目录号 | 产品详情 | 靶点 | |
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T60365 | |||
SY-LB-35 是骨形态发生蛋白 (BMP) 受体的有效激动剂。SY-LB-35 可以刺激 C2C12 成肌细胞系中细胞数量和细胞活力的显著增加,并引起细胞周期向 S 期和 G2/M 期转变。SY-LB-35 刺激典型的 Smad 和非典型的 PI3K/Akt、ERK、p38和 JNK 胞内信号通路。 | |||
TN4263 | MMP GSK-3 NF-κB ROS Akt PI3K CDK JNK | ||
Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Isoangustone A dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-κB signaling. Isoangustone A also shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals. | |||
T70058 | |||
PQR514 is a potent pan-PI3K inhibitor (Ki 110alpha =2.2 nM). PQR514 is a follow-up compound for the phase-II clinical compound PQR309. PQR514 has an improved potency both in vitro and in cellular assays with respect to its predecessor compounds. It shows superiority in the suppression of cancer cell proliferation and demonstrates significant antitumor activity in an OVCAR-3 xenograft model at concentrations approximately eight times lower than PQR309 | |||
T61476 | |||
Thioridazine is a chemical compound characterized by its potent anti-psychotic and anti-anxiety activities. As an antagonist of the dopamine receptor D2 family proteins, it exhibits a strong inhibitory effect on the PI3K-Akt-mTOR signaling pathways, resulting in anti-angiogenic effects. It also demonstrates significant antiproliferative and apoptosis induction effects in a diverse range of cancer cells, specifically targeting cancer stem cells (CSCs) [1] [2] [3] [4]. | |||
T71284 | |||
Glimepiride urethane is a third generation sulfonylurea compound, which increases the release of insulin from pancreatic beta cells. In addition, glimepiride increases the activity of intracellular insulin receptors. Glimepiride increases osteoblast proliferation and differentiation, which is thought to be related to its ability to activate the PI3K and Akt pathway. Furthermore, Glimepiride enhances intrinsic peroxisome proliferator-activated receptor γ activity. Glimepiride also increases protein expression of glucose transports 1 and 4, and is a potent KIR channel blocker. | |||
T77629 | PI3K mTOR | ||
FD274 是一种高效的 PI3K/mTOR 双重抑制剂,对 PI3Kα/β/γ/δ 和 mTOR 具有抑制作用, IC50 分别为 0.65 nM、1.57 nM、0.65 nM、0.42 nM 和 2.03 nM。 FD274 在 AML 细胞系抗增殖实验中显示出显着的抗增殖活性。 FD274 在 HL-60 异种移植模型中表现出剂量依赖性的坑肿瘤生长活性。 FD274具有用于急性髓系白血病研究的潜力。 | |||
TP2097 | |||
Potent, high affinity apelin receptor agonist (IC50 = 0.27 nM; Kd = 0.51 nM). Exhibits no binding GPR15 and GPR25. Activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. Also potentiates the T | |||
T68477 | |||
XL-418 is a selective, orally active small molecule, targeting protein kinase B (PKB or AKT) and ribosomal protein S6 Kinase (p70S6K), with potential antineoplastic activity. XL418 inhibits the activities of PKB and p70S6K, both acting downstream of phosphoinosotide-3 kinase (PI3K). These kinases are often upregulated in a variety of cancers. Inhibition of PKB by this agent will induce apoptosis, while inhibition of p70S6K will result in the inhibition of translation within tumor cells. | |||
T38263 | |||
TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IKKε-IN-4 (Compound II; 0-2 μM; 30 minutes; HCC44 cells) treatment inhibits the AKT activity[1].TBK1/IKKε-IN-4 (Compound II) inhibits LPS-induced expression of IFNβ (IC50 =62 nM), and the IFNβ target genes IP10 (IC50 =78 nM) and Mx1 (IC50=20 nM). TBK1/IKKε-IN-4 effectively blocksTLR3-dependent IRF3 nuclear translocation in cells with an IC50 under 100 nM, but does not impair TNFR1-dependent p65 NFκB nuclear translocation with doses as high as 20 μM[1]. [1]. Ou YH, et al. TBK1 directly engages Akt/PKB survival signaling to support oncogenic transformation. Mol Cell. 2011 Feb 18;41(4):458-70. | |||
T8996 | |||
AQX-016A 是一种口服有效的 SHIP1激动剂。AQX-016A 是 Pelorol 的结构类似物,在相同摩尔浓度下,其效力是海洋天然产物 Pelorol 的 3 倍。AQX-016A 可以在体外激活重组 SHIP1酶并刺激 SHIP1活性。AQX-016A 还可抑制 PI3K 通路和 TNFa 的产生,可用于各种炎症疾病的研究。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPJ-00059 | IL-7 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Human Interleukin 7 (IL-7) is a potent lymphoid cell growth factor stimulating the proliferation of lymphoid progenitors. IL7 can associate with the hepatocyte growth factor (HGF) to form a hybrid cytokine that functions as a pre-pro-B cell growth-stimulating factor. Human IL7 cDNA encodes a 177 amino acid precursor protein containing a 25 amino acid signal peptide and a 152 amino acid mature protein. Human and mouse IL7 share 65% sequence identity in the mature region and both exhibit cross-species activity. IL-7 signals via IL-7 receptor (IL7R) activating multiple pathways including JaK/STAT and PI3K/AKT, which regulate lymphocyte survival, glucose uptake, proliferation, and differentiation. IL-7 is also associated with cytoplasmic IL2-R gamma for signal transduction.
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TMPK-01034 | SEMA4B Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Semaphorin 4B (SEMA4B) inhibits the invasion of non-small cell lung cancer (NSCLC) through PI3K-dependent suppression of MMP9 activation. SEMA4B may induce FoxO1 nuclear retention through suppressing PI3K/Akt signaling pathway, which subsequently inhibited cell growth through the direct nuclear target of FoxO1, p21. A role of SEMA4B in suppressing NSCLC growth, besides its role in inhibiting cell metastasis, and highlights SEMA4B as a promising therapeutic target for NSCLC.
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TMPH-01348 | FSHR Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
G protein-coupled receptor for follitropin, the follicle-stimulating hormone. Through cAMP production activates the downstream PI3K-AKT and ERK1/ERK2 signaling pathways. FSHR Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with N-6xHis tag. The predicted molecular weight is 43.5 kDa and the accession number is P23945.
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TMPH-03365 | REG3A Protein, Rat, Recombinant (E.coli, His) | Rat | E. coli | ||
Bactericidal C-type lectin. Regulates keratinocyte proliferation and differentiation after skin injury via activation of EXTL3-PI3K-AKT signaling pathway. REG3A Protein, Rat, Recombinant (E.coli, His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 20.5 kDa and the accession number is P35231.
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TMPH-01347 | FSHR Protein, Human, Recombinant (E. coli, His) | Human | E. coli | ||
G protein-coupled receptor for follitropin, the follicle-stimulating hormone. Through cAMP production activates the downstream PI3K-AKT and ERK1/ERK2 signaling pathways. FSHR Protein, Human, Recombinant (E. coli, His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 44.0 kDa and the accession number is P23945.
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TMPK-00136 | ULBP-2 Protein, Human, Recombinant (His & Avi) | Human | HEK293 Cells | ||
ULBPs activate multiple signaling pathways in primary NK cells, resulting in the production of cytokines and chemokines. Binding of ULBPs ligands to NKG2D induces calcium mobilization and activation of the JAK2, STAT5, ERK and PI3K kinase/Akt signal transduction pathway, mediating natural killer cell cytotoxicity.
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TMPH-02538 | Beclin-1 Protein, Mouse, Recombinant (His & SUMO) | Mouse | E. coli | ||
Plays a central role in autophagy. Acts as core subunit of different PI3K complex forms that mediate formation of phosphatidylinositol 3-phosphate and are believed to play a role in multiple membrane trafficking pathways: PI3KC3-C1 is involved in initiation of autophagosomes and PI3KC3-C2 in maturation of autophagosomes and endocytosis. Involved in regulation of degradative endocytic trafficking and required for the abcission step in cytokinesis, probably in the context of PI3KC3-C2. Essential for the formation of PI3KC3-C2 but not PI3KC3-C1 PI3K complex forms. Involved in endocytosis including endosome formation in neuronal cells. May play a role in antiviral host defense.; Beclin-1-C 35 kDa localized to mitochondria can promote apoptosis; it induces the mitochondrial translocation of BAX and the release of proapoptotic factors.
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TMPH-02019 | REG3A Protein, Human, Recombinant (GST) | Human | E. coli | ||
Bactericidal C-type lectin which acts exclusively against Gram-positive bacteria and mediates bacterial killing by binding to surface-exposed carbohydrate moieties of peptidoglycan. Regulates keratinocyte proliferation and differentiation after skin injury via activation of EXTL3-PI3K-AKT signaling pathway. REG3A Protein, Human, Recombinant (GST) is expressed in E. coli expression system with N-GST tag. The predicted molecular weight is 43.6 kDa and the accession number is Q06141.
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TMPK-00524 | CA9/Carbonic Anhydrase IX Protein, Cynomolgus, Recombinant (His) | Cynomolgus | HEK293 Cells | ||
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. CA9/Carbonic Anhydrase IX Protein, Cynomolgus, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 41.03 kDa and the accession number is A0A2K5VQG9.
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TMPJ-01271 | PIK3IP1 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Phosphoinositide-3-kinase-interacting protein 1(PIK3IP1) is an enzyme that in humans is encoded by the PIK3IP1 gene.It is a negative regulator of phosphatidylinositol-3-kinase (PI3K), suppresses the development of hepatocellular carcinoma. The gene encoding PIK3IP1 maps to human chromosome 22, which houses over 500 genes and is the second smallest human chromosome. Mutations in several of the genes that map to chromosome 22 are involved in the development of Phelan-McDermid syndrome, Neurofibromatosis type 2, autism and schizophrenia.
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TMPK-00283 | CA9/Carbonic Anhydrase IX Protein, Human, Recombinant (His & Avi) | Human | HEK293 Cells | ||
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. CA9/Carbonic Anhydrase IX Protein, Human, Recombinant (His & Avi) is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 43.7 kDa and the accession number is Q16790.
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TMPJ-00352 | CD98 Protein, Human, Recombinant (mFc) | Human | HEK293 Cells | ||
CD98 is a multifunctional glycoprotein that is involved in various biological processes such as amino acid transport, cell adhesion, diffusion, adhesion, and proliferation. CD98 can interact with CD147 to induce integrin 1 function to promote cyclosporine B-induced cell adhesion and p44/p42 MAPK activation following PI3K activation. CD98 heavy chain has been studied to be a key player in tumorigenesis due to its role in activating integrin signaling to promote tumor progression via angiogenesis, invasiveness, and proliferation in addition to promoting malignant transformation of cells. Fibrotic progression in the liver could be linked to the activation of integrin αvβ1 via CD98. CD98’s role in T cell activation in which the TGF activation could also play a profibrotic role.
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TMPJ-00181 | PD-1 Protein, Human, Recombinant (His & Avi), Biotinylated | Human | HEK293 Cells | ||
Programmed cell death protein 1(PDCD1) is a single-pass type I membrane protein and contains 1 Ig-like V-type domain. PD-1 is a member of the extended CD28/CTLA-4 family of T cell regulators. PDCD1 inhibits the T-cell proliferation and production of related cytokines including IL-1, IL-4, IL-10 and IFN-γ by suppressing the activation and transduction of PI3K/AKT pathway. In addition, coligation of PDCD1 inhibits BCR-mediating signal by dephosphorylating key signal transducer. PDCD1 has been suggested to be involved in lymphocyte clonal selection and peripheral tolerance, and thus contributes to the prevention of autoimmune diseases. As a cell surface molecule, PDCD1 regulates the adaptive immune response. Engagement of PD-1 by its ligands PD-L1 or PD-L2 transduces a signal that inhibits T-cell proliferation, cytokine production, and cytolytic function.
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TMPY-05250 | CLEC3A Protein, Mouse, Recombinant (His) | Mouse | Baculovirus Insect Cells | ||
C-type lectin domain family 3 member A (CLEC3A) is a poorly characterized protein belonging to the superfamily of C-type lectins. Elevated CLEC3A expression may correlate with breast IDC metastatic potential and indicated a poor prognosis in breast IDC. CLEC3A knockdown inhibited BC cell growth and metastasis might be through suppressing PI3K/AKT signaling activity. That CLEC3A is a promising therapeutic target for BC in the future. Matrilysin (MMP-7) plays important roles in tumor progression. Previous studies have suggested that MMP-7 binds to tumor cell surface and promotes their metastatic potential. C-type lectin domain family 3 member A (CLEC3A) as a membrane-bound substrate of MMP-7. CLEC3A binds to heparan sulfate proteoglycans on cell surface, leading to the enhancement of cell adhesion to integrin ligands on ECM. It can be speculated that the cleavage of CLEC3A by MMP-7 weakens the stable adhesion of tumor cells to the matrix and promotes their migration in tumor microenvironments.
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TMPY-03795 | EIF5A2 Protein, Human, Recombinant (His) | Human | E. coli | ||
Eukaryotic translation initiation factor 5A2 (EIF5A2) has been demonstrated to be upregulated in numerous types of human cancer and is associated with cancer progression. Silencing of EIF5A2 in the NSCLC cells resulted in the downregulation of the tumorigenic proteins, apoptosis regulator Bcl-2 and myc proto-oncogene protein, and upregulation of E-cadherin, suggesting that EIF5A2 promotes proliferation and metastasis through these proteins. EIF5A2 may therefore serve as a novel therapeutic target for the treatment of NSCLC. EIF5A2 might be a novel therapeutic target for the inhibition of NPC progress. EIF5A2 overexpression may contribute to cancer progression and poor prognosis, it could be a novel potential prognostic marker for FIGO stage I-II cervical cancer. EIF5A2 upregulation plays an important oncogenic role in gastric cancer. EIF5A2 may represent a new predictor for poor survival and is a potential therapeutic target for gastric cancer. The eukaryotic initiation factor 5A2 (EIF5A2) over-expression enhances HCC cell metastasis. EIF5A2, as a target of PI3K/Akt, promotes melanoma cell invasion and may serve as a promising prognostic marker and a potential therapeutic target for melanoma.
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