目录号 | 产品详情 | 靶点 | |
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T14363 | Trk receptor | ||
AZ-23是一种 ATP-竞争性的,口服具有活性的 Trk 激酶 A/B/C 抑制剂,IC50值分别为2 nM (TrkA),8 nM (TrkB),24 nM (FGFR1),52 nM (Flt3),55 nM (Ret),84 nM (MuSk),99 nM (Lck)。 | |||
TQ0059 | VEGFR FLT c-RET PDGFR Aurora Kinase | ||
Ilorasertib (ABT-348) 是一种 ATP 竞争性多靶点激酶抑制剂,可抑制 Aurora A、Aurora B 和Aurora C,IC50值为120 nM、7 nM 和1 nM。它还抑制 RET 酪氨酸激酶、PDGFRβ 和 Flt1,IC50为7 nM、3 nM 和 32 nM。 | |||
T3599 | VEGFR | ||
BFH772 是 VEGFR2抑制剂(IC50:3 nM),具有口服活性。 | |||
T2288L | VEGFR c-Kit | ||
Motesanib Diphosphate (AMG 706) 是一种有效的VEGFR1/2/3的 ATP 竞争性抑制剂,IC50值为 2 nM/3 nM/6 nM,与对 Kit 的选择性相似,是 PDGFR 和 Ret 的 10 倍多。 | |||
TQ0277L | |||
Pralsetinib is a selective and next-generation RET inhibitor (IC50: 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T, and CCDC6-RET fusion). BLU-667 is an effective and selective inhibitor of RET mutations, fusions, and predicted resistant mutants. | |||
T70130 | |||
NPA101.3 is a a Second-Generation RET/VEGFR2 Inhibitor. It is a potential clinical candidate for RET-driven cancers. | |||
T39688 | |||
Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase. It demonstrates nanomolar potency against RET while exhibiting over 300-fold selectivity against VEGFR2. Zeteletinib exhibits remarkable efficacy against the wild-type RET, RET V804M/L gatekeeper mutants, as well as the frequently occurring oncogenic RET mutation M918T. Its antitumor activity is potent. | |||
T70382 | |||
KBP-7018 Hydrochloride is a novel, tyrosine kinase-selective inhibitor with potent effects on three fibrotic kinases (c-KIT, PDGFR, and RET). | |||
T39927 | |||
Zeteletinib hemiadipate (BOS-172738; DS-5010) is an orally active compound that functions as a selective inhibitor of RET kinase. It exhibits nanomolar potency against RET and a 300-fold selectivity towards VEGFR2. Notably, Zeteletinib hemiadipate demonstrates exceptional effectiveness against various forms of RET, including the wild type, RET V804M/L gatekeeper mutants, and the oncogenic RET mutation M918T. Additionally, Zeteletinib hemiadipate exerts potent antitumor effects. | |||
T78797 | |||
FHND5071为选择性RET激酶抑制剂,通过抑制RET自磷酸化以发挥抗肿瘤效应,适用于肿瘤疾病研究。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-02270 | RET Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
RET Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 69.1 kDa and the accession number is P07949-1.
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TMPY-04418 | RET Protein, Human, Recombinant (aa 658-1114, His & GST) | Human | Baculovirus Insect Cells | ||
RET Protein, Human, Recombinant (aa 658-1114, His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 76.7 kDa and the accession number is P07949-1.
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TMPJ-00290 | GFR Alpha-2/GFRA2 Protein, Human, Recombinant (hFc & His) | Human | HEK293 Cells | ||
GDNF family receptor alpha-2 is a glycosylphosphatidylinosito l (GPI)-linked cell surface receptor. It is part of the GDNF receptor family. Glial cell line-derived neurotrophic factor (GDNF) and neurturin (NTN) are two structurally related, potent neurotrophic factors that play key roles in the control of neuron survival and differentiation. GFRA2 mediates the NRTN-induced autophosphorylation and activation of the RET receptor. It also able to mediate GDNF signaling through the RET tyrosine kinase receptor. It acts preferentially as a receptor for NTN compared to its other family member, GDNF family receptor alpha 1.
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TMPH-03247 | Artemin Protein, Rat, Recombinant (His & Myc) | Rat | E. coli | ||
Ligand for the GFR-alpha-3-RET receptor complex but can also activate the GFR-alpha-1-RET receptor complex. Supports the survival of sensory and sympathetic peripheral neurons in culture and also supports the survival of dopaminergic neurons of the ventral mid-brain. Strong attractant of gut hematopoietic cells thus promoting the formation Peyer's patch-like structures, a major component of the gut-associated lymphoid tissue. Artemin Protein, Rat, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 17.1 kDa and the accession number is Q6AYE8.
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TMPH-02842 | CD133/PROM1 Protein, Mouse, Recombinant (His & SUMO) | Mouse | E. coli | ||
May play a role in cell differentiation, proliferation and apoptosis. Binds cholesterol in cholesterol-containing plasma membrane microdomains and may play a role in the organization of the apical plasma membrane in epithelial cells. During early retinal development acts as a key regulator of disk morphogenesis. Involved in regulation of MAPK and Akt signaling pathways. In neuroblastoma cells suppresses cell differentiation such as neurite outgrowth in a RET-dependent manner.
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TMPK-00109 | Artemin Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Artemin (ARTN) is a member of glial cell line-derived neurotrophic factor (GDNF) family of ligands, and its signaling is mediated via a multi-component receptor complex including the glycosylphosphatidylinositol-anchored GDNF family receptors a (GFRa1, GFRa3) and RET receptor tyrosine kinase. The major mechanism of ARTN action is via binding to a non-signaling co-receptor. The major function of ARTN is to drive the molecule to induce migration and axonal projection from sympathetic neurons.
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TMPY-04207 | Motilin Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
MLN (Motilin) is a Protein Coding gene. 3 alternatively spliced human isoforms have been reported. This gene encodes a small peptide hormone that is secreted by cells of the small intestine to regulate gastrointestinal contractions and motility. The encoded protein belongs to the motilin family. Proteolytic processing of the secreted protein produces the mature peptide and a byproduct referred to as motilin-associated peptide (MAP). MLN plays an important role in the regulation of Interdigestive Gastrointestinal Motility and indirectly causes rhythmic contraction of duodenal and colonic smooth muscle. Diseases associated with MLN include Gastroparesis and Duodenogastric Reflux. Among its related pathways are RET signaling and Signaling by GPCR.
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TMPH-00001 | CD133/PROM1 Protein-VLP, Human, Recombinant (His) | Human | HEK293 Cells | ||
May play a role in cell differentiation, proliferation and apoptosis. Binds cholesterol in cholesterol-containing plasma membrane microdomains and may play a role in the organization of the apical plasma membrane in epithelial cells. During early retinal development acts as a key regulator of disk morphogenesis. Involved in regulation of MAPK and Akt signaling pathways. In neuroblastoma cells suppresses cell differentiation such as neurite outgrowth in a RET-dependent manner. CD133/PROM1 Protein-VLP, Human, Recombinant (His) is expressed in HEK293 mammalian cells with C-10xHis tag. The predicted molecular weight is 96.7 kDa and the accession number is O43490.
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TMPJ-00100 | Artemin Protein, Human, Recombinant | Human | E. coli | ||
Human Artemin is a GDNF family ligand that is distantly related to the TGF-β superfamily of molecules. It is synthesized as a preproprotein, and contains a variable length pre-, or signal sequence, plus a 68 amino acid (aa) proregion and a 113 aa mature segment. Following synthesis and proteolytic processing, mature ARTN is secreted as a presumably glycosylated, 28 kDa disulfide-linked homodimer that contains three intrachain disulfide bonds and the typical TGF-β signature cysteine-knot motif. In the mature region, human ARTN is 89% and 88% aa identical to rat and mouse ARTN, respectively. Human ARTN is active on rodent cells. The receptor for ARTN has been identified as the ligand binding subunit GFRα-3 plus the signal transducing subunit, RET. The GFRα-1/RET receptor complex has also been suggested to be a ligand binding unit for ARTN. ARTN is known to be a chemoattractant for sympathetic neuron axons innervating the developing cardiovascular system. It also promotes sensory neuron survival and likely plays a role in the development of the peripheral nervous system. Finally, it has been reported to reverse neuropathic pain due to nerve injury, and to help resolve morphological changes associated with nerve damage.
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TMPJ-01414 | GDF-15 Protein, Mouse, Recombinant (His & Flag) | Mouse | HEK293 Cells | ||
Growth Differentiation Factor 15 (GDF-15), also called Macrophage Inhibitory Cytokine 1 (MIC-1), is a divergent member of the TGF-beta superfamily. GDF15 can be secreted by a wide variety of cell types in response to a broad range of stressors. GDF-15 expression is dramatically upregulated during acute brain injury, cancer, cardiovascular disease, and inflammation, suggesting its potential value as a disease biomarker. GDF15 was shown to inhibit proliferation of primitive hematopoietic progenitors and introduced as a putative placental mediator of embryonic development. GDF15 has recently gained scientific and translational prominence with the discovery that its receptor is a GFRAL-RET heterodimer of which GFRAL is expressed solely in the hindbrain.
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TMPJ-00688 | Persephin Protein, Human, Recombinant | Human | E. coli | ||
Persephin is a secreted protein, belongs to the glial cell linederived neurotrophic factor (GDNF) family of the TGF-β superfamily. It shares 38-46% amino acid (aa) identity with family members GDNF, neurturin and artemin. It is expressed at very low levels in most tissues. Mature protein contains a signal sequence, a pro-domain and a 96 aa mature sequence with several cysteines that are conserved among family members. It circulates as an unglycosylated disulfide-linked homodimer. Like other GDNF family members, Persephin acts through engagement of GRFα4, a glycosylphosphatidylinositol (GPI)-linked GDNF receptor family Persephin is reported to promote both the survival and growth of central dopaminergic and motor neurons, and kidney development. These effects are correlated with the expression patterns of GFRα4, and RET.
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TMPY-01576 | Artemin Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
Artemin (ARTN) is a member of glial cell line-derived neurotrophic factor (GDNF) family of ligands, and its signaling is mediated via a multi-component receptor complex including the glycosylphosphatidylinositol-anchored GDNF family receptors a (GFRa1, GFRa3) and RET receptor tyrosine kinase. The major mechanism of ARTN action is via binding to a non-signaling co-receptor. The major function of ARTN is to drive the molecule to induce migration and axonal projection from sympathetic neurons. It also promotes the survival, proliferation and neurite outgrowth of sympathetic neurons in vitro. ARTN triggers oncogenicity and metastasis by the activation of the AKT signaling pathway. Recent studies have reported that the expression of ARTN in hepatocellular carcinoma is associated with increased tumor size, quick relapse and shorter survival. Furthermore, ARTN promotes drug resistance such as antiestrogens, doxorubicin, fulvestrant, paclitaxel, tamoxifen and trastuzumab. Moreover, ARTN also stimulates the radio-therapeutic resistance. Hypoxia has been reported to regulate the cancer stem cell (CSC) population yet the underlying mechanism is poorly characterized. Artemin (ARTN) is a member of the glial cell derived neurotrophic factor family of ligands, is a hypoxia-responsive factor and is essential for hypoxia-induced CSC expansion in hepatocellular carcinoma (HCC). Clinically, elevated expression of ARTN in HCC was associated with larger tumor size, faster relapse and shorter survival. In vitro, HCC cells with forced expression of ARTN exhibited reduced apoptosis, increased proliferation, epithelial-mesenchymal transition (EMT) and enhanced motility. Additionally, ARTN dramatically increased xenograft tumor size and metastasis in vivo. Moreover, ARTN also enhanced tumorsphere formation and the tumor initiating capacity of HCC cells, consequent to expansion of the CD133+ CSC population. ARTN transcription was directly activated by hypoxia-induced factor-1α (HIF-1α) and hypoxia induced ARTN promoted EMT and increased the CSC population via AKT signaling.
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