目录号 | 产品详情 | 靶点 | |
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T36704 | |||
Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes. Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID:21186793 | |||
T28455 | |||
ProTAME is an inhibitor of APC/CFzr and APC/CCdc20. Combinations of proTAME with topoisomerase inhibitors, doxorubicin and etoposide, significantly increase cell death in primary cells and Multiple Myeloma (MM) cell lines, particularly if TOPIIα levels ar | |||
T68403 | |||
AZD6918 is a novel potent and selective inhibitor of the Trk tyrosine kinases. AZD-6918 attenuates the BDNF/TrkB-induced protection of neuroblastoma cells from etoposide in vitro and in vivo. AZD6918 inhibited wild-type TrkB-induced cell migration and cell growth. | |||
T35607 | |||
10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and teniposide and cisplatin-resistant A2780 cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM). | |||
T71361 | |||
CHS-828 nicotinate is a CHS-828 salt with Nicotinic acid.. CHS-828 also known as GMX-1778, is a potent and selective NAMPT inhibitor. CHS-828 inhibits cellular synthesis of NAD. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. CHS 828 has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. CHS 828 showed a synergistic effect with melphalan in 67%, doxorubicin in 47%, etoposide in 38% and Ara-C in 14% of AML samples. | |||
T82202 | |||
H-Gly-Leu-Phe-OH (GLF)为源于α-乳白蛋白的三肽,具有免疫刺激性,能够抑制抗癌药物依托泊苷所引起的脱发、表皮增厚以及脂肪细胞层的变薄。 | |||
T69936 | |||
NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes. The DNA breaks occurred within 1h after treatment with NK314 even without digestion of topoisomerase II by proteinase K, whereas etoposide required digestion of the enzyme protein in cleavable complex to detect DNA breaks. Pretreatment with topoisomerase II catalytic inhibitors, ICRF-193 and suramin, reduced both cleavable complex-mediated DNA breaks and proteinase K-independent DNA breaks, but protease inhibitors and nuclease inhibitors only decreased the latter. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-03452 | NDPK Protein, S. cerevisiae, Recombinant (His) | Saccharomyces cerevisiae | Yeast | ||
Major role in the synthesis of nucleoside triphosphates other than ATP. The ATP gamma phosphate is transferred to the NDP beta phosphate via a ping-pong mechanism, using a phosphorylated active-site intermediate. Required for repair of UV radiation- and etoposide-induced DNA damage.
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TMPH-03451 | NDPK Protein, S. cerevisiae, Recombinant (E. coli, His) | Saccharomyces cerevisiae | E. coli | ||
Major role in the synthesis of nucleoside triphosphates other than ATP. The ATP gamma phosphate is transferred to the NDP beta phosphate via a ping-pong mechanism, using a phosphorylated active-site intermediate. Required for repair of UV radiation- and etoposide-induced DNA damage.
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TMPH-00090 | UGT71C1 Protein, Arabidopsis thaliana, Recombinant (E. coli, His) | Arabidopsis thaliana | E. coli | ||
Possesses quercetin 7-O-glucosyltransferase and 3'-O-glucosyltransferase activities in vitro. Also active in vitro on benzoates and benzoate derivatives. Glucosylates other secondary metabolites in vitro like trans-resveratrol, curcumin, vanillin and etoposide.
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TMPH-00091 | UGT71C1 Protein, Arabidopsis thaliana, Recombinant (Baculovirus, His) | Arabidopsis thaliana | Yeast | ||
Possesses quercetin 7-O-glucosyltransferase and 3'-O-glucosyltransferase activities in vitro. Also active in vitro on benzoates and benzoate derivatives. Glucosylates other secondary metabolites in vitro like trans-resveratrol, curcumin, vanillin and etoposide.
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TMPJ-01411 | HSPB11 Protein, Human, Recombinant (His) | Human | E. coli | ||
Heat Shock Protein β-11 (HSPB11) is a stress-responsive protein that is required to deal with proteotoxic stresses. HSPB11 is composed of an IFT complex B composed of IFT88, IFT57, TRAF3IP1, IFT52, IFT27, HSPB11 and IFT20 and is detected in placenta. HSPB11 has beeb shown to form oligomeric complexes and prevent the aggregation of in vitro denaturated aldolase and glyceraldehyde-3-phosphate dehydrogenase in accordance with the chaperone model of HSPB1 and HSPB5. HSPB11 overexpression protected against etoposide-induced cell death that correlated with a decreased release of mitochondrial Cytochrome C into the cytosol. Inhibition of HSP90 function completely abrogated the protective effect of HSPB11. This data suggests that at least in the case of HSPB11, interaction with other chaperone machines besides HSPA1A may contribute to functional specificity and cellular functioning.
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