目录号 | 产品详情 | 靶点 | |
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T12224 | Others | ||
Nilotinib D6 is a deuterium labeled Nilotinib which is an orally available inhibitor of Bcr-Abl tyrosine kinase ,and with antineoplastic activity. | |||
T69296 | |||
PHA-680626 is a potent and selective PLK inhibitor. PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases. PHA-680626 inhibits Plk1 (IC50 = 0.53 μM), Plk2 (IC50 = 0.07 μM) and Plk3 (IC50 = 1.61 μM). | |||
T68383 | |||
BIIB028 is a small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2/Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to other molecules involved in cell cycle regulation and immune responses. | |||
T16750 | Apoptosis FLT PLK PI3K Bcr-Abl CDK PDGFR Src | ||
Rigosertib (ON-01910) 是一种多激酶抑制剂和选择性抗癌剂,通过抑制 PI3K/Akt 途径诱导细胞凋亡,促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。它是一种选择性的非 ATP 竞争性PLK1抑制剂,IC50值为 9 nM。 | |||
T36578 | |||
Commendamide (N-acyl-3-hydroxypalmitoyl-glycine) is a newly discovered GPCR G2A/GPR132 agonist (EC50=11.8 μM) that isolated from Bacteroides vulgatus. [1] G2A/GPR132 belongs to the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily. GPR132/G2A is first reported to be a transcriptional target for BCR-ABL tyrosine kinase attenuating B-cell expansion in vitro and arresting cells at G2 during mitosis. It has been involved in autoimmune disease and atherosclerosis. [1] Commendamide and structurally related endogenous long-chain N-Acyl-amides activates discrete human receptors. In a screen for agonist activity against a library of 242 GPCRs, commendamide is found to activate a single receptor G2A/GPR132. This activity is confirmed by a synthetic sample of commendamide. Commendamide analogs with changes in the head group or acyl chain also exhibited reduced GPR132/G2A activity. [1] | |||
T6070 | PLK | ||
ON-01910 是一种非 ATP 竞争性 PLK1 抑制剂(IC50 为 9 nM,在无细胞试验中)。它对 Plk2 的选择性高出 30 倍,对 Plk3 没有活性。 Rigosertib 抑制 PI3K/Akt 通路并激活氧化应激信号。 Rigosertib 可诱导多种癌细胞凋亡。它是一种合成的苄基苯乙烯基砜类似物,具有潜在的抗肿瘤活性。 | |||
T5818 | Apoptosis PLK PI3K | ||
Rigosertib sodium (ON-01910) 是一种选择性的非 ATP 竞争性PLK1抑制剂,IC50值为 9 nM。它是一种多激酶抑制剂和选择性抗癌剂,通过抑制PI3K/Akt 途径诱导细胞凋亡,促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。 | |||
T11523 | PDGFR | ||
GZD856 is an orally bioavailable PDGFRα/β inhibitor (IC50s: 68.6 and 136.6 nM) with anti-lung cancer activities. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-04396 | C-ABL/ABL1 Protein, Human, Recombinant (GST) | Human | Baculovirus-Insect Cells | ||
c-Abl belongs to the class of tyrosine kinases and is the prototype of a subfamily which includes two members, c-Abl and Arg (Abl-related gene). Both proteins are localized at the cell membrane, actin cytoskeleton and cytosol, and c-Abl is present in the nucleus as well. c-Abl is a non-receptor tyrosine kinase that participates in multiple signaling pathways linking the cell surface, cytoskeleton, and the nucleus. Recent in vitro studies have also linked c-Abl to amyloid-beta-induced toxicity and tau phosphorylation. c-Abl has been implicated in many cellular processes including differentiation, division, adhesion, death, and stress response. c-Abl is a latent tyrosine kinase that becomes activated in response to numerous extra- and intra-cellular stimuli. The c-Abl protein is a ubiquitously expressed nonreceptor tyrosine kinase involved in the development and function of many mammalian organ systems, including the immune system and bone. It regulates the cellular response to TAM through functional interaction with the estrogen receptor, which suggests c-Abl as a therapeutic target and a prognostic tumor marker for breast cancer. c-Abl also plays a key role in signaling chemokine-induced T-cell migration. In addition, c-Abl contains NLSs (nuclear localization signals) and DNA-binding sequences important for nuclear functions. c-Abl has become an important therapeutic target in human chronic myeloid leukaemia.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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TMPY-00758 | Aminopeptidase N/CD13 Protein, Mouse, Recombinant (His) | Mouse | HEK293 | ||
Aminopeptidase N (ANPEP or APN), also known as CD13, is a cell-surface metalloprotease located in the small-intestinal and renal microvillar membrane, as well as other plasma membranes. It belongs to the peptidase M1 family. CD13 plays a role in the final digestion of peptides generated from hydrolysis of proteins by gastric and pancreatic proteases and is involved in the metabolism of regulatory peptides by diverse cell types. CD13/APN is a potent regulator of angiogenesis which is essential for tumor invasion and metastasis, and its transcription in activated endothelial cells is induced by angiogenic growth factors via the RAS/MAPK pathway. In addition, this enzyme has been shown to participate in antigen processing and presentation, and accordingly, defects in this gene appear to be a cause of various types of leukemia or lymphoma and carcinomas.
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TMPY-00665 | Aminopeptidase N/CD13 Protein, Human, Recombinant (I603M, His) | Human | HEK293 | ||
Aminopeptidase N (ANPEP or APN), also known as CD13, is a cell-surface metalloprotease located in the small-intestinal and renal microvillar membrane, as well as other plasma membranes. It belongs to the peptidase M1 family. CD13 plays a role in the final digestion of peptides generated from hydrolysis of proteins by gastric and pancreatic proteases and is involved in the metabolism of regulatory peptides by diverse cell types. CD13/APN is a potent regulator of angiogenesis which is essential for tumor invasion and metastasis, and its transcription in activated endothelial cells is induced by angiogenic growth factors via the RAS/MAPK pathway. In addition, this enzyme has been shown to participate in antigen processing and presentation, and accordingly, defects in this gene appear to be a cause of various types of leukemia or lymphoma and carcinomas.
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