cat.No: T2S0690

Synonym: 早莲苷 A,旱莲苷A,Echinocystic acid-3-o-glucoside

Target: Others

trans-Trimethoxyresveratrol

Cat.No: T3330

Synonym: trans-trismethoxy Resveratrol,E-Resveratrol Trimethyl Ether,MR-3,Tri-O-methylresveratrol,白藜芦醇三甲醚,3,4',5-Trimethoxy-trans-stilbene,Trimethoxystilbene

Target: Reactive Oxygen Species

3,6-Dihydroxyflavone

Cat.No: T7982

Target: Others

Cat.No: T4S1383

Synonym: Aescin IA,Escin IA;Aescin IA,Escin IA

Target: HIV Protease

Cat.No: TN1433

Target: FAK, Others, Akt

Cat.No: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

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