目录号 | 产品详情 | 靶点 | |
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T78816 | NF-κB | ||
Anti-osteoporosis agent-4 (Compound 11h) 在生物医学领域中表现为有效抑制原代破骨细胞的分化,减弱RANKL诱导的破骨细胞生成,并展示出强抑制作用,具有 IC50 值为358.29 nM。此外,该化合物还能抑制关键的 PI3K/AKT 和 IκBα/NF-κB 信号通路激活,表明其在防治骨质疏松症中的潜在应用价值。 | |||
T6143L | |||
PI-103 Hydrochloride 是一种有效的PI3K 和mTOR 双重抑制剂,抑制p110α,p110β,p110δ,p110γ,mTORC1和mTORC2,IC50分别为 8 nM,88 nM,48 nM,150 nM,20 nM 和 83 nM。PI-103 Hydrochloride 也可抑制DNA-PK,IC50为 2 nM。PI-103 Hydrochloride 诱导细胞自噬 (autophagy)。 | |||
TN3655 | ERK TNF ROS Akt PI3K PKC PPAR | ||
Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/2, PI3K, and PKC are involved in this effect.Cimiside E may be an effective chemopreventive agen | |||
T79971 | Apoptosis | ||
Asparanin A 是一种具有抗癌活性的凋亡 (apoptosis) 诱导剂。它能够通过线粒体和 PI3K/AKT 信号通路使细胞周期在 G0/G1 期停滞,并有效抑制癌细胞生长。此外,Asparanin A 在小鼠Ishikawa子宫内膜癌异种移植模型中显示出显著的体内抑制肿瘤生长效力。 | |||
T36641 | |||
RAS inhibitor Abd-7 is a powerful compound (Kd=51 nM) that binds to RAS and inhibits the protein-protein interaction (PPI) between RAS and its effectors. By interacting with RAS within cells, RAS inhibitor Abd-7 hinders RAS-effector interactions and suppresses endogenous RAS-dependent signaling. Additionally, RAS inhibitor Abd-7 disrupts the PPI of different mutant KRAS proteins with PI3K, CRAF, RALGDS, as well as NRAS Q61H and HRAS G12V[1]. | |||
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。 | |||
T76052 | |||
ELA-32(human) TFA is a potent, high affinityapelin receptoragonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells. | |||
T36308 | |||
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy[1]. PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively[1].PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells with IC50s of 7.8 nM and 8.7 nM, respectively[1]. In rats, PF-06843195 can rapidly and quantitatively transform from PF-06862309[1].PF-06843195 exhibits oral bioavailability (rat 25 %) following oral administration (rat 10 mg/kg)[1].PF-06843195 exhibits a moderate half-life (rat 3.6 h) due to high plasma clearance (30 mL/min/kg) combined with large volumes of distribution (3.0 L/kg) following intravenous administration (rat 2 mg/kg)[1]. [1]. Hengmiao Cheng, et al. Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195). J Med Chem. 2021 Jan 14;64(1):644-661. | |||
TN4213 | ERK EGFR IL Receptor NF-κB Akt PI3K Antifection mTOR p53 Autophagy | ||
Hirsutenone has potent antioxidant activity, it shows significant free radical scavenging activity and exhibits inhibition effect on the mitochondrial lipid peroxidation.Hirsutenone exhibits anti-cancer, and anti-filarial effects, it may exert a preventive effect against microbial endotoxin lipopolysaccharide-induced inflammatory skin diseases through inhibition of ERK pathway-mediated NF-kappaB activation. Hirsutenone attenuates adipogenesis by directly targeting PI3K and ERK during MCE in 3T3-L1 preadipocytes, underscoring the potential therapeutic application of Hirsutenone in preventing obesity. | |||
T71827 | |||
(rac)-AG-205 是一种对孕激素受体膜组分1 (Pgrmc1) 的有效抑制剂,并能诱导参与甾醇合成的基因表达,这些基因涉及 INSIG1 蛋白与 PGRMC1 形成复合物的过程。(rac)-AG-205 能够抑制 NF-kB 信号及 BDNF/PI3K/AKT 通路的活化,从而防止神经元对缺氧缺血状况的抵抗。 |
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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