目录号 | 产品详情 | 靶点 | |
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T73479 | |||
JA2131为一种小分子PARG抑制剂,具有靶向性(IC50=0.4 μM)。该化合物通过调节DNA损伤反应,能引起复制叉停止以及癌细胞的死亡。 | |||
T68536 | |||
WP-1034 is a novel Jak-Stat inhibitor, which is active against AML blasts. WP-1034 effectively inhibited proliferation of OCIM2 cells and fresh AML samples. WP-1034 caused cell cycle arrest of OCIM2 cells in sub-Go phase. WP-1034 induced apoptosis of OCIM2 cells and that induction of apoptosis involved cleavage of caspase 3 and the DNA repair enzyme poly (adenosine diphosphate [ADP]-ribose) polymerase (PARP). | |||
T79608 | JAK | ||
DPP,一种含紫檀芪衍生轴向配体的铂(IV)络合物,能够抑制乳腺癌(BC)细胞的JAK2-STAT3通路并显示出抗增殖特性。它通过激活caspase-3和裂解聚ADP-核糖聚合酶诱导细胞凋亡(apoptosis),同时促进树突状细胞成熟及抗原呈现功能,并已证明体内具有安全性。 | |||
T36703 | |||
CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bagnolini, G., Milano, D., Manerba, M., et al.Synthetic lethality in pancreatic cancer: Discovery of a new RAD51-BRCA2 small molecule disruptor that inhibits homologous recombination and synergizes with olaparibJ. Med. Chem.63(5)2588-2619(2020) | |||
TN4046 | MMP FAK PARP GSK-3 NF-κB Wnt/beta-catenin Akt Caspase PI3K Prostaglandin Receptor JNK | ||
ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP). | |||
T74510 | |||
TFMU-ADPr作为监测聚ATP-核糖糖水解酶(PARG)活性的底物,以其释放的荧光团直接反映PAR水解酶总活性而常用。该化合物因具备优良的反应性、通用性、稳定性及易用性,成为体外评估小分子抑制剂及研究ATP-核糖基分解代谢酶调控的首选工具。 | |||
T70039 | |||
BIM-46174 is a New Inhibitor of the Heterotrimeric Gα/Gβγ Protein Complex. BIM-46174 acts as a selective inhibitor of heterotrimeric G-protein complex. BIM-46174 prevents the heterotrimeric G-protein signaling linked to several GPCRs mediating (a) cyclic AMP generation (Gαs), (b) calcium release (Gαq), and (c) cancer cell invasion by Wnt-2 frizzled receptors and high-affinity neurotensin receptors (Gαo/i and Gαq). BIM-46174 inhibits the growth of a large panel of human cancer cell lines, including anticancer drug-resistant cells. Exposure of cancer cells to BIM-46174 leads to caspase-3-dependent apoptosis and poly(ADP-ribose) polymerase cleavage. | |||
T75074 | |||
6-Methoxypurine-9-β-D-5’(R)-C-methylriboside 是一种嘌呤碱基,属于次黄嘌呤似物,主要在肌肉组织中发现。作为黄嘌呤在嘌呤氧化酶作用下的代谢产物,次黄嘌呤具备显著的抗炎性质,并可作为内源性 poly(ADP-ribose) polymerase (PARP) 的抑制剂。其通过抑制 PARP 活性,防止过氧亚硝酸盐引起的线粒体去极化及次级超氧化物的产生,展现出细胞保护作用。同时,次黄嘌呤也被用作缺氧的生物标志物。 | |||
T72017 | |||
6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimental autoimmune encephalomyelitis (EAE). It also decreases serum levels of lactate dehydrogenase as well as hepatic lipid peroxidation, oxidative DNA damage, and PARP levels. | |||
T74511 | |||
TFMU-ADPr triethylamine 作为监测聚 ATP-核糖糖水解酶 (PARG) 活性的标准底物,能够通过释放荧光团直接报告 PAR 水解酶的总活性。其特点包括高反应性、广泛的通用性、稳定性以及便于使用,使其成为体外评估小分子抑制剂以及研究 ATP-核糖基分解代谢酶调控的优选工具。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-01188 | PARP Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
PARP Protein, Human, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 114.5 kDa and the accession number is A0A024R3T8.
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TMPY-02465 | PARP Protein, Mouse, Recombinant (His) | Mouse | Baculovirus Insect Cells | ||
PARP Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 115 kDa and the accession number is Q921K2.
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TMPY-02421 | PARP3 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
Poly(ADP-ribose) polymerase 3 (PARP3) is an important member of the PARP family and shares high structural similarities with both PARP1 and PARP2. Poly(ADP-ribose) polymerase 3 (PARP3), a critical player in cellular response to DNA double-strand breaks (DSBs), plays an essential role in the maintenance of genome integrity. The ADP ribosyl transferase [poly(ADP-ribose) polymerase] ARTD3(PARP3) is a newly characterized member of the ARTD(PARP) family that catalyzes the reaction of ADP ribosylation, a key posttranslational modification of proteins involved in different signaling pathways from DNA damage to energy metabolism and organismal memory.
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TMPH-01091 | CHD1L Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
DNA helicase which plays a role in chromatin-remodeling following DNA damage. Targeted to sites of DNA damage through interaction with poly(ADP-ribose) and functions to regulate chromatin during DNA repair. Able to catalyze nucleosome sliding in an ATP-dependent manner. Helicase activity is strongly stimulated upon poly(ADP-ribose)-binding. CHD1L Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 37.3 kDa and the accession number is Q86WJ1.
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TMPY-02831 | Caspase-7 Protein, Human, Recombinant (His) | Human | E. coli | ||
Caspase 7, also known as caspase-7 and MCH3, belongs to the cysteine-aspartic acid protease (caspase) family. Caspases play a role in the signal transduction pathways of apoptosis, necrosis and inflammation. There are two major classes of caspases: initiators and effectors. The initiator isoforms (caspases-1,-4,-5,-8,-9,-10,-11,-12) are activated by, and interact with, upstream adaptor molecules through protein-protein interaction domains known as CARD and DED. Effector caspases (-3,-6,-7) are responsible for cleaving downstream substrates and are sometimes referred to as the executioner caspases. Caspase 7 exists in lung, skeletal muscle, liver, kidney, spleen, heart, and moderately in testis. Caspase 7 cannot be detected in the brain. Caspase 7 functions in the activation cascade of caspases responsible for apoptosis execution. It cleaves and activates sterol regulatory element binding proteins (SREBPs). It proteolytically cleaves poly(ADP-ribose) polymerase (PARP) at a '216-Asp- -Gly-217' bond. Overexpression promotes programmed cell death.
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