目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T71815 | |||
TX-1918 is a cell-permeable tyrphostin derivative that inhibits eukaryotic elongation factor-2 kinase (eEF-2K). TX-1918 disrupts the proliferation of HepG2 and HCT116 tumor cells. | |||
T63509 | |||
Top/HDAC-IN-1 是拓扑异构酶 (Top)/HDAC 双重抑制剂,能够作用于 HDAC1 (IC50: 18 nM)、HDAC2 (IC50: 230 nM)、HDAC3 (IC50: 790 nM)、HDAC6 (IC50: 87 nM) 和 HDAC8 (IC50: 5250 nM)。Top/HDAC-IN-1 对 HCT116 细胞表现出有效的抗肿瘤作用 (IC50: 180 nM),可将 HCT116 细胞的细胞周期阻滞 G2 期,有效诱导其凋亡 (apoptosis)。 | |||
T60689 | |||
ZDLD13 是一种 β-咔啉,具有强大的抗 HCT116 活性,包括抑制侵袭和迁移、抑制集落形成、诱导细胞凋亡以及阻止细胞周期的 G1 期。ZDLD13是口服有效的 CDK4/CycD3选择性抑制剂 (IC50 = 0.38 μM)。ZDLD13 在 HCT116 肿瘤异种移植模型中表现出显着的抑制肿瘤生长作用。 | |||
T62349 | |||
Tubulin aggregation-IN-8 (compound IIc) 是一种有效的tubulin 聚合抑制剂。Tubulin aggregation-IN-8 浓度依赖性地导致 HCT116 肿瘤细胞 G2/M 期细胞周期停滞,并显示显着抑制微管蛋白聚合,IC50值为 12.7 μM。Tubulin aggregation-IN-8 具有研究癌症疾病的潜力。 | |||
TN4340 | PARP | ||
Ivangustin exhibits remarkable cytotoxicity against HEp2, SGC-7901 and HCT116 human cancer cell lines. | |||
T82344 | |||
Gambogic acid B,一种从Garcinia hanburyi树脂中分离得到的活性化合物,对A549、HCT116 和 MDA-MB-231 细胞显示细胞毒性,其IC50值分别为1.60 μM、6.88 μM 和 0.87 μM。 | |||
T37644 | |||
Potent inhibitor of NF-κB activation (IC50 = 85 nM); decreases IκBα phosphorylation. Attenuates LPS-induced nitric oxide production and expression of TNF-α, IL-6 and MCP. Suppresses proliferation of HeLa and HCT116 cells. Anti-inflammatory and antitumor. Hu et al (2007) Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem.Biol. 14 764 PMID:17656313 |Johnson et al (2012) Myxobacteria versus sponge-derived alkaloids: the bengamide family identified as potent immune modulating agents by scrutiny of LC-MS/ELSD libraries. Bioorg.Med.Chem. 20 4348 PMID:22705020 |Kinder et al (2001) Synthesis and antitumor activity of ester-modified analogues of bengamide B. J.Med.Chem. 44 3692 PMID:11606134 | |||
T63383 | |||
SZ-015268 是 CDK7 抑制剂 (IC50: 23.56 nM),对HCC70 (IC50: 33 nM)、OVCAR-3 (IC50: 80.56 nM)、HCT116 (IC50: 12.53 nM) 和 HCC1806 (IC50: 61.55nM) 细胞增殖具有抑制作用。SZ-015268 表现出极显着的抗肿瘤作用。 | |||
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). | |||
T81740 | Trk receptor | ||
Multi-kinase-IN-6 (compound 10e) 是一种效能极高的多激酶抑制剂,具有对 TrkA、ALK2、c-KIT、EGFR、PIM1、CK2α、CHK1 和 CDK2 等多种酶的显著抑制作用。在 MCF7、HCT116 和 EKVX 癌细胞系上,其抗增殖活性突出,IC50 值分别达到 3.36 μM、1.40 μM 与 3.49 μM。此外,Multi-kinase-IN-6 能引起 MCF7 与 HCT116 细胞的细胞周期在 G1/S 期及 G1 期停滞,并有效诱导凋亡。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
TMPY-04023 | BCCIP Protein, Human, Recombinant (His & GST) | Human | Baculovirus-Insect Cells | ||
BCCIP was originally identified as a BRCA2 and CDKN1A interacting protein that has been implicated in maintenance of genomic stability, cell cycle regulation, and microtubule dynamics. The secondary genetic alternations may overcome the progression suppression imposed by BCCIP deficiency through a synthetic viability mechanism. Knockdown of YY1 inhibited the binding of BCCIP itself at BCCIP promoter region proximal to TSS, demonstrating that transcriptional regulation of the YY1 on BCCIP can be modulated by BCCIP itself in a YY1-dependent fashion. BCCIP (BRCA2 and CDKN1A interacting protein) plays a critical role in maintaining the critical functions of p53 in tumor suppression and response to therapy. Celecoxib affects the functions of p53 and inhibits the recovery from the irradiation-induced injury by up-regulating the expression of BCCIP, and subsequently regulates the expressions of genes such as p21 and Cyclin B1 to enhance the radiosensitivity of HCT116 cells in a COX-2 independent manner.
|
|||||
TMPY-00578 | BCCIP Protein, Human, Recombinant | Human | Baculovirus-Insect Cells | ||
BCCIP was originally identified as a BRCA2 and CDKN1A interacting protein that has been implicated in maintenance of genomic stability, cell cycle regulation, and microtubule dynamics. The secondary genetic alternations may overcome the progression suppression imposed by BCCIP deficiency through a synthetic viability mechanism. Knockdown of YY1 inhibited the binding of BCCIP itself at BCCIP promoter region proximal to TSS, demonstrating that transcriptional regulation of the YY1 on BCCIP can be modulated by BCCIP itself in a YY1-dependent fashion. BCCIP (BRCA2 and CDKN1A interacting protein) plays a critical role in maintaining the critical functions of p53 in tumor suppression and response to therapy. Celecoxib affects the functions of p53 and inhibits the recovery from the irradiation-induced injury by up-regulating the expression of BCCIP, and subsequently regulates the expressions of genes such as p21 and Cyclin B1 to enhance the radiosensitivity of HCT116 cells in a COX-2 independent manner.
|