目录号 | 产品详情 | 靶点 | |
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T3112 | Apoptosis YAP VDA Autophagy | ||
Verteporfin (BPD-MA) 是一种 YAP 抑制,抑制 YAP-TEAD 相互作用。Verteporfin 也是一种光敏剂,用于光动力疗法。Verteporfin 还可以诱导细胞凋亡,抑制自噬。 | |||
T72888 | YAP | ||
YAP-TEAD-IN-2 (化合物6)作为一种YAP-TEAD PPI抑制剂,表现出高效性,其半抑制浓度(IC50)仅为2.7 nM。 | |||
T77725 | YAP | ||
YAP-TEAD-IN-3 是 YAP/TAZ-TEAD 相互作用的抑制剂,对于 Avi-人 TEAD4217-434 的 IC50 为 9 nM。 YAP-TEAD-IN-3 抑制 YAP 报告基因表达 (IC50 = 0.048 μM) 和 NCI-H2052 细胞增殖 (IC50 = 0.048 μM)。 | |||
T1477 | Mitophagy YAP AMPK Autophagy | ||
AICAR (NSC105823) 是一种腺苷类似物,是一种 AMP 激活的蛋白激酶激活剂,可用于治疗急性淋巴细胞白血病和糖尿病。 | |||
T2008 | Apoptosis DNA-PK Casein Kinase PI3K Autophagy | ||
LY294002 (SF 1101) 是一种 PI3K 的广谱抑制剂,抑制 PI3Kα、PI3Kδ 和 PI3Kβ (IC50=0.5/0.57/0.97 μM)。LY294002 也是 DNA-PK 抑制剂 (IC50=1.4 μM) 和 CK2 抑制剂 (IC50=98 nM)。LY294002 可以激活凋亡和自噬。 | |||
T77729 | Apoptosis YAP | ||
MY-1076 是一种高效的 YAP 抑制剂,具有抗胃癌活性。MY-1076 剂量依赖性诱导G2/M期阻滞,诱导 YAP 降解和细胞凋亡,抑制微管蛋白聚合。MY-1076 抑制 MGC-803、SGC-7901、HCT-116 和 KYSE450 细胞增殖。 | |||
T9566 | Annexin A YAP | ||
PY-60 有效激活针对膜联蛋白 A2 (Kd = 1.4 µM) 的 YAP 转录活性。 PY-60 在能够通过增殖重塑表皮的成年动物中激活促增殖、依赖于 YAP 的转录程序。 | |||
T67872 | YAP | ||
VT104是一种有效的YAP/TAZ 抑制剂,具有口服活性,可用于癌症研究。VT104阻止内源性TEAD1和TEAD3蛋白棕榈酰化。 | |||
T62077 | YAP | ||
VT103 是一种具有口服活性和选择性的 TEAD1 蛋白棕榈酰化抑制剂,是 VT101 的类似物。 VT103 有潜在的抗肿瘤活性,可抑制 YAP/TAZ-TEAD 促进的基因转录,阻断 TEAD auto-palmitoylation,阻断 YAP/TAZ和TEAD 之间的相互作用。VT103 可用于研究HER2阳性乳腺癌、前列腺癌和三阴性乳腺癌。 | |||
T14149 | Mitophagy NOS YAP AMPK | ||
AICAR phosphate (Acadesine phosphate) 是 AMPK 激活剂且是自噬、YAP 和 mitophagy 抑制剂,也是一种腺苷类似物, 可调节糖代谢和脂代谢,抑制促炎细胞因子和 iNOS 的产生。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-00005 | YAP1 Protein, Human, Recombinant (Isoform 9, His) | Human | Yeast | ||
YAP1 Protein, Human, Recombinant (Isoform 9, His) is expressed in Yeast with C-terminal 6xHis tag. The predicted molecular weight is 56.4 kDa. Accession number: P46937-9
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TMPH-03764 | YAP1 Protein, Human, Recombinant (His) | Human | 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, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Plays a key role in tissue tension and 3D tissue shape by regulating cortical actomyosin network formation. Acts via ARHGAP18, a Rho GTPase activating protein that suppresses F-actin polymerization. Plays a key role in controlling cell proliferation in response to cell contact. Phosphorylation of YAP1 by LATS1/2 inhibits its translocation into the nucleus to regulate cellular genes important for cell proliferation, cell death, and cell migration. The presence of TEAD transcription factors are required for it to stimulate gene expression, cell growth, anchorage-independent growth, and epithelial mesenchymal transition (EMT) induction. Suppresses ciliogenesis via acting as a transcriptional corepressor of the TEAD4 target genes AURKA and PLK1. In conjunction with WWTR1, involved in the regulation of TGFB1-dependent SMAD2 and SMAD3 nuclear accumulation.; Activates the C-terminal fragment (CTF) of ERBB4 (isoform 3).; Activates the C-terminal fragment (CTF) of ERBB4 (isoform 3).
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TMPY-04398 | MST1 Protein, Human, Recombinant (His) | Human | Baculovirus-Insect Cells | ||
Dysregulation of MST1/STK4, a key kinase component of the Hippo-YAP pathway, is linked to the etiology of many cancers with poor prognosis. STK4/Hippo pathway may have important therapeutic implications for cancer. The tumor suppressor serine/threonine-protein kinase 4 (STK4) differentially regulates TLR3/4/9-mediated inflammatory responses in macrophages and thereby is protective against chronic inflammation-associated Hepatocellular carcinoma (HCC). STK4 has potential as a diagnostic biomarker and therapeutic target for inflammation-induced HCC.
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TMPH-03208 | IL-6 Protein, Rabbit, Recombinant (His) | Rabbit | Yeast | ||
Cytokine with a wide variety of biological functions in immunity, tissue regeneration, and metabolism. Binds to IL6R, then the complex associates to the signaling subunit IL6ST/gp130 to trigger the intracellular IL6-signaling pathway. The interaction with the membrane-bound IL6R and IL6ST stimulates 'classic signaling', whereas the binding of IL6 and soluble IL6R to IL6ST stimulates 'trans-signaling'. Alternatively, 'cluster signaling' occurs when membrane-bound IL6:IL6R complexes on transmitter cells activate IL6ST receptors on neighboring receiver cells.; IL6 is a potent inducer of the acute phase response. Rapid production of IL6 contributes to host defense during infection and tissue injury, but excessive IL6 synthesis is involved in disease pathology. In the innate immune response, is synthesized by myeloid cells, such as macrophages and dendritic cells, upon recognition of pathogens through toll-like receptors (TLRs) at the site of infection or tissue injury. In the adaptive immune response, is required for the differentiation of B cells into immunoglobulin-secreting cells. Plays a major role in the differentiation of CD4(+) T cell subsets. Essential factor for the development of T follicular helper (Tfh) cells that are required for the induction of germinal-center formation. Required to drive naive CD4(+) T cells to the Th17 lineage. Also required for proliferation of myeloma cells and the survival of plasmablast cells.; Acts as an essential factor in bone homeostasis and on vessels directly or indirectly by induction of VEGF, resulting in increased angiogenesis activity and vascular permeability. Induces, through 'trans-signaling' and synergistically with IL1B and TNF, the production of VEGF. Involved in metabolic controls, is discharged into the bloodstream after muscle contraction increasing lipolysis and improving insulin resistance. 'Trans-signaling' in central nervous system also regulates energy and glucose homeostasis. Mediates, through GLP-1, crosstalk between insulin-sensitive tissues, intestinal L cells and pancreatic islets to adapt to changes in insulin demand. Also acts as a myokine. Plays a protective role during liver injury, being required for maintenance of tissue regeneration. Also has a pivotal role in iron metabolism by regulating HAMP/hepcidin expression upon inflammation or bacterial infection. Through activation of IL6ST-YAP-NOTCH pathway, induces inflammation-induced epithelial regeneration.
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TMPH-03500 | IL-6 Protein, Sheep, Recombinant (GST) | Sheep | E. coli | ||
Cytokine with a wide variety of biological functions in immunity, tissue regeneration, and metabolism. Binds to IL6R, then the complex associates to the signaling subunit IL6ST/gp130 to trigger the intracellular IL6-signaling pathway. The interaction with the membrane-bound IL6R and IL6ST stimulates 'classic signaling', whereas the binding of IL6 and soluble IL6R to IL6ST stimulates 'trans-signaling'. Alternatively, 'cluster signaling' occurs when membrane-bound IL6:IL6R complexes on transmitter cells activate IL6ST receptors on neighboring receiver cells.; IL6 is a potent inducer of the acute phase response. Rapid production of IL6 contributes to host defense during infection and tissue injury, but excessive IL6 synthesis is involved in disease pathology. In the innate immune response, is synthesized by myeloid cells, such as macrophages and dendritic cells, upon recognition of pathogens through toll-like receptors (TLRs) at the site of infection or tissue injury. In the adaptive immune response, is required for the differentiation of B cells into immunoglobulin-secreting cells. Plays a major role in the differentiation of CD4(+) T cell subsets. Essential factor for the development of T follicular helper (Tfh) cells that are required for the induction of germinal-center formation. Required to drive naive CD4(+) T cells to the Th17 lineage. Also required for proliferation of myeloma cells and the survival of plasmablast cells.; Acts as an essential factor in bone homeostasis and on vessels directly or indirectly by induction of VEGF, resulting in increased angiogenesis activity and vascular permeability. Induces, through 'trans-signaling' and synergistically with IL1B and TNF, the production of VEGF. Involved in metabolic controls, is discharged into the bloodstream after muscle contraction increasing lipolysis and improving insulin resistance. 'Trans-signaling' in central nervous system also regulates energy and glucose homeostasis. Mediates, through GLP-1, crosstalk between insulin-sensitive tissues, intestinal L cells and pancreatic islets to adapt to changes in insulin demand. Also acts as a myokine. Plays a protective role during liver injury, being required for maintenance of tissue regeneration. Also has a pivotal role in iron metabolism by regulating HAMP/hepcidin expression upon inflammation or bacterial infection. Through activation of IL6ST-YAP-NOTCH pathway, induces inflammation-induced epithelial regeneration.
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TMPH-01689 | PLD6 Protein, Human, Recombinant (His) | Human | E. coli | ||
Presents phospholipase and nuclease activities, depending on the different physiological conditions. Interaction with Mitoguardin (MIGA1 or MIGA2) affects the dimer conformation, facilitating the lipase activity over the nuclease activity. Plays a key role in mitochondrial fusion and fission via its phospholipase activity. In its phospholipase role, it uses the mitochondrial lipid cardiolipin as substrate to generate phosphatidate (PA or 1,2-diacyl-sn-glycero-3-phosphate), a second messenger signaling lipid. Production of PA facilitates Mitofusin-mediated fusion, whereas the cleavage of PA by the Lipin family of phosphatases produces diacylgycerol (DAG) which promotes mitochondrial fission. Both Lipin and DAG regulate mitochondrial dynamics and membrane fusion/fission, important processes for adapting mitochondrial metabolism to changes in cell physiology. Mitochondrial fusion enables cells to cope with the increased nucleotide demand during DNA synthesis. Mitochondrial function and dynamics are closely associated with biological processes such as cell growth, proliferation, and differentiation. Mediator of MYC activity, promotes mitochondrial fusion and activates AMPK which in turn inhibits YAP/TAZ, thereby inducing cell growth and proliferation. The endonuclease activity plays a critical role in PIWI-interacting RNA (piRNA) biogenesis during spermatogenesis. Implicated in spermatogenesis and sperm fertility in testicular germ cells, its single strand-specific nuclease activity is critical for the biogenesis/maturation of PIWI-interacting RNA (piRNA). MOV10L1 selectively binds to piRNA precursors and funnels them to the endonuclease that catalyzes the first cleavage step of piRNA processing to generate piRNA intermediate fragments that are subsequently loaded to Piwi proteins. Cleaves either DNA or RNA substrates with similar affinity, producing a 5' phosphate end, in this way it participates in the processing of primary piRNA transcripts. piRNAs provide essential protection against the activity of mobile genetic elements. piRNA-mediated transposon silencing is thus critical for maintaining genome stability, in particular in germline cells when transposons are mobilized as a consequence of wide-spread genomic demethylation. PA may act as signaling molecule in the recognition/transport of the precursor RNAs of primary piRNAs. Interacts with tesmin in testes, suggesting a role in spermatogenesis via association with its interacting partner.
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