目录号 | 产品详情 | 靶点 | |
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T69826 | |||
U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. It was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase and mammalian target of rapamycin pathways. | |||
T72654 | |||
(R)-PD 0325901CL为PD 0325901CL的异构体,后者为一种用于癌症研究的有丝分裂原活化蛋白激酶(MEK)选择性抑制剂,能够在体外和体内抑制癌细胞生长。 | |||
T28862 | |||
ST-168 is a potent inhibitor of PI3K and MEK. ST-168 displays improved PI3K and MEK1 isoform inhibition. ST-168 demonstrated a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ isoforms and a 2.2-fold improvement | |||
T70430 | |||
XK489 is a synthetic quinoxaline phenoxypropionic acid derivative with proapoptotic and antiproliferative activities. R(+)XK469 selectively inhibits topoisomerase II-beta, blocks activation of MEK/MAPK signaling kinases, stimulates caspases, and upregulates p53-dependent proteins, including cyclins A and B1, thereby arresting cancer cells in the G2/M phase of the cell cycle. Both R(+) and S(-) isomers of this agent are cytotoxic, although the R-isomer is more potent. | |||
T71891 | |||
G-573 is an allosteric inhibitor of MEK that is both potent and selective. The IC(50) value for pERK inhibition in HCT116 tumours by G-573 was estimated to be 0.406 µM. The IC(50) values for tumour growth inhibition in HCT116 and H2122 were estimated to be 3.43 and 2.56 µM, respectively. ED(50) estimates in HCT116 and H2122 mouse xenograft models were estimated to be ~4.6 and 1.9 mg/kg/day, respectively. | |||
T78608 | Apoptosis | ||
CML-IN-1(compound 7)是一种高效抗癌药物,针对人类慢性粒细胞白血病(CML)细胞系K562,能有效诱导凋亡(apoptosis)。该化合物主要通过显著抑制PI3K/Akt信号通路的蛋白磷酸化来发挥作用,同时CML-IN-1(compound 4)也能通过抑制结直肠癌的MEK/ERK信号通路来阻止细胞增殖。 | |||
T71163 | |||
Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types. | |||
T78777 | Raf | ||
Vem-L-Cy5 (化合物3)是一款改造自Vemurafenib的BRAF抑制剂, 其结构通过近红外荧光团Cy5进行修饰。该化合物针对BRAFV600E具有特异性,并能有效阻断MEK的磷酸化作用。Vem-L-Cy5展现了良好的细胞内渗透能力,并能抑制多种癌细胞系的生长。 | |||
T21547 | ERK MEK MAPK Endogenous Metabolite | ||
PAF (C16) 是有效的 MAPK 和 MEK/ERK 激活剂,可诱导血管通透性增加。PAF (C16) (PAF (C16)) 是血小板活化因子,是一种磷脂衍生介质,也是 PAF G 蛋白偶联受体 (PAFR) 的配体。PAF (C16) 在体外实验中显示出抗凋亡和抗炎活性,通过与其受体 (PAF-R) 相互作用以执行细胞信号传导来抑制 caspase 依赖性凋亡。 | |||
T35594 | |||
The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 μM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Raf-MEK signaling, which results in an increased rate of SMN translation. |
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-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-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-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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