目录号 | 产品详情 | 靶点 | |
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T79560 | Akt | ||
22-(4′-py)-JA是久那霉素A的半合成衍生物,源自泰国蓝海绵(Xestospongia sp.)。该化合物显示出抗转移活性,能抑制AKT/mTOR/p70S6K信号通路,并阻断人脐静脉内皮细胞(HUVEC)中肿瘤细胞侵袭及管形成作用。它通过下调金属蛋白酶(MMP-2和MMP-9)、缺氧诱导因子1α(HIF-1α)和血管内皮生长因子(VEGF)来发挥作用。此外,22-(4′-py)-JA对非小细胞肺癌(NSCLC)显示出显著的抗癌效果。 | |||
T83877 | |||
2-(cyclohexylmethyl)-Plumbagin是naphthoquinone plumbagin的衍生物。在模拟胰腺癌肿瘤微环境的营养匮乏条件下,与营养丰富条件下的PANC-1细胞相比,对PANC-1人类胰腺癌细胞表现出选择性的细胞毒性,50%优选细胞毒性值(PC50s)分别为0.11和47.2 µM。1 µM浓度下,还可诱导PANC-1细胞发生凋亡。此外,2-(cyclohexylmethyl)-Plumbagin在营养匮乏条件下,而非营养丰富条件下,选择性降低PANC-1细胞中Akt和哺乳动物雷帕霉素靶蛋白(mTOR)的磷酸化。在以每周五次、每次50和250 µg/动物剂量给药的MiaPaCa-2胰腺癌小鼠异种移植模型中,能减少肿瘤体积和重量。 | |||
T69963 | |||
Birabresib dihydrate was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibitor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and differentiation to energy homeostasis and neurological processes. OTX015 has potent antiproliferative activity accompanied by c-MYC down-regulation in several tumor types, and has demonstrated synergism with the mTOR inhibitor everolimus in different models. Oral administration of OTX-015 markedly inhibited tumor growth and reduced tumor volume. OTX015 is currently in Phase 1b studies for the treatment of hematological malignancies and advanced solid tumors such as Triple Negative Breast ...... | |||
T62771 | |||
AKT-IN-9 是一种 AKT 的有效抑制剂。其中蛋白激酶 B (PKB,也称为 AKT) 是细胞中 PI3K/AKT/mTOR 信号传导的核心,在细胞生长、存活、分化和代谢中发挥着重要用处。AKT-IN-9 具有潜力进行乳腺癌和前列腺癌的研究。 | |||
T39733 | Akt | ||
Hu7691 free base 是一种具有口服活性、高效性和选择性的 Akt 抑制剂,对多种神经母细胞瘤细胞系的抗增殖和神经发生作用。Hu7691 free base 抑制 Akt1、Akt2 和 Akt3 ,诱导神经母细胞瘤细胞分化。 | |||
T35519 | |||
Aflatoxin B2-13C17(AFB2-13C17) is intended for use as an internal standard for the quantification of AFB2by GC- or LC-MS. AFB2is a mycotoxin that has been found inA. terricola.1It induces hepatic autophagy and apoptosis in broiler chickens when administered at doses of 0.2, 0.4, and 0.8 mg/kg.2AFB2(0.5 and 1 mg/animal) also induces parenchymal cell hyperplasia in rats.3 1.Moubasher, A.H., el-Kady, I.A., and Shoriet, A.Toxigenic Aspergilli isolated from different sources in EgyptAnn. Nutr. Aliment.31(4-6)607-615(1977) 2.Chen, B., Li, D., Li, M., et al.Induction of mitochondria-mediated apoptosis and PI3K/Akt/mTOR-mediated autophagy by aflatoxin B2 in hepatocytes of broilersOncotarget7(51)84989-84998(2016) 3.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins and analogsCancer Res.31(12)1936-1942(1971) | |||
TN2095 | NOS NF-κB PDE | ||
Pomiferin is a natural product inhibitor of carbonic anhydrase I and II isoenzymes. It has anticancer, antibacterial and antidiabetic properties. Pomiferin has anti-inflammatory and neuroprotective activities. | |||
T16365 | Others | ||
Buparlisib Hydrochloride is an inhibitor of pan-class I PI3K (IC50: 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively). |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-02089 | mTOR Protein, Human, Recombinant (His & Myc) | Human | E. coli | ||
mTOR Protein, Human, Recombinant (His & Myc) is expressed in E. coli.
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TMPY-02252 | LAMTOR2 Protein, Human, Recombinant (His) | Human | E. coli | ||
Ragulator complex protein LAMTOR2, also known as Endosomal adaptor protein p14, Late endosomal/lysosomal Mp1-interacting protein, Late endosomal/lysosomal adaptor and MAPK and MTOR activator 2, Mitogen-activated protein-binding protein-interacting protein, Roadblock domain-containing protein 3, LAMTOR2, MAPBPIP, and ROBLD3, is a protein which belongs to the GAMAD family. LAMTOR2 / ROBLD3 is a regulator of the TOR pathway, a signaling cascade that promotes cell growth in response to growth factors, energy levels, and amino acids. As part of the Ragulator complex, LAMTOR2 / ROBLD3 recruits the Rag GTPases and the mTORC1 complex to lysosomes, a key step in the activation of the TOR signaling cascade by amino acids. LAMTOR2 / ROBLD3 is an adapter protein that enhances the efficiency of the MAP kinase cascade facilitating the activation of MAPK2. Defects in LAMTOR2 are the cause of immunodeficiency due to defects in MAPBP-interacting protein (ID-MAPBPIP). This form of primary immunodeficiency syndrome includes congenital neutropenia, partial albinism, short stature, and B-cell and cytotoxic T-cell deficiency.
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TMPJ-01378 | Mp1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Mitogen-Activated Protein Kinase Scaffold Protein 1 (MAPKSP1) was identified as an interacting protein that belongs to the LAMTOR3 family. MAPKSP1 restricted to late endosomes by the mitogen-activated protein-binding protein-interacting protein, and binds specifically to MAP kinase kinase MAP2K1/MEK1, MAP kinase MAPK3/ERK1, and MAP kinase MAPK1/ERK2. MAPKSP1 interacts with MAP2K1/MEK1 and MAPK2 and enhances the activation of MAPK2, and thus is thought to function as an adaptor to enhance the efficiency of the MAP kinase cascade.
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TMPK-00524 | CA9/Carbonic Anhydrase IX Protein, Cynomolgus, Recombinant (His) | Cynomolgus | HEK293 | ||
CA9 is a member of the carbonic anhydrases' family, that is often expressed in cancer cells under hypoxic condition. CA9 expression potentially contributes to the regulation of cancer cell differentiation and mediates tumour-associated genes and signalling pathways, including apoptosis, hypoxia, G2M checkpoint, PI3K/AKR/mTOR signalling and TGF-beta signalling pathways.
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TMPK-00283 | CA9/Carbonic Anhydrase IX Protein, Human, Recombinant (His & Avi) | Human | HEK293 | ||
CA9 is a member of the carbonic anhydrases' family, that is often expressed in cancer cells under hypoxic condition. CA9 expression potentially contributes to the regulation of cancer cell differentiation and mediates tumour-associated genes and signalling pathways, including apoptosis, hypoxia, G2M checkpoint, PI3K/AKR/mTOR signalling and TGF-beta signalling pathways.
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TMPY-04540 | S6K1/RPS6KB1 Protein, Human, Recombinant (GST) | Human | Baculovirus-Insect Cells | ||
PS6K, also known as RPS6KB1, is a serine/threonine-protein kinase. It belongs to the RSK (ribosomal s6 kinase) family. Members of this family function in signal transduction. PS6K is an isoform of p70 ribosomal S6 kinase (S6K). S6K can be activated by mitogenic stimuli such as growth factors, insulin and cytokines. It phosphorylates the ribosomal protein S6. PS6K also phosphorylates other proteins such as elF4B, eEF2K and SKAR. It is a crucial effector of mTOR(rapamycin) signaling. PS6K is dissociated from the EIF3 complex and activated upon mitogenic stimulation, phosphorylation by the mammalian target of mTOR complex 1 (mTORC1). Its active form then phosphorylates and activates several substrates in the preinitiation complex, including the EIF2B complex and the cap-binding complex component EIF4B. PS6K also functions in cell proliferation, cell growth and cell cycle progression.
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TMPK-00416 | FLT3 Protein, Human, Recombinant (His & Avi), Biotinylated | Human | CHO | ||
The Flt-3 (fms-like tyrosine kinase) receptor, also named Flk-2 (fetal liver kinase) and Stk-1(stem cell tyrosine kinase) is a member of the class III subfamily of receptor tyrosine kinases that also includes KIT, the receptor for SCF and FMS, the receptor for M-CSF. Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells. Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or MAPK3/ERK1.
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TMPK-00523 | FLT3 Protein, Cynomolgus, Recombinant (hFc) | Cynomolgus | HEK293 | ||
The Flt-3 (fms-like tyrosine kinase) receptor, also named Flk-2 (fetal liver kinase) and Stk-1(stem cell tyrosine kinase) is a member of the class III subfamily of receptor tyrosine kinases that also includes KIT, the receptor for SCF and FMS, the receptor for M-CSF. Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells. Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or MAPK3/ERK1.
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TMPY-06821 | THRB Protein, Human, Recombinant (His) | Human | E. coli | ||
Thyroid hormone receptor beta (THRB), also known as TRbeta and NR1A2, belongs to the nuclear hormone receptor family. Featuring an N-terminal transactivation domain, a central DNA-binding domain, and a hormone/ligand-binding domain, THRB isoform 1/2 expression localizes predominately to the liver and pituitary, respectively. THRB regulates the feedback of T3-dependent thyrotropin-stimulating hormone (TSH) transcription in the pituitary by binding to thyroid hormone (TH) response elements present on promoters of TH-responsive genes. Located on chromosome 3p24, THRB gene mutation has been linked to autosomal dominant resistance to TH (RTH), which is characterized by goiter and elevated levels of T3, T4, and TSH. THRB is a known pharmacological target for the treatment of non-alcoholic steatohepatitis (NASH). THRB may be a target for future cancer therapies since its knockdown enhanced the viability of endometrial cancer cells and activated the mTOR-4EBP1/eIF4G pathway.
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TMPY-01275 | 14-3-3 sigma Protein, Human, Recombinant | Human | E. coli | ||
14-3-3 protein sigma (YWHAS), also known as stratifin (SFN) and epithelial cell marker protein 1, is a member of the 14-3-3 proteins which are a family of conserved regulatory molecules expressed in all eukaryotic cells. The name 14-3-3 refers to the particular elution and migration pattern of these proteins on DEAE-cellulose chromatography and starch-gel electrophoresis. The 14-3-3 proteins eluted in the 14th fraction of bovine brain homogenate and were found on positions 3.3 of subsequent electrophoresis. There are seven genes that encode 14-3-3s in most mammals. 14-3-3 proteins have been identified as adapter proteins implicated in the regulation of a large spectrum of both general and specialized signaling pathways. More than 1 signaling proteins have been reported as 14-3-3 ligands including kinases, phosphatases, and transmembrane receptors, and the binding generally results in the modulation of the activity of the binding partner. YWHAE exists as a homodimer and present mainly in tissues enriched in stratified squamous keratinising epithelium. YWHAS has been repoted to interact with KRT17 and GAB2, and may regulate protein synthesis and epithelial cell growth by stimulating Akt/mTOR pathway upon binding to KRT17. Additionally, YWHAS (SFN) may also act as a p53-regulated inhibitor of G2/M progression.
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TMPH-02855 | PML Protein, Mouse, Recombinant (His & Myc) | Mouse | E. coli | ||
Functions via its association with PML-nuclear bodies (PML-NBs) in a wide range of important cellular processes, including tumor suppression, transcriptional regulation, apoptosis, senescence, DNA damage response, and viral defense mechanisms. Acts as the scaffold of PML-NBs allowing other proteins to shuttle in and out, a process which is regulated by SUMO-mediated modifications and interactions. Positively regulates p53/TP53 by acting at different levels (by promoting its acetylation and phosphorylation and by inhibiting its MDM2-dependent degradation). Regulates phosphorylation of ITPR3 and plays a role in the regulation of calcium homeostasis at the endoplasmic reticulum. Regulates RB1 phosphorylation and activity. Acts as both a negative regulator of PPARGC1A acetylation and a potent activator of PPAR signaling and fatty acid oxidation. Regulates translation of HIF1A by sequestering MTOR, and thereby plays a role in neoangiogenesis and tumor vascularization. Regulates PER2 nuclear localization and circadian function. Cytoplasmic PML is involved in the regulation of the TGF-beta signaling pathway. Required for normal development of the brain cortex during embryogenesis. Plays a role in granulopoiesis or monopoiesis of myeloid progenitor cells. May play a role regulating stem and progenitor cell fate in tissues as diverse as blood, brain and breast. Shows antiviral activity towards lymphocytic choriomeningitis virus (LCMV) and the vesicular stomatitis virus (VSV).
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TMPY-01263 | 14-3-3 sigma Protein, Human, Recombinant (GST) | Human | E. coli | ||
14-3-3 protein sigma (YWHAS), also known as stratifin (SFN) and epithelial cell marker protein 1, is a member of the 14-3-3 proteins which are a family of conserved regulatory molecules expressed in all eukaryotic cells. The name 14-3-3 refers to the particular elution and migration pattern of these proteins on DEAE-cellulose chromatography and starch-gel electrophoresis. The 14-3-3 proteins eluted in the 14th fraction of bovine brain homogenate and were found on positions 3.3 of subsequent electrophoresis. There are seven genes that encode 14-3-3s in most mammals. 14-3-3 proteins have been identified as adapter proteins implicated in the regulation of a large spectrum of both general and specialized signaling pathways. More than 1 signaling proteins have been reported as 14-3-3 ligands including kinases, phosphatases, and transmembrane receptors, and the binding generally results in the modulation of the activity of the binding partner. YWHAE exists as a homodimer and present mainly in tissues enriched in stratified squamous keratinising epithelium. YWHAS has been repoted to interact with KRT17 and GAB2, and may regulate protein synthesis and epithelial cell growth by stimulating Akt/mTOR pathway upon binding to KRT17. Additionally, YWHAS (SFN) may also act as a p53-regulated inhibitor of G2/M progression.
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TMPY-02113 | 14-3-3 sigma Protein, Mouse, Recombinant | Mouse | E. coli | ||
14-3-3 protein sigma (YWHAS), also known as stratifin (SFN) and epithelial cell marker protein 1, is a member of the 14-3-3 proteins which are a family of conserved regulatory molecules expressed in all eukaryotic cells. The name 14-3-3 refers to the particular elution and migration pattern of these proteins on DEAE-cellulose chromatography and starch-gel electrophoresis. The 14-3-3 proteins eluted in the 14th fraction of bovine brain homogenate and were found on positions 3.3 of subsequent electrophoresis. There are seven genes that encode 14-3-3s in most mammals. 14-3-3 proteins have been identified as adapter proteins implicated in the regulation of a large spectrum of both general and specialized signaling pathways. More than 1 signaling proteins have been reported as 14-3-3 ligands including kinases, phosphatases, and transmembrane receptors, and the binding generally results in the modulation of the activity of the binding partner. YWHAE exists as a homodimer and present mainly in tissues enriched in stratified squamous keratinising epithelium. YWHAS has been repoted to interact with KRT17 and GAB2, and may regulate protein synthesis and epithelial cell growth by stimulating Akt/mTOR pathway upon binding to KRT17. Additionally, YWHAS (SFN) may also act as a p53-regulated inhibitor of G2/M progression.
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TMPH-01710 | Mucolipin-1/MCOLN1 Protein, Human, Recombinant (His) | Human | in vitro E. coli expression system | ||
Nonselective cation channel probably playing a role in the regulation of membrane trafficking events and of metal homeostasis. Proposed to play a major role in Ca(2+) release from late endosome and lysosome vesicles to the cytoplasm, which is important for many lysosome-dependent cellular events, including the fusion and trafficking of these organelles, exocytosis and autophagy. Required for efficient uptake of large particles in macrophages in which Ca(2+) release from the lysosomes triggers lysosomal exocytosis. May also play a role in phagosome-lysosome fusion. Involved in lactosylceramide trafficking indicative for a role in the regulation of late endocytic membrane fusion/fission events. By mediating lysosomal Ca(2+) release is involved in regulation of mTORC1 signaling and in mTOR/TFEB-dependent lysosomal adaptation to environmental cues such as nutrient levels. Seems to act as lysosomal active oxygen species (ROS) sensor involved in ROS-induced TFEB activation and autophagy. Functions as a Fe(2+) permeable channel in late endosomes and lysosomes. Proposed to play a role in zinc homeostasis probably implicating its association with TMEM163 In adaptive immunity, TRPML2 and TRPML1 may play redundant roles in the function of the specialized lysosomes of B cells.; May contribute to cellular lipase activity within the late endosomal pathway or at the cell surface which may be involved in processes of membrane reshaping and vesiculation, especially the growth of tubular structures. However, it is not known, whether it conveys the enzymatic activity directly, or merely facilitates the activity of an associated phospholipase.
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