目录号 | 产品详情 | 靶点 | |
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T79557 | Apoptosis | ||
fac-[Re(CO)3(L6)(H2O)][NO3](compound 6)是一种具有针对线粒体功能失调的抗癌活性的铼(I)三羰基水配合物。该化合物对前列腺癌细胞展现出显著的细胞毒性,具有50 nM的IC50值(PC-3细胞)。fac-[Re(CO)3(L6)(H2O)][NO3]能够主要集中在细胞核,抑制PC3细胞的ATP生成并诱导细胞凋亡,而不触发坏死、焦亡或自噬过程。 | |||
T41297 | |||
Lometrexol hydrate (DDATHF hydrate) 是一种抗嘌呤类抗叶酸 (antifolate) 药,可抑制甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 的活性,但不会诱导可检测水平的 DNA 链断裂。Lometrexol hydrate 可以进一步抑制嘌呤从头合成,引起异常的细胞增殖和凋亡,甚至细胞周期停滞。Lometrexol hydrate 具有抗癌活性。Lometrexol hydrate 还是一种有效的人丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。 | |||
T83774 | |||
Shepherdin是人体survivin的79-87氨基酸对应的合成肽,也是survivin与heat shock protein 90 (Hsp90)之间蛋白质-蛋白质相互作用的抑制剂。它以浓度依赖的方式与Hsp90的N末端结构域结合,并在150 µM的浓度下抑制了在分离的人源网状红细胞提取物中重组人survivin与Hsp90之间的相互作用。结合了穿膜肽penetratin或HIV Tat序列的Shepherdin肽结合物,体内外具有抗癌活性。 | |||
T61369 | |||
p53 Activator 2 (compound 10ah) 插入DNA,导致显著的DNA双链断裂。该化合物通过增加p53、p-p53、CDK4、p21的表达,使细胞周期在G2/M期停滞,诱导细胞凋亡,并显著降低抗凋亡蛋白Bcl-2、Bcl-xL和cyclin B1的水平。此外,p53 Activator 2表现出对MGC-803细胞的抗增殖效果,其IC50为1.73 μM,且在MGC-803异种移植肿瘤模型中展示出有效的抗癌活性。 | |||
T73581 | |||
HI5 是一种有效的微管蛋白 (tublin)和IDO 抑制剂,对 HeLa 细胞的IC50为 70 nM。HI5 抑制IDO 的表达,减少犬尿氨酸的产生,从而刺激 T 细胞活化和增殖。HI5 对 HeLa 细胞可抑制微管蛋白聚合和细胞迁移,引起 G2/M 期阻滞,同时通过线粒体依赖性凋亡途径诱导细胞凋亡 (apoptosis) 并引起反应性氧化应激。HI5 可用于抗癌研究。 | |||
T78875 | Mitochondrial Metabolism | ||
BTM-3528是一种线粒体蛋白酶OMA1的激活剂,能够过度激活线粒体整合应激反应(ISR)。该化合物促进了OMA1依赖的DELE1和OPA1的裂解,导致线粒体断裂。此外,BTM-3528通过激活eIF2α激酶HRI,引发细胞生长停滞及apoptosis。在多种DLBCL细胞系中表现出抗癌活性,且在异种移植人DLBCL SU-DHL-10细胞小鼠模型中显示出明显的体内抑制作用。 | |||
T83876 | |||
L-抗坏血酸6硬脂酸酯是L-抗坏血酸与硬脂酸的衍生物,在K. coccinea中发现,具有抗氧化和抗癌作用。在细胞外试验中清除DPPH(IC50 = 3.31 µg/ml)。包裹L-抗坏血酸6硬脂酸酯的脂质纳米颗粒(LNPs)在190 µM浓度下诱导HL-60前髓母细胞凋亡。含有L-抗坏血酸6硬脂酸酯的配方已用于化妆品和个人护理产品中。 | |||
T83922 | |||
Pep2 peptide是一种针对跨膜糖蛋白CD36的肽配体,CD36也被称为清道夫受体B2。在1 mM浓度使用时,Pep2 peptide在无细胞检测中选择性地与CD36结合,相比于人血清白蛋白(HSA)、IgG和CD44具有更高的亲和力。与不含Pep2 peptide的胶束相比,包裹抗癌剂多柔比星的Pep2 peptide功能化胶束能增加多柔比星在过表达CD36的HepG2肝细胞癌细胞中的细胞内输送,并提升细胞毒性。 | |||
T78871 | |||
PLM-101是一种口服抗癌剂,针对FLT3和RET具有选择性抑制作用,有效抑制急性髓系白血病(AML)细胞。通过抑制RET,PLM-101促使FLT3的自噬降解,并且通过抑制PI3K和Ras/ERK信号通路来发挥其抗白血病的活性。在小鼠MV4-11侧翼异种移植模型中,PLM-101以口服剂量3及10 mg/kg显示出抗肿瘤效果,并且在同种异种移植小鼠模型中,剂量为40 mg/kg(口服)亦展现出明显的抗肿瘤功效。 | |||
T79558 | |||
fac-[Re(CO)3(L3)(H2O)][NO3](简称compound 3),是一种与线粒体功能障碍相关的抗前列腺癌剂。这种铼(I)三羰基水配合物对前列腺癌细胞系(PC-3)表现出显著的细胞毒性,其IC50值为0.32 μM。研究表明,fac-[Re(CO)3(L3)(H2O)][NO3]主要在线粒体中积聚,能够降低PC-3细胞的ATP生成,进而触发细胞副凋亡(paraptosis)机制,而不通过引发坏死、凋亡或自噬途径作用。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-05033 | 5T4/TPBG Protein, Human, Recombinant (aa 60-345, His) | Human | HEK293 Cells | ||
Trophoblast glycoprotein (TPBG), also known as 5T4, is the therapeutic target of several anticancer agents currently in clinical development, largely due to its high expression in tumors and low expression in normal adult tissues. 5T4/TPBG Protein, Human, Recombinant (aa 60-345, His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 33.1 kDa and the accession number is Q13641.
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TMPY-04644 | PDGFB Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
Platelet-derived growth factor-B (PDGFB) is necessary for normal cardiovascular development. The administration of PDGFB alone normalized tumor vasculature by increasing periendothelial coverage and vascular functionality. Interestingly, this effect exerted by PDGFB was also observed in the presence of DAPT. So PDGFB is able to improve tumor vascularity and allows the anticancer action of DAPT in the tumor. PDGFB Protein, Human, Recombinant (His) is expressed in yeast with His tag. The predicted molecular weight is 14.3 kDa and the accession number is P01127-2.
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TMPY-06214 | 5T4/TPBG Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
Trophoblast glycoprotein (TPBG), also known as 5T4, is the therapeutic target of several anticancer agents currently in clinical development, largely due to its high expression in tumors and low expression in normal adult tissues. 5T4/TPBG Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 62.5 kDa and the accession number is Q9Z0L0.
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TMPY-06191 | 5T4/TPBG Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Trophoblast glycoprotein (TPBG), also known as 5T4, is the therapeutic target of several anticancer agents currently in clinical development, largely due to its high expression in tumors and low expression in normal adult tissues. 5T4/TPBG Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 37.2 kDa and the accession number is Q9Z0L0.
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TMPK-01310 | Syndecan-1 Protein, Rabbit, Recombinant (His) | Rabbit | HEK293 Cells | ||
CD138 (syndecan-1, Sdc-1) is a member of the syndecan family that comprises heparan sulfate proteoglycans. CD138 is significant for cell-cell and cell-matrix interactions.CD138 plays a crucial role in carcinogenesis and is an attractive target for anticancer treatment with heparanase inhibitors and anti-CD138 antibodies for immunotherapy.
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TMPY-06317 | 5T4/TPBG Protein, Human, Recombinant (aa 1-355, His) | Human | HEK293 Cells | ||
Trophoblast glycoprotein (TPBG), also known as 5T4, is the therapeutic target of several anticancer agents currently in clinical development, largely due to its high expression in tumors and low expression in normal adult tissues. 5T4/TPBG Protein, Human, Recombinant (aa 1-355, His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 36.15 kDa and the accession number is NP_006661.1.
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TMPK-00721 | CX3CL1/Fractalkine Protein, Mouse, Recombinant (His & Avi), Biotinylated | Mouse | HEK293 Cells | ||
Fractalkine/CX3C chemokine ligand 1 (CX3CL1) is a chemokine involved in the anticancer function of lymphocytes-mainly NK cells, T cells and dendritic cells. Its increased levels in tumors improve the prognosis for cancer patients, although it is also associated with a poorer prognosis in some types of cancers, such as pancreatic ductal adenocarcinoma.
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TMPY-05077 | PDGFB Protein, Rhesus, Recombinant (His) | Rhesus | P. pastoris (Yeast) | ||
Platelet-derived growth factor-B (PDGFB) is necessary for normal cardiovascular development. The administration of PDGFB alone normalized tumor vasculature by increasing periendothelial coverage and vascular functionality. Interestingly, this effect exerted by PDGFB was also observed in the presence of DAPT. So PDGFB is able to improve tumor vascularity and allows the anticancer action of DAPT in the tumor. PDGFB Protein, Rhesus, Recombinant (His) is expressed in yeast with His tag. The predicted molecular weight is 14.2 kDa and the accession number is A0A1D5Q4I7.
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TMPK-00060 | IL-17B Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
IL-17A, the prototypic member of the IL-17 family, several experimental findings strongly support the role of the IL-17B/IL-17 receptor B (IL-17RB) pathway in tumorigenesis and resistance to anticancer therapies. IL-17B/IL-17RB expression patterns and biological activities in cancer and highlight issues that remain to be addressed to better characterize IL-17B and its receptor as potential targets for enhancing the effectiveness of the existing cancer therapies.
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TMPY-04877 | PDGFB Protein, Mouse, Recombinant (His) | Mouse | P. pastoris (Yeast) | ||
Platelet-derived growth factor-B (PDGFB) is necessary for normal cardiovascular development. The administration of PDGFB alone normalized tumor vasculature by increasing periendothelial coverage and vascular functionality. Interestingly, this effect exerted by PDGFB was also observed in the presence of DAPT. So PDGFB is able to improve tumor vascularity and allows the anticancer action of DAPT in the tumor. PDGFB Protein, Mouse, Recombinant (His) is expressed in yeast with His tag. The predicted molecular weight is 14.2 kDa and the accession number is Q8R3X9.
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TMPY-02395 | PDGFB Protein, Cynomolgus, Recombinant (mFc) | Cynomolgus | HEK293 Cells | ||
Platelet-derived growth factor-B (PDGFB) is necessary for normal cardiovascular development. The administration of PDGFB alone normalized tumor vasculature by increasing periendothelial coverage and vascular functionality. Interestingly, this effect exerted by PDGFB was also observed in the presence of DAPT. So PDGFB is able to improve tumor vascularity and allows the anticancer action of DAPT in the tumor. PDGFB Protein, Cynomolgus, Recombinant (mFc) is expressed in HEK293 mammalian cells with mFc tag. The predicted molecular weight is 38.9 kDa and the accession number is G7PFK7.
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TMPK-00710 | Claudin-4 Protein-VLP, Human, Recombinant | Human | HEK293 Cells | ||
Claudin-4 (CLDN4) is a key component of tight junctions (TJs) in epithelial cells. CLDN4 is overexpressed in many epithelial malignancies and correlates with cancer progression. Changes in CLDN4 expression have been associated with epigenetic factors (such as hypomethylation of promoter DNA), inflammation associated with infection and cytokines, and growth factor signaling. CLDN4 helps to maintain the tumor microenvironment by forming TJs and acts as a barrier to the entry of anticancer drugs into tumors.
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TMPY-05076 | PDGFB Protein, Canine, Recombinant (His) | Canine | P. pastoris (Yeast) | ||
Platelet-derived growth factor-B (PDGFB) is necessary for normal cardiovascular development. The administration of PDGFB alone normalized tumor vasculature by increasing periendothelial coverage and vascular functionality. Interestingly, this effect exerted by PDGFB was also observed in the presence of DAPT. So PDGFB is able to improve tumor vascularity and allows the anticancer action of DAPT in the tumor. PDGFB Protein, Canine, Recombinant (His) is expressed in yeast with His tag. The predicted molecular weight is 14.9 kDa and the accession number is Q6Q7I7.
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TMPJ-00247 | METAP1 Protein, Human, Recombinant | Human | E. coli | ||
Methionine Aminopeptidase 1 is a member of the M24 family of metalloproteases. METAP1 plays an important role in G(2)/M phase regulation of the cell cycle and may serve as a promising target for the discovery and development of new anticancer agents. METAP1 and METAP2 have different substrate specificity due to the differences in both size and shape of the active sites. The proteolytic removal of N-terminal methionine from nascent peptides is catalyzed by a family of enzymes known as methionine aminopeptidases (MetAPs) and is essential for cell growth. Inhibition of METAPs provides a novel strategy in developing anti-cancer drugs.
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TMPY-01865 | BLMH Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
The papain superfamily member bleomycin hydrolase (BLMH) is a cytoplasmic cysteine peptidase that is highly conserved through evolution. The only known activity of the enzyme is metabolic inactivation of the glycopeptide bleomycin (BLM), an essential component of combination chemotherapy regimens for cancer. The papain superfamily member bleomycin hydrolase (BLMH) is a neutral cysteine protease with structural similarity to a 20S proteasome. Bleomycin (BLM), a clinically used glycopeptide anticancer agent. BLMH is an essential protectant against BLM-induced death and has an important role in neonatal survival and in maintaining epidermal integrity. Sequencing revealed several putative sites phosphorylated by different types of protein kinases, but no signal sequence, transmembrane domain, N-linked glycosylation site or DNA-binding motif.
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TMPY-02072 | HSF1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Heat shock factor protein 1, also known as heat shock transcription factor 1, HSF1, and HSTF1, is a cytoplasm and nucleus protein that belongs to the HSF family. HSF1 is the major transcription factor of HSPs (heat shock proteins) in response to various stresses. Wild type HSF1 (heat shock transcriptional factor 1) is normally inactive. HSF1 / HSTF1 is a DNA-binding protein that specifically binds heat shock promoter elements (HSE) and activates transcription. In higher eukaryotes, HSF is unable to bind to the HSE unless the cells are heat shocked. HSF1 / HSTF1 protects cells and organisms against various types of stress, either by triggering a complex response that promotes cell survival or by triggering cell death when stress-induced alterations cannot be rescued. HSF1 / HSTF1 is the key protein in regulating the stress response. It can be activated under heat, oxidative, or other stress conditions. Dominant-positive and dominant-negative HSF1 are two types of HSF1 mutants. Both of them gain DNA binding activity in the absence of stress. Also, dominant-positive HSF1 acquires transcriptional activity, which dominant-negative HSF1 does not acquire. HSF1 / HSTF1 was also reported to contribute to cell resistance against genotoxic stress, such as that caused by doxorubicin, an anticancer drug in common clinical use.
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