目录号 | 产品详情 | 靶点 | |
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T22677 | MEK | ||
Cobimetinib racemate (Cobimetinib (racemate)) 是 Cobimetinib 的外消旋体,是一种选择性 MEK 抑制剂。 | |||
T12697 | MEK | ||
Refametinib R enantiomer (RDEA119 R enantiomer) 是一种 MEK 抑制剂,EC50为 2.0-15 nM。Refametinib R enantiomer 具有抗癌活性,可用于研究癌症。 | |||
T4178 | Others | ||
NSC 80538 是多重 HTS 检测中 MEK Kinase PB1 Domains 的抑制剂。 | |||
T9460 | PI3K | ||
iMDK 是PI3K 抑制剂,能够抑制生长因子MDK。它能够与 MEK 抑制剂协同抑制非小细胞肺癌,而不会伤害正常细胞和小鼠。 | |||
T6419 | Apoptosis FAK MEK IGF-1R Src | ||
BMS-536924 (BMS 536924) 是一种具有口服活性,竞争性和选择性的胰岛素样生长因子受体激酶和胰岛素受体抑制剂,IC50分别为 100 nM 和 73 nM。它具有抗癌活性。 | |||
T2327 | EGFR Raf MEK Src | ||
Pelitinib (EKB-569) 是一种可逆的EGFR 抑制剂,IC50值为38.5 nM。它也抑制Src、MEK/ERK 和 ErbB2,IC50值分别为282、800 和 1255 nM。 | |||
T6S1740 | Others | ||
Nardosinone 是一个 dbcAMP 和 staurosporine 的神经生成作用增强剂,分离自Nardostachys chinensis 中。Nardosinone 可能成为一种有用的药理学工具,不仅可用于研究神经生长因子 (NGF) 的作用机理,而且可用于研究神经毒性物质的作用机理。 | |||
T7190 | Apoptosis Akt JNK Autophagy | ||
Actein 是从升麻的根茎中分离的一种三萜糖苷,通过促进ROS/JNK 活化和钝化人膀胱癌中的AKT 途径来抑制细胞增殖,诱导自噬和凋亡。 | |||
T15193 | MEK | ||
EBI-1051 is a highly potent and orally efficacious inhibitor of MEK (IC50: 3.9 nM). | |||
T75110 | |||
Trametiglue 是 Trametinib 的衍生物,通过独特的界面结合相互作用,以前所未有的效力和选择性靶向 KSR-MEK 和 RAF-MEK。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-04544 | MEK2 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
Dual specificity mitogen-activated protein kinase kinase 2, also known as MAP kinase kinase 2, MAPKK2, ERK activator kinase 2, MAPK / ERK kinase 2, MEK2 and MAP2K2, is a member of the protein kinase superfamily, STE Ser/Thr protein kinase family and MAP kinase kinase subfamily. MAP2K2 / MEK2 contains one protein kinase domain. MEK1 and MEK2 (also known as MAP2K1 and MAP2K2, respectively) are evolutionarily conserved, dual-specificity kinases that mediate Erk1 and Erk2 activation during adhesion and growth factor signaling. MAP2K1 / MEK1 is a crucial modulator of Mek and Erk signaling and have potential implications for the role of MEK1 and MEK2 in tumorigenesis. MAP2K2 / MEK2 catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. It also activates the ERK1 and ERK2 MAP kinases. Defects in MAP2K2 are a cause of Cardiofaciocutaneous Syndrome (CFC Syndrome) which is characterized by a distinctive facial appearance, heart defects, and mental retardation. Heart defects include pulmonic stenosis, atrial septal defects, and hypertrophic cardiomyopathy.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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TMPY-04572 | MKK4 Protein, Mouse, Recombinant (His & GST) | Mouse | Baculovirus Insect Cells | ||
Dual specificity mitogen-activated protein kinase kinase 4, also known as MAP kinase kinase 4, MAPKK4, JNK-activating kinase 1, MAPK/ERK kinase 4, SAPK/ERK kinase 1, c-Jun N-terminal kinase kinase 1, JNKK, and MAP2K4, is a protein that belongs to the protein kinase superfamily, STE Ser/Thr protein kinase family and MAP kinase kinase subfamily. MAP2K4 / JNKK1 is a protein kinase that is a direct activator of MAP kinases in response to various environmental stresses or mitogenic stimuli. MAP2K4 / JNKK1 has been shown to activate MAPK8 / JNK1, MAPK9 / JNK2, and MAPK14 / p38, but not MAPK1 / ERK2 or MAPK3 / ERK1. MAP2K4 / JNKK1 is phosphorylated, and thus activated by MAP3K1 / MEKK. The stress-activated protein kinase (SAPK) pathways represent phosphorylation cascades that convey pro-apoptotic signals. The mitogen-activated protein kinase kinase (MAPKK) homolog MAP2K4 ( MKK4, SEK, JNKK1 ) is a centrally-placed mediator of the SAPK pathways.
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TMPK-00024 | Midkine Protein, Human, Recombinant (His & Avi), Biotinylated | Human | E. coli | ||
Midkine is a heparin-binding growth factor, originally reported as the product of a retinoic acid-responsive gene during embryogenesis, but currently viewed as a multifaceted factor contributing to both normal tissue homeostasis and disease development. Midkine is abnormally expressed at high levels in various human malignancies and acts as a mediator for the acquisition of critical hallmarks of cancer, including cell growth, survival, metastasis, migration, and angiogenesis. Midkine Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in E. coli expression system with N-His-Avi tag. The predicted molecular weight is 16.46 kDa and the accession number is P21741-1.
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TMPK-00023 | Midkine Protein, Human, Recombinant (His & Avi) | Human | E. coli | ||
Midkine is a heparin-binding growth factor, originally reported as the product of a retinoic acid-responsive gene during embryogenesis, but currently viewed as a multifaceted factor contributing to both normal tissue homeostasis and disease development. Midkine is abnormally expressed at high levels in various human malignancies and acts as a mediator for the acquisition of critical hallmarks of cancer, including cell growth, survival, metastasis, migration, and angiogenesis. Midkine Protein, Human, Recombinant (His & Avi) is expressed in E. coli expression system with N-His-Avi tag. The predicted molecular weight is 16.46 kDa and the accession number is P21741-1.
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TMPK-00812 | Midkine Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Midkine is a heparin-binding growth factor, originally reported as the product of a retinoic acid-responsive gene during embryogenesis, but currently viewed as a multifaceted factor contributing to both normal tissue homeostasis and disease development. Midkine is abnormally expressed at high levels in various human malignancies and acts as a mediator for the acquisition of critical hallmarks of cancer, including cell growth, survival, metastasis, migration, and angiogenesis. Midkine Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-His tag. The predicted molecular weight is 14.03 kDa and the accession number is P12025.
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TMPY-04756 | MEK1 Protein, Mouse, Recombinant | Mouse | Baculovirus Insect Cells | ||
MEK1 Protein, Mouse, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 43.6 kDa and the accession number is P31938.
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TMPY-04569 | MEK1 Protein, Mouse, Recombinant (His & GST) | Mouse | Baculovirus Insect Cells | ||
MEK1 Protein, Mouse, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 71.3 kDa and the accession number is P31938.
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TMPY-04364 | MKK6 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
MKK6 Protein, Human, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 65.3 kDa and the accession number is P52564-1.
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TMPY-04749 | MKK6 Protein, Human, Recombinant (S207D, T211D) | Human | Baculovirus Insect Cells | ||
MKK6 Protein, Human, Recombinant (S207D, T211D) is expressed in Baculovirus insect cells. The predicted molecular weight is 37.7 kDa and the accession number is P52564-1.
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TMPY-04365 | MKK6 Protein, Human, Recombinant (S207D, T211D, His & GST) | Human | Baculovirus Insect Cells | ||
MKK6 Protein, Human, Recombinant (S207D, T211D, His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 65.3 kDa and the accession number is P52564-1.
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TMPY-04748 | MKK6 Protein, Human, Recombinant | Human | Baculovirus Insect Cells | ||
MKK6 Protein, Human, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 37.6 kDa and the accession number is A8K3Y2.
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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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TMPY-05004 | FGF-4 Protein, Human, Recombinant | Human | E. coli | ||
FGF (fibroblast growth factor) signalling is known to be required for many aspects of mesoderm formation and patterning during Xenopus development and has been implicated in regulating genes required for the specification of both blood and skeletal muscle lineages. Fibroblast growth factor 4 (FGF4) signaling induces differentiation from embryonic stem cells (ESCs) via the phosphorylation of downstream molecules such as mitogen-activated protein kinase/extracellular signal-related kinase (MEK) and extracellular signal-related kinase 1/2 (ERK1/2). Fibroblast Growth Factor 4 (FGF-4) could not only increase the proliferation of bone marrow mesenchymal stem cells (BMSCs), but also induce BMSCs into hepatocyte-like cells in vitro. FGF4 transduced BMSCs contributed to liver regeneration might by the transplanted microenvironment. The FGF4-bFGF BMSCs thus can enhance the survival of the transplanted cells, diminish myocardial fibrosis, promote myocardial angiogenesis, and improve cardiac functions.
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TMPH-03368 | SG3/Secretogranin 3 Protein, Rat, Recombinant (His & Myc) | Rat | E. coli | ||
Member of the granin protein family that regulates the biogenesis of secretory granules. Acts as a sorting receptor for intragranular proteins including chromogranin A/CHGA. May also play a role in angiogenesis. Promotes endothelial proliferation, migration and tube formation through MEK/ERK signaling pathway. SG3/Secretogranin 3 Protein, Rat, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 58.2 kDa and the accession number is P47868.
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TMPY-04410 | MAP4K5 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
Mitogen-activated protein kinase kinase kinase kinase 5, also known as Kinase homologous to SPS1/STE2, MAPK/ERK kinase kinase kinase 5, MEK kinase kinase 5, and MAP4K5, is a cytoplasm protein that belongs to the protein kinase superfamily, STE Ser/Thr protein kinase family and STE2 subfamily. MAP4K5 is ubiquitously expressed in all tissues examined, with high levels in the ovary, testis, and prostate. It contains one CNH domain and one protein kinase domain. MAP4K5 is highly similar to yeast SPS1/STE2 kinase. Yeast SPS1/STE2 functions near the beginning of the MAP kinase signal cascades that are essential for yeast pheromone response. MAP4K5 has been shown to interact with CRKL and TRAF2. This kinase was shown to activate Jun kinase in mammalian cells. MAP4K5 is an early component of MAP kinase signal cascades. It may play a role in the response to environmental stress. MAP4K5 appears to act upstream of the JUN N-terminal pathway.
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TMPY-04412 | Germinal Center Kinase/MAP4K2 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
Mitogen-activated protein kinase kinase kinase kinase 2, also known as B lymphocyte serine/threonine-protein kinase, Germinal center kinase, MAPK/ERK kinase kinase kinase 2, MEK kinase kinase 2, Rab8-interacting protein, and MAP4K2, is cytoplasm and peripheral membrane protein that belongs to the protein kinase superfamily, STE Ser/Thr protein kinase family and STE2 subfamily. MAP4K2 contains one CNH domain and one protein kinase domain. Although this kinase is found in many tissues, its expression in lymphoid follicles is restricted to the cells of the germinal center, where it may participate in B-cell differentiation. MAP4K2 can be activated by TNF-alpha and has been shown to specifically activate MAP kinases. It is also found to interact with TNF receptor-associated factor 2 (TRAF2), which is involved in the activation of MAP3K1 / MEKK1. MAP4K2 enhances MAP3K1 oligomerization, which may relieve amino-terminal mediated MAP3K1 autoinhibition and lead to activation following autophosphorylation. It may also play a role in the regulation of vesicle targeting or fusion.
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TMPY-04389 | MAP3K8 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
Mitogen-activated protein kinase kinase kinase 8, also known as Cancer Osaka thyroid oncogene, Proto-oncogene c-Cot, Serine/threonine-protein kinase cot, Tumor progression locus 2 and MAP3K8, is a cytoplasm protein that belongs to the protein kinase superfamily, STE Ser/Thr protein kinase family and MAP kinase kinase kinase subfamily. MAP3K8 is expressed in several normal tissues and human tumor-derived cell lines. Isoform 1 of MAP3K8 is activated specifically during the S and G2/M phases of the cell cycle. MAP3K8 is required for TLR4 activation of the MEK/ERK pathway. It can activate NF-kappa-B 1 by stimulating proteasome-mediated proteolysis of NF-kappa-B 1/p15. MAP3K8 plays a role in the cell cycle. The longer form has some transforming activity, although it is much weaker than the activated cot oncoprotein. MAP3K8 oncogene linked to human endometrial carcinoma suggesting that it may be another molecule involved in human endometrial cancer. MAP3K8 may also be an important mediator of intracellular mechanotransduction in human bone marrow-derived mesenchymal stem cells (MSCs).
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TMPY-04374 | MST4 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
MST4, also known as mammalian STE2-like protein kinase 4, is a novel member of the germinal center kinase subfamily of human Ste2-like kinases and is closely related to MST3. The 416 amino acid full-length MST4 contains a C-terminal regulatory domain and an N-terminal kinase domain, both of which are required for full activation of the kinase. MST4 is highly expressed in the placenta, thymus, and peripheral blood leukocytes. MST4 specifically activates ERK but not JNK or p38 MAPK in transiently transfected cells or stable cell lines, and thus is biologically active in the activation of the MEK/ERK pathway mediating cell growth and transformation. Further, MST4 kinase activity is stimulated significantly by epidermal growth factor receptor (EGFR) ligands, which are known to promote the growth of certain cancer cells. Accordingly, MST4 has a potential role in signal transduction pathways involved in cancer progression. Three alternatively spliced isoforms of MST4 have been isolated, and isoform 3 lacks an exon encoding kinase domain and may function as a dominant-negative regulator of the MST4 kinase.
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TMPY-02519 | BLVRB Protein, Human, Recombinant (His) | Human | E. coli | ||
Biliverdin reductase (hBVR) is a serine/threonine kinase that catalyzes reduction of the heme oxygenase (HO) activity product, biliverdin, to bilirubin. BVR consists of an N-terminal dinucleotide-binding domain (Rossmann-fold) and a C-terminal domain that contains a six-stranded β-sheet that is flanked on one face by several α-helices. The C-terminal and N-terminal domains interact extensively, forming the active site cleft at their interface. Biliverdin reductase (BVR) catalyzes the last step in heme degradation by reducing the γ-methene bridge of the open tetrapyrrole, biliverdin IXα, to bilirubin with the concomitant oxidation of a β-nicotinamide adenine dinucleotide (NADH) or β-nicotinamide adenine dinucleotide phosphate (NADPH) cofactor. It is now recognized that human BVR (hBVR) is a dual-specificity kinase (Ser / Thr and Tyr) upstream activator of the insulin/insulin growth factor-1 (IGF-1) and mitogen-activated protein kinase (MAPK) signaling pathways. Human BVR (hBVR) is essential for MAPK-extracellular signal-regulated kinase (ERK)1/2 (MEK)-eukaryotic-like protein kinase (Elk) signaling and has been identified as the cytoplasm-nuclear heme transporter of ERK1/2 and hematin, the key components of stress-responsive gene expression.
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TMPY-04562 | GRK2 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
G-protein coupled receptor kinase 2 (GRK2), also referred as Adrenergic, beta, receptor kinase 1 (ADRBK1), is a ubiquitous member of the G protein-coupled receptor kinase (GRK) family that appears to play a central, integrative role in signal transduction cascades. GRK2 can phosphorylate a growing number of non-GPCR substrates and associate with a variety of proteins related to signal transduction, thus suggesting that this kinase could also have diverse 'effector' functions. GRK2 has been reported to interact with a variety of signal transduction proteins related to cell migration such as MEK, Akt, PI3Kgamma or GIT. Interestingly, the levels of expression and activity of this kinase are altered in a number of inflammatory disorders (as rheumatoid arthritis or multiple sclerosis), thus suggesting that GRK2 may play an important role in the onset or development of these pathologies. The important physiological function of GRK2 as a modulator of the efficacy of GPCR signal transduction systems is exemplified by its relevance in cardiovascular physiopathology as well as by its emerging role in the regulation of chemokine receptors. Besides its canonical role in the modulation of the signalling mediated by many G protein-coupled receptors (GPCR), this protein can display a very complex network of functional interactions with a variety of signal transduction partners, in a stimulus, cell type, or context-specific way.
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