目录号 | 产品详情 | 靶点 | |
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T4700 | |||
1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 3.0 μM; it shows in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 valu | |||
T69815 | |||
SB-284851-BT 是一种 BRD4/p38α/BRDT 抑制剂。SB-284851-BT 抑制BRD4-BD1(IC50=1.7 µM)、p38α(Kd=0.47 nM)、BRDT(1) (IC50=18 µM) 和BRD4(1) (IC50=3.7 µM)。SB-284851-BT 通过抑制p38α以减少IL-8的产生,抑制BRD4以下调癌症的c-Myc 和NF-κB 基因通路。SB-284851-BT 能与溴结构域和超末端结构域 (BET) 结合。 | |||
T62317 | |||
α7 nAchR-JAK2-STAT3 agonist 1 是一种 α7 nAchR-JAK2-STAT3 通路的有效抑制剂,能够作用于一氧化氮 (NO) (IC50: 0.32 μM)。α7 nAchR-JAK2-STAT3 agonist 1 在小鼠巨噬细胞 RAW264.7 中对 iNOS、IL-1β 和 IL-6 的表达具有有效的抑制作用。α7 nAchR-JAK2-STAT3 agonist 1 对 LPS 诱导的 NO 释放、NF-κB 激活和细胞因子产生具有抑制作用。α7 nAchR-JAK2-STAT3 agonist 1 能够用于研究败血症。 | |||
T62239 | |||
HSR1304 (Compound 5d) 是一种 NFκB 的有效抑制剂。其中多功能转录因子核因子-κB (NF-κB) 广泛的参与多种人类疾病(如癌症、慢性炎症)。HSR1304 具有潜力进行癌症疾病的研究。 | |||
T61585 | |||
Sulindac (sodium) (MK-231) 是一种非甾体抗炎剂,具有口服活性。Sulindac (sodium) 用于减轻疼痛,肿胀和关节僵硬的关节炎。Sulindac 还用于脊柱关节炎、痛风性关节炎的研究。Sulindac (sodium) 作为一种免疫调节剂,可通过阻断 NF-κB 信号通路下调 PD-L1,调节 pMMR CRC 对抗 PD-L1 免疫治疗的应答,抑制结直肠癌 CRC 的发生发展。 Sulindac 还可通过下调 SIRT1 抑制 TGF-β1-诱导的 EMT,抑制肺癌细胞的迁移和侵袭。 | |||
T36408 | |||
Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically increasing TNF-α, IL-1β, and HMBG1 expression.2 Rhein shows efficacy against pancreatic fibrosis, chronic pancreatitis, and hyperglycemia-induced pancreatic β-cell apoptosis.3,4 It also inhibits angiogenesis of breast cancer cells under normoxic and hypoxic conditions.5 | |||
T82049 | NF-κB | ||
IR-Crizotinib是一种结合了近红外染料IR-786和Crizotinib的复合物,能穿透血脑屏障及在小鼠颅内荧光定位GBM。作为NIK抑制剂,其IC50值为3.381 μM,既能有效抑制胶质瘤细胞体外生长及侵袭,也适用于体内研究,对癌症治疗具有研究意义。 | |||
T36192 | |||
(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKK (IC50s = 80.5, 78.2, and 57.1 μM, respectively). CAY10682 blocks the growth of cancer cells in vitro (IC50s = 2-6 μM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight. | |||
T82189 | |||
HMGB1-IN-2 (compound 15) 是一种针对高度保守的核蛋白 HMGB1 的抑制剂,其在 RAW264.7 细胞中展现出 NO 抑制活性,IC50 为 20.2 μM。 HMGB1-IN-2 (30 μM) 能够减少 IL-1β、TNF-α、caspase-1 p20 的表达,并抑制 NF-κB p65 的磷酸化作用,显示出抗凋亡特性。在脓毒症急性肾损伤模型的小鼠中,HMGB1-IN-2(15 mg/kg;腹腔注射)可有效减轻肾脏伤害。此外,HMGB1-IN-2 对 Huh7 细胞和 A549 细胞的 IC50 分别为 77.0 μM 和 82.0 μM。 | |||
TN5901 | |||
Cudratricusxanthone A has potent anti-proliferative, antioxidative, and monoamine oxidase inhibitory effects, it also possesses anti-cancer activities and provide a basis for developing effective therapeutic agents to inhibit growth and metastasis of brea |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-02603 | STAT6 Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
Signal transducer and activator of transcription 6 (STAT6) is a transcription factor that is activated by interleukin-4 (IL-4)-induced tyrosine phosphorylation and mediates most of the IL-4-induced gene expression. STAT6 plays a central role in exerting interleukin-4 (IL-4) mediated biological responses and is found to induce the expression of BCL2L1/BCL-XL, which is responsible for the anti-apoptotic activity of IL4. Transcriptional activation by STAT6 requires the interaction with coactivators like p300 and the CREB-binding protein (CBP). NF-κB and tyrosine-phosphorylated Stat6 can directly bind each other in vitro and in vivo, which suggests that the direct interaction between Stat6 and NF-κB may provide a basis for synergistic activation of transcription by IL-4 and activators of NF-κB.
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TMPJ-00662 | RANKL/TNFSF11/CD254 Protein, Human, Recombinant (E. coli) | Human | E. coli | ||
CD254, also known as RANKL, TNFSF11, TRANCE, OPGL and ODF, is a type II membrane protein of the tumor necrosis factor (TNF) superfamily, and affects the immune system and control bone regeneration and remodeling. RANKL is the ligand of nuclear factor (NF)-κB (RANK). When RANKL binds to RANK, it will undergo trimerization and then bind to an adaptor molecule TNF receptor-associated factor 6 (TRAF6). This results in the activation of several downstream signaling cascades, including the NFκB, mitogen-activated protein kinases (MAPK), activating protein 1 (AP-1), and nuclear factor of activated T cells (NFATc1), resulting in the formation of multinucleated bone-resorbing osteoclasts. RANKL is widely expressed in skeletal muscle, thymus, liver, colon, small intestine, adrenal gland, osteoblast, mammary gland epithelial cells, prostate and pancreas.
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TMPJ-01466 | Osteoprotegerin Protein, Human, Recombinant (aa 22-401, His) | Human | HEK293 Cells | ||
TNFRSF11B is a secreted protein, containing 2 death domains and 4 TNFR-Cys repeats. TNFRSF11B is a decoy receptor for the receptor activator of nuclear factor kappa B ligand (RANKL). By binding RANKL, TNFRSF11B inhibits nuclear kappa B (NF-κB) which is a central and rapid acting transcription factor for immune-related genes, and a key regulator of inflammation, innate immunity, and cell survival and differentiation. TNFRSF11B levels are influenced by voltage-dependent calcium channelsCav1.2. TNFRSF11B can reduce the production of osteoclasts by inhibiting the differentiation of osteoclast precursors (osteoclasts are related to monocytes/macrophages and are derived from granulocyte/macrophage-forming colony units (CFU-GM)) into osteoclasts and also regulates the resorption of osteoclasts in vitroand in vivo. TNFRSF11B binding to RANKL on osteoblast/stromal cells, blocks the RANKL-RANK ligand interaction between osteoblast/stromal cells and osteoclast precursors. This has the effect of inhibiting the differentiation of the osteoclast precursor into a mature osteoclast.
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TMPK-00351 | RANK/TNFRSF11A Protein, Human, Recombinant (aa 30-212, hFc) | Human | HEK293 Cells | ||
TNFRSF11A, also known as receptor activator of NF-κB (RANK), activates several signaling pathways, such as NF-κB, JNK, ERK, p38α, and Akt/PKB. RANK/TNFRSF11A is a novel and frequent target for de novo methylation in gliomas, which affects apoptotic activity and focus formation thereby contributing to the molecular pathogenesis of gliomas. RANK/TNFRSF11A Protein, Human, Recombinant (aa 30-212, hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 46.85 kDa and the accession number is Q9Y6Q6-1.
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TMPK-00723 | RANK/TNFRSF11A Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
TNFRSF11A, also known as receptor activator of NF-κB (RANK), activates several signaling pathways, such as NF-κB, JNK, ERK, p38α, and Akt/PKB. RANK/TNFRSF11A is a novel and frequent target for de novo methylation in gliomas, which affects apoptotic activity and focus formation thereby contributing to the molecular pathogenesis of gliomas. RANK/TNFRSF11A Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 47.0 kDa and the accession number is O35305.
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TMPJ-00674 | RANK/TNFRSF11A Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Receptor activator of NF-κB(RANK,TNFRSF11A) belongs to one member of tumor necrosis factor receptor family.It is a receptor for TNFSF11/RANKL/TRANCE/OPGL. This gene encodes a type 1 membrane protein with a 30 amino acids (aa) signal peptide, 184 aa extracellular region , a 20 aa transmembrane domain and a 391 aa cytoplasmic region. Human and murine RANK share 81% aa identity in their extracellular domains. RANK is ubiquitous highly expressed in trabecular bone, thymus, small intestine, lung, brain and kidney, but weakly expressed in spleen and bone marrow. After binding its ligand RANKL, RANK can activate signaling pathways such as NF-κB, JNK, ERK, p38, and Akt/PKB, through TRAF protein phosphorylation. RANK/TNFRSF11A signaling is largely considered to be growth promoting and apoptosis reducing such as the effects observed in osteoclasts. RANK/TNFRSF11A was also found to be involved in the regulation of interactions between T-cells and dendritic cells.
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TMPK-00820 | AREG Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Amphiregulin (AREG) is a member of the epidermal growth factor (EGF) family and is expressed in a plethora of cancers. Tumour growth and metastasis were decreased by AREG silencing in an orthotopic model of pancreatic cancer. AREG may play a critical role in cell migration, invasion, and EMT by activating the EGFR/ERK/NF‑κB signalling pathway in pancreatic cancer cells.
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TMPY-03983 | CIRBP Protein, Human, Recombinant (His) | Human | E. coli | ||
CIRBP, also known as cold-inducible RNA-binding protein, plays a protective role in the genotoxic stress response by stabilizing transcripts of genes involved in cell survival. CIRBP responds to a wide array of cellular stresses, including short wavelength ultraviolet light (UVC), at the transcriptional and post-translational level. It acts as a translational activator.CIRBP can bind the 3 translated region of specific transcripts to stabilize them and facilitate their transport to ribosomes for translation. CIRBP affects NF-κB signaling as opposed to IL1B mRNA stability directly.
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TMPY-01710 | IkB alpha/NFKBIA Protein, Human, Recombinant (His) | Human | E. coli | ||
Nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, alpha (IkB alpha, NFKBIA, or IKBA), is a member of the NF-kappa-B inhibitor family that function to inhibit the NF-kB transcription factor. NFKBIA inhibits NF-kB by masking the nuclear localization signals (NLS) of NF-kB proteins and keeping them sequestered in an inactive state in the cytoplasm. Also, NFKBIA blocks the ability of NF-κB transcription factors to bind to DNA, which is required for NF-kB's proper functioning. Signal-induced degradation of I kappa B alpha exposes the nuclear localization signal of NF-kappa B, thus allowing it to translocate into the nucleus and activate transcription from responsive genes. An autoregulatory loop is established when NF-kappa B induces expression of the I kappa B alpha gene and newly synthesized I kappa B alpha accumulates in the nucleus where it negatively regulates NF-kappa B-dependent transcription. As part of this post-induction repression, the nuclear export signal on I kappa B alpha mediates the transport of NF-kappa B-I kappa B alpha complexes from the nucleus to the cytoplasm. Deletion of NFKBIA has an effect that is similar to the effect of EGFR amplification in the pathogenesis of glioblastoma and is associated with comparatively short survival. Polymorphisms in NFKBIA may be important in pre-disposition to and outcome after treatment, of multiple myeloma (MM). The NFKBIA gene product, IkappaBalpha, binds to NF-kappaB preventing its activation and is important in mediating resistance to apoptosis in B-cell lymphoproliferative diseases.
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TMPJ-00617 | IL-33 Protein, Rhesus macaque, Recombinant (His) | Rhesus | E. coli | ||
Interleukin-33 (IL-33) belongs to the IL-1 superfamily. IL33 is highly expressed in endothelial venules found in tonsils, Peyer patches and mesenteric lymph nodes, but almost undetectable in placenta. IL33 induces the production of T helper-2 (Th2)-associated cytokines. IL-33 is a cytokine that mediates its biological effects by binding to and signals through IL1RL1/ST2 and IL-1 Receptor Accessory Protein (IL1RAP), activating intracellular molecules in the NF-κB and MAP kinase signaling pathways that drive production of type 2 cytokines from polarized Th2 cells.
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TMPJ-00086 | CT-1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Cardiotrophin-1, also known as CT-1 and CTF1, is a member of the IL-6 superfamily. It is a sreted cytokine that is expressed in heart, skeletal muscle, prostate and ovary, and to lower levels in lung, kidney, pancreas, thymus, testis and small intestine. The protein exerts its cellular effects by interacting with the glycoprotein 130 (gp130)/leukemia inhibitory factor receptor beta (LIFR) heterodimer. In addition, CT-1 activates phosphatidylinositol 3-kinase (PI-3 kinase) in cardiac myocytes and enhances transcription factor NF-κB DNA -binding activities.
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TMPJ-00280 | TNF R1 Protein, Mouse, Recombinant | Mouse | E. coli | ||
Tumor necrosis factor receptor superfamily member 1A (Tnfrsf1a) is a member of the tumor necrosis factor receptor superfamily. Tnfrsf1a is one of the major receptors for the tumor necrosis factor-alpha. It can activate the transcription factor NF-κB, mediate apoptosis, and function as a regulator of inflammation. Antiapoptotic protein BCL2-associated athanogene 4 (BAG4/SODD) and adaptor proteins TRADD and TRAF2 have been shown to interact with this receptor, and thus play regulatory roles in the signal transduction mediated by the receptor. Germline mutations of the extracellular domains of this receptor were found to be associated with the human genetic disorder called tumor necrosis factor associated periodic syndrome (TRAPS) or periodic fever syndrome
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TMPJ-00083 | NCR3 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Natural Cytotoxicity Triggering Receptor 3 (NCR3) along with NKp44 and NKp46 constitute a group of receptors termed “Natural Cytotoxicity Receptors”. They play a major role in triggering NK-mediated killing of most tumor cells lines. NKp30 is a type I transmembrane protein having a single extracellular V-like immunoglobulin domain. NKp30 is selectively expressed both in resting and activated human NK cells. In addition, NKp30 is also involved in NK-mediated induction of dendritic cell (DC) maturation. It has been demonstrated that NK cell activation signaling specifically induces lytic activity against several tumor cell types and synthesis of new NF-κB dependent proteins during the initiation of cytotoxicity.
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TMPY-01176 | cIAP1 Protein, Human, Recombinant (Avi) | Human | E. coli | ||
The cellular inhibitor of apoptosis protein-1 (cIAP1) is a member of the Inhibitor of Apoptosis family proteins are (IAP) whose members are characterized by a novel domain of about 70 amino acids termed baculoviral IAP repeats (BIRs). The BIR domains of cIAP1 and cIAP2 bind to caspases, the key effector proteases of apoptosis. The IAP protein family which can enhance cell survival are crucial regulators of programmed cell death. Both cIAP1 and cIAP2 are the E3 ubiquitin protein isopeptide ligases for Smac, taking part in promoting cancer survival through functioning as E3 ubiquitin ligases. Removal of cIAP1 by genetic deletion may result in NF-κB signaling activation that induces TNFα production and in killing sensitive tumor cells through enhanced TNF-R1 death-receptor signaling and caspase 8 activation. The substrate-dependent E3 activity of cIAPs is mediated by their RING domains and is dependent on the specific interactions between cIAPs and Smac. cIAP1 and cIAP2 are also reported to be regulators of NF-kB activation upon TNFαtreatment.
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TMPJ-00072 | IL-18BPd Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
Interleukin 18 binding protein (IL-18BP) is a physiological inhibitor that acts through binding to the receptor-binding site of IL-18. IL-18 stimulates INF-γ, which then stimulates 18BP production via NF-κB. The interaction between IL-18 and IL-18BP has a significant role in the inflammation process. IL-18 BPs have four isoforms, a, b, c and d, which are spliced by different ways. The IL-18 BP isoforms a and c each contain one immunoglobulin (Ig)-like C2-type domain which is essential to the binding and neutralizing properties of the binding proteins. The IL-18 BP isoforms b and d lack a complete Ig domain. The expression of IL-18 and the IL-18BP are indentified in immune tissues such as the spleen, but also in nonimmune cells including keratinocytes.
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TMPJ-00060 | IL-25/IL17E Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Interleukin 25 (IL-25) belongs to the Interleukin 17 (IL-17) family of proteins, which is comprised of six members (IL-17, IL-17B through IL-17F). These proteins are secreted and are structurally related by sharing a conserved cysteine-knot fold near the C-terminus, but have considerable sequence divergence at the N-terminus. With the exception of IL-17B, which exists as a non-covalently linked dimer, all IL-17 family members are disulfide-linked dimers. IL-17 family proteins are pro-inflammatory cytokines that induce local cytokine production and are involved in the regulation of immune functions. Human interleukin-17E (IL17E), also referred to as Interleukin-25 (IL25), is a distinct member of the IL17 cytokine family comprised of at least six members sharing a conserved cysteine-knot structure but divergent at the N-terminus. IL25 is a glycoprotein secreted as dimers by innate effector eosinophils and basophils, and present at very low levels in various peripheral tissues. IL25, together with IL17B, are ligands for the cytokine receptor IL17BR, and the cross-linking induces NF-κB activation and production of the proinflammatory chemokine IL-8, as well as ERK, JNK, and p38 activation. Overexpression of IL25 gene in transgenic mice suggested that this cytokine can regulate hematopoietic and immune functions, and additionally is identified as a proinflammatory cytokine favoring Th2-type immune responses possibly by enhancing the maintenance and functions of adaptive Th2 memory cells.
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