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Search Results for " epithelial-mesenchymal transition (emt) "
Targets Recommended: Aurora Kinase

21

抑制剂 & 化合物

1

天然产物

9

重组蛋白

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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。
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。
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。
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.
T72880 PI3K/AKT-IN-2

Others Others
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

Others Others
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

Others Others
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。
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。
T73035 STAT3-IN-15

Others Others
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

Others Others
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。
T63768 Antitumor agent-78

Others Others
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。
T62814 Antitumor agent-77

Others Others
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。
T71884 ß-Carboline-1-carboxylic acid

Others Others
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...
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。
T62822 CT1-3

Others Others
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

Others Others
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 ...
T36460 CAY10736

CAY10736

Others Others
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 ...
T61585 Sulindac sodium

Others Others
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
Synonym:
Target: Aurora Kinase
Sulindac
Cat.No: T0459
Synonym: Arthrocine,MK-231,舒林酸,Clinoril,Sulindac sulfoxide
Target: COX, Autophagy
ML327
Cat.No: T4252
Synonym:
Target: c-Myc, Autophagy
EW-7195
Cat.No: T38752
Synonym:
Target: ALK, TGF-beta/Smad
AXL-IN-13
Cat.No: T73300
Synonym:
Target: FLT, TAM Receptor, PDGFR, TGF-beta/Smad
KY-05009
Cat.No: T11793
Synonym:
Target: Wnt/beta-catenin
EMT inhibitor-2
Cat.No: T11187
Synonym:
Target: Others
PI3K/AKT-IN-2
Cat.No: T72880
Synonym:
Target: Others
Anticancer agent 94
Cat.No: T83075
Synonym:
Target: Others
Anticancer agent 93
Cat.No: T83076
Synonym:
Target: Others
DT-6
Cat.No: T79789
Synonym:
Target: TGF-beta/Smad
STAT3-IN-15
Cat.No: T73035
Synonym:
Target: Others
CPUL1
Cat.No: T73547
Synonym:
Target: Others
Antitumor agent-78
Cat.No: T63768
Synonym:
Target: Others
Antitumor agent-77
Cat.No: T62814
Synonym:
Target: Others
ß-Carboline-1-carboxylic acid
Cat.No: T71884
Synonym:
Target: Others
CPF-7
Cat.No: T82673
Synonym: Caerulein precursor fragment
Target:
CT1-3
Cat.No: T62822
Synonym:
Target: Others
CAY10735
Cat.No: T36497
Synonym: CAY10735
Target: Others
CAY10736
Cat.No: T36460
Synonym: CAY10736
Target: Others
Sulindac sodium
Cat.No: T61585
Synonym:
Target: Others
Cat. No. Product Name Target Signaling Pathways
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。

天然产物

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
Cat. No. Product Name Species Expression System
TMPY-00322 DEC-205 Protein, Human, Recombinant (His)

GP200-MR6,CD205,CLEC13B,lymphocyte antigen 75,LY-75,DEC-205

Human HEK293 Cells
LY75 (Lymphocyte Antigen 75) is a Protein Coding gene. It is broadly expressed in the lymph node, appendix, and other tissues. LY75 knockdown in SKOV3 cells resulted in predominant upregulation of functional pathways implicated in cell proliferation and metabolism, while pathways associated with cell signaling and adhesion, complement activation, and immune response were mostly suppressed. Moreover, LY75 suppression had an opposite effect on EOC cell lines with the epithelial phenotype (A2780s a...
TMPH-03764 YAP1 Protein, Human, Recombinant (His)

YAP1-2gamma,YAP2L,YAP65

Human P. pastoris (Yeast)
Transcriptional regulator which can act both as a coactivator and a corepressor and is the critical downstream regulatory target in the Hippo signaling pathway that plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1,...
TMPY-01000 BVES Protein, Human, Recombinant (GST)

CARICK,LGMD2X,POP1,blood vessel epicardial substance,POPDC1,...

Human E. coli
Blood vessel epicardial substance (BVES), or POPDC1, is a tight junction-associated transmembrane protein that modulates epithelial-to-mesenchymal transition (EMT) via junctional signaling pathways. BVES plays a protective role both in ulcerative and infectious colitis and identify BVES as a critical protector of colonic mucosal integrity. The Popeye domain containing1, also called Bves (Popdc1/Bves), is a transmembrane protein that functions in muscle regeneration, heart rate regulation, hypoxi...
TMPH-02226 TEAD3 Protein, Human, Recombinant (His & SUMO)

DTEF-1,TEA domain family member 3,Transcriptional enhancer f...

Human E. coli
Transcription factor which plays a key role in the Hippo signaling pathway, a pathway involved in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein MST1/MST2, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Acts by mediating gene expr...
TMPY-04203 RAB1B Protein, Human, Recombinant (hFc)

RAB1B, member RAS oncogene family

Human HEK293 Cells
RAB1B, a member of the RAS oncogene family, was significantly down-regulated in highly metastatic breast cancer cells. Moreover, down-regulation of RAB1B was also found to promote the proliferation and migration of TNBC cells in vitro and in vivo. Mechanistically, loss of RAB1B resulted in elevated expression of TGF-beta receptor 1 (TbetaR1) through decreased degradation of ubiquitin, increased levels of phosphorylated SMAD3 and TGF-beta-induced epithelial-mesenchymal transition (EMT). Furthermo...
TMPH-02225 TEAD2 Protein, Human, Recombinant (His & Myc)

TEA domain family member 2,Transcriptional enhancer factor T...

Human E. coli
Transcription factor which plays a key role in the Hippo signaling pathway, a pathway involved in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein MST1/MST2, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Acts by mediating gene expr...
TMPH-02222 TEAD1 Protein, Human, Recombinant (His)

TEAD1,Transcriptional enhancer factor TEF-1,Transcription fa...

Human E. coli
Transcription factor which plays a key role in the Hippo signaling pathway, a pathway involved in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein MST1/MST2, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Acts by mediating gene expr...
TMPY-01576 Artemin Protein, Mouse, Recombinant (hFc)

artemin,neublastin

Mouse HEK293 Cells
Artemin (ARTN) is a member of glial cell line-derived neurotrophic factor (GDNF) family of ligands, and its signaling is mediated via a multi-component receptor complex including the glycosylphosphatidylinositol-anchored GDNF family receptors a (GFRa1, GFRa3) and RET receptor tyrosine kinase. The major mechanism of ARTN action is via binding to a non-signaling co-receptor. The major function of ARTN is to drive the molecule to induce migration and axonal projection from sympathetic neurons. It a...
TMPH-02217 SMARCA4 Protein, Human, Recombinant (His)

Transcription activator BRG1,Protein brahma homolog 1,SWI/SN...

Human P. pastoris (Yeast)
Involved in transcriptional activation and repression of select genes by chromatin remodeling (alteration of DNA-nucleosome topology). Component of SWI/SNF chromatin remodeling complexes that carry out key enzymatic activities, changing chromatin structure by altering DNA-histone contacts within a nucleosome in an ATP-dependent manner. Component of the CREST-BRG1 complex, a multiprotein complex that regulates promoter activation by orchestrating the calcium-dependent release of a repressor compl...

重组蛋白

DEC-205 Protein, Human, Recombinant (His)
Cat.No: TMPY-00322
Species: Human
Expression System: HEK293 Cells
YAP1 Protein, Human, Recombinant (His)
Cat.No: TMPH-03764
Species: Human
Expression System: P. pastoris (Yeast)
BVES Protein, Human, Recombinant (GST)
Cat.No: TMPY-01000
Species: Human
Expression System: E. coli
TEAD3 Protein, Human, Recombinant (His & SUMO)
Cat.No: TMPH-02226
Species: Human
Expression System: E. coli
RAB1B Protein, Human, Recombinant (hFc)
Cat.No: TMPY-04203
Species: Human
Expression System: HEK293 Cells
TEAD2 Protein, Human, Recombinant (His & Myc)
Cat.No: TMPH-02225
Species: Human
Expression System: E. coli
TEAD1 Protein, Human, Recombinant (His)
Cat.No: TMPH-02222
Species: Human
Expression System: E. coli
Artemin Protein, Mouse, Recombinant (hFc)
Cat.No: TMPY-01576
Species: Mouse
Expression System: HEK293 Cells
SMARCA4 Protein, Human, Recombinant (His)
Cat.No: TMPH-02217
Species: Human
Expression System: P. pastoris (Yeast)
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