目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T37594 | |||
Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable thioethers as odorless products.2 1.Yamada, T., Iritani, M., Ohishi, H., et al.Pericosines, antitumour metabolites from the sea hare-derived fungus Periconia byssoides. Structures and biological activitiesOrg. Biomol. Chem.5(24)3979-3986(2007) 2.Du, L., Munteanu, C., King, J.B., et al.An electrophilic natural product provides a safe and robust odor neutralization approach to counteract malodorous organosulfur metabolites encountered in skunk sprayJ. Nat. Prod.82(7)1989-1999(2019) | |||
T83912 | |||
HR68是一种抗癌化合物,是过氧化物酶体增殖物激活受体(PPAR)激动剂非诺贝酯的衍生物。它能降低LN-229胶质母细胞瘤细胞的存活率(IC50 = 1.17 µM)。HR68能够穿越血脑屏障,在对替莫唑胺耐药的原位患者衍生的异种移植(PDX)小鼠胶质母细胞瘤模型中发挥作用。 | |||
T73301 | |||
ATR-IN-20是一种高效的ATR(ATM/ATR)抑制剂, IC50值仅为3 nM。该化合物还能抑制mTOR(IC50值为18 nM),并展示出对PI3Kα(100 nM)、ATM(100 nM)和DNA-PK(662 nM)的良好选择性。ATR-IN-20具备优秀的药代动力学属性(F=30%),同时显示了其抗癌潜力。 | |||
T63879 | |||
microRNA-21-IN-1(compound 7A)是一种高效microRNA抑制剂,对Hela和HCT-116细胞显示出抗增殖活性,IC50值分别为5.5 μM和2.8 μM,并能促进Hela细胞凋亡(apoptosis)。该化合物通过上调microRNA-21下游功能靶点(PTEN、EGR1、SLIT2)的表达,有助于抗癌研究。 | |||
T62521 | |||
A2AAR/HDAC-IN-1 (compound 14c) 是一种口服具有活力的、平衡的 A2AAR/HDAC 双抑制剂,作用于 A2AAR (Ki: 163.5 nM)、HDAC1 (IC50: 145.3 nM)。A2AAR/HDAC-IN-1 具有抗癌 (anticancer) 效果。 | |||
T36887 | |||
8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland microsomes (IC50= 31 μM).4 1.Crombie, L., and Holloway, S.J.The biosynthesis of calendic acid, octadeca-(8E,10E, 12Z)-trienoic, acid, by developing marigold seeds: origins of (E,E,Z) and (Z,E,Z) conjugated triene acids in higher plantsJ. Chem. Soc. Perk. T. 12425-2434(1985) 2.Yasui, Y., Hosokawa, M., Kohno, H., et al.Growth inhibition and apoptosis induction by all-trans-conjugated linolenic acids on human colon cancer cellsAnticancer Res.26(3A)1855-1860(2006) 3.Shinohara, N., Ito, J., Tsuduki, T., et al.Jacaric acid, a linolenic acid isomer with a conjugated triene system, reduces stearoyl-CoA desaturase expression in liver of miceJ. Oleo Sci.61(8)433-441(2012) 4.Nugteren, D.H., and Christ-Hazelhof, E.Naturally occurring conjugated octadecatrienoic acids are strong inhibitors of prostaglandin biosynthesisProstaglandins33(3)403-417(1987) | |||
T36096 | |||
Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA synthesisin vitro(IC50s = 0.008 and 0.4 μg/ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg/ml, respectively). 1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007) | |||
T73125 | HSP | ||
SMTIN-T140(化合物6a)是一种TRAP1(肿瘤坏死因子受体相关蛋白1)的高效抑制剂,IC50值为1.646 μM。该化合物表现出显著的抗癌活性,可引起线粒体功能障碍,增加线粒体ROS产生以及激活AMPK。在PC3前列腺癌细胞异种移植的小鼠模型中,SMTIN-T140有效抑制了肿瘤生长,并显示出良好的体内安全性。 | |||
T63416 | |||
HDAC-IN-39 是 HDAC 的有效抑制剂,能够作用于HDAC1、HDAC2、HDAC3,他们的IC50值分别为 1.07 μM、1.47 μM 和 2.27 μM。HDAC-IN-39 能够诱导细胞周期阻滞在 G2/M 期,同时也能够明显抑制微管聚合。HDAC-IN-39 对耐药癌细胞表现出良好的抗癌作用。 | |||
T79322 | |||
Antiproliferative agent-30 (Compound 8g) 抑制微管蛋白组装且可抑制FLT3及Abl1。该化合物展现出对血管的破坏活性,并对多种癌细胞系表现出强效的抗增殖能力,包括HCT-116、K562及MV-4-11细胞(IC50值分别为0.054 nM、0.008 nM、0.144 nM)。此外,Antiproliferative agent-30 亦对携带FLT3-ITD-TKD突变的AML显示出抗癌效果。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|