Tubulysin C 是一种高度细胞毒性的肽，是从粘细菌 Archangium geophyra 和 Angiococcus disciformis 中分离的。 Tubulysin 在哺乳动物细胞中显示出极其有效的细胞毒活性，包括多药耐药细胞系，IC50 值在较低的纳摩尔范围内。 Tubulysin C 是一种具有细胞毒性活性微管溶素，抑制微管蛋白聚合并导致细胞周期停滞和凋亡。
Tubulysin C Chemical Structure
CAS No. : 205304-88-7
规格
是否有货
5 mg
询价
10 mg
询价
25 mg
询价
* Please select Quantity before adding items.
生物活性
Tubulysin C is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin C is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
分子量
816.02
Formula
C41H61N5O10S
CAS 号
205304-88-7
中文名称
微管蛋白抑制剂 C
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Kubicek K, et al. The tubulin-bound structure of the antimitotic drug tubulysin. Angew Chem Int Ed Engl. 2010 Jun 28;49(28):4809-12.
[2]. Vlahov IR, et al. Acid mediated formation of an N-acyliminium ion from tubulysins: a new methodology for the synthesis of natural tubulysins and their analogs. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6778-81.
Rhodamine B labeled polyethylene glycol is a fluorescent PEG derivative that has a maximum absorption at 570 nm and emission around 595 nm. Rhodamine B can be easily traced from its pink color and red fluorescence. Additional functionality allows these fluorescent PEG derivatives to be easily conjugated to other molecule or material surfaces.
Physical Properties:
Pink or dark red solid or viscous liquid depends on molecule weight;
Soluble in regular aqeous solution as well as most organic solvents;
Storage Conditions:
Store at -20 0C, dessiccated Protect from light. Avoid frequent thaw and freeze.
Carbenicillin solution is the solution form of Carbenicillin disodium (sc-202519B). Carbenicillin is an ampicillin analog that inhibits bacterial cell wall synthesis even at low pH. Carbenicillin also tends to be more resistant to β-lactamase enzyme degradation than ampicillin and can be used with ampicillin-resistant strains of|Pseudomonas aerogenosa|, gram-positive, and gram-negative bacteria. Carbenicillin solutionis an ampicillin analog stable at low pH
相关属性
折光率
n20D1.68 (Predicted)
熔点
278.34° C (Predicted)
沸点
>36° C (Predicted)
pKa值
pKₐ: 2.44 (Predicted), pK1: 2.76, pK2: 3.5
溶解性
Soluble in water (833 mg/ml), alcohol (40 mg/ml), and methanol. Insoluble in chloroform, and acetone.
Nanocs’ metal chelate PEG conjμgates were made to chelate metal ions for biomedical applications. Pegylated metal chelators have strong afinity with many metal ions and they are water soluble. Conjμgates were provided in lyophilized powder form.
Nanocs’ metal chelate PEG conjugates were made to chelate metal ions for biomedical applications. Pegylated metal chelators have strong afinity with many metal ions and they are water soluble. Conjugates were provided in lyophilized powder form.
相关属性
溶解性
Lyophilized powder form;Soluble in regular aqeous solution and common organic solvents;
Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
IC50 & Target
CYP[1]
体外研究 (In Vitro)
There is decreased N-acetyltransferase (NAT) activity in SC-M1 cells at concentrations of Bergapten (5-Methoxypsoralen, 5-MOP) from 0.05 mM to 25 mM, but no obvious dose-dependent effect is found between these doses (r=0.5687). In COLO 205 cells, there is decreased NAT activity at low doses of Bergapten (0.05 mM and 0.5 mM) and increased NAT activity at a high dose (50 mM). Bergapten induces a dosedependent effect in our experimental concentrations on COLO 205 cells (r=0.8912); a promotion effect at a higher dose (50 mM) and an inhibition effect at lower doses (0.05-0.5 mM), while the concentrations 5-25 mM has no significant difference compared with the control regimen[1]. Bergapten (5-Methoxypsoralen) exerts inhibitory effects on diabetes-related osteoporosis via the regulation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways in osteoprotegerin knockout mice. Bergapten has also been shown to significantly inhibit the production of pro-inflammatory cytokines. Bergapten exhibits the ability to significantly inhibit RANKL-RANK signaling transduction, and to suppress the activation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways, thus protecting trabecular structure and decreasing osteoclastogenic differentiation[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
The metabolic activity of NAT of the rat colon is higher than that of the stomach, and Bergapten (5-Methoxypsoralen, 5-MOP) causes a decrease of AF concentration in the stomach at the 24-h time-period. The concentrations of AAF in the stomach and colon are low. Although DMSO (solvent) influenced the metabolism of AAF, compared with the control regimen, Bergapten still causes an increase in the further metabolism of AAF, and a decrease in the concentration of AAF in the stomach at 24 h, and in the colon during the 24- to 72-h time-period[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
216.19
Formula
C12H8O4
CAS 号
484-20-8
中文名称
佛手苷内酯；佛手柑内酯；佛手醇甲醚；佛手烯；5-甲氧基补骨脂素；香柑内酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Lee YM, et al. Effects of 5-methoxypsoralen (5-MOP) on arylamine N-acetyltransferase activity in the stomach and colon of rats and human stomach and colon tumor cell lines. In Vivo. 2005 Nov-Dec;19(6):1061-9.
[2]. Li XJ, et al. Bergapten exerts inhibitory effects on diabetes-related osteoporosis via the regulation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways in osteoprotegerin knockout mice. Int J Mol Med. 2016 Dec;38(6):1661-1672.
Cell Assay [1]
The human colon adenocarcinoma cell line (COLO 205, from a 70-year-old male Caucasian) sre placed into 75-cm2 tissue culture flasks and grown in RPMI1640 medium, supplemented with 10% fetal bovine serum, containing penicillin and streptomycin (100 μg/mL) and 1 mM glutamine, at 37°C in a humidified atmosphere of 5% CO2 and 95% O2. The human stomach adenocarcinoma cell line are placed into 75-cm2 tissue culture flasks and grown in RPMI 1640 medium, supplemented with 10% fetal bovine serum, containing penicillin and streptomycin (100 μg/mL) and 1 mM glutamine, at 37°C in a humidified atmosphere of 5% CO2 and 95% O2. SC-M1 and COLO 205 cells are treated with different concentrations of Bergapten (0.05, 0.5, 5, 10, 25 and 50 mM) and incubated for 72 h for the dose-effect study of Bergapten on NAT activity. To determine the time-course effect of 0.5 mM Bergapten on NAT activity, the cells are incubated at 37AC and harvested at 12, 24, 48 and 72 h, respectively. Bergapten is dissolved in DMSO and the final concentration of vehicle is <0.1%. Only DMSO (solvent) is added for the control regimen[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [1]
Rats[1] Seventy-two male Sprague-Dawley (SD) rats, weighing approximately 200 g are used. A total of 72 rats are subjected to 3 different regimens, each regimen divided into 4 groups with 6 rats in each group. Gastric intubation is used for delivery of the test compounds into each animal. The first regimen received 1 mL Bergapten (dissolved in DMSO) at a dose of 0.5 mmol per Kg of body weight. Regimen 2, the control regimen, received only 1 mL solvent (DMSO), without any Bergapten. Regimen 3, the contrast regimen, received nothing at that time. Twenty-four h later, all of the rats from the 3 regimens received 1mL AF (dissolved in DMSO) at a dose of 0.3 mmol per Kg of body weight. The groups are divided by different collecting time: 12, 24, 48 and 72 h after AF administration, and then the animals are transferred to individual metabolism cages. The stomachs and the colons of the rats from each regimen are collected and are immediately extracted with ethyl acetate/methanol (95:5). The solvent is evaporated and the residue redissolved in methanol and assayed for AF and AAF by HPLC.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Lee YM, et al. Effects of 5-methoxypsoralen (5-MOP) on arylamine N-acetyltransferase activity in the stomach and colon of rats and human stomach and colon tumor cell lines. In Vivo. 2005 Nov-Dec;19(6):1061-9.
[2]. Li XJ, et al. Bergapten exerts inhibitory effects on diabetes-related osteoporosis via the regulation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways in osteoprotegerin knockout mice. Int J Mol Med. 2016 Dec;38(6):1661-1672.
This peptide is tumor suppressor protein p53 (368-393). There is a biotinylated lysine follwed by a GG linker at the N-terminal and is acetylated at lysine 382. p53 is an ideal tumor suppressor gene because of its ability to control cell proliferation, and senescence. In response to cell stress, cell damage, or ectopic oncogene, p53 also mediates apoptosis.
溶解度
分子量
4034.7
化学式
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
Kubbutat, M. et al. Lett Nature 387, 299 (1997) Li, M. et al. J Biol Chem 277, 50607 (2002)
GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.
IC50 & Target
IC50: 6 nM (Wip1 phosphatase)[1]
体外研究 (In Vitro)
GSK 2830371 potently inhibits Wip1 (2-420) dephosphorylation of FDP and the endogenous substrates phospho-p38 MAPK (T180) with IC50 values of 6 nM and 13 nM, respectively. In the PPM1D-amplified MCF7 breast carcinoma cells, treatment with GSK 2830371 (0.04, 0.11, 0.33, 1, 3, and 9 μM) increased phosphorylation of substrates in a concentration-dependent manner. Treatment of MX-1 and MCF7 cells (Wip1amplified, p53 wild type) with GSK 2830371 (0.001, 0.01, 0.1, 1, and 10 μM) causes concentration-dependent effects in cell growth assays[1]. GSK2830371 has a 50% growth inhibitory concentration (GI50) of 2.65 μM±0.54 (SEM) in MCF-7 cells. Treatment of MCF-7 cells with 2.5μM GSK2830371 results in marked time-dependent degradation of both isoforms of WIP1 over 8 hours which correlated with p53 stabilisation and phospho-p53Ser15 (pp53Ser15)[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
In a pharmacodynamic assay, orally administered GSK 2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreased Wip1protein concentrations in DOHH2 tumors. Following 14 d of oral dosing at 150 mg per kg body weight, BID (twice daily) and TID (thrice daily), GSK 2830371 inhibits the growth of DOHH2 tumor xenografts by 41% and 68%, respectively. Comparable tumor growth inhibition is observed in mice treated BID with either 75 or 150 mg per kg body weight. Greater tumor growth inhibition with the TID schedule is consistent with a short half-life of GSK 2830371 in mice and suggests that sustained inhibition of Wip1 may be required for maximal antitumor effect[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
461.02
Formula
C23H29ClN4O2S
CAS 号
1404456-53-6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Gilmartin AG, et al. Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat Chem Biol. 2014 Mar;10(3):181-7.
[2]. Esfandiari A, et al. Chemical Inhibition of Wild-Type p53-Induced Phosphatase 1 (WIP1/PPM1D) by GSK2830371 Potentiates the Sensitivity to MDM2 Inhibitors in a p53-Dependent Manner. Mol Cancer Ther. 2016 Mar;15(3):379-91.
Kinase Assay [1]
The primary in vitro Wip1 enzymatic assay measured fluorescence generated by Wip-1 (2-420) hydrolysis of fluorescein diphosphate (FDP). 50 μM FDP substrate is added with GSK 2830371 or DMSO at room temperature before addition of 10 nM Wip1 in assay buffer (50 mM TRIS, pH 7.5, 30 mM MgCl2, 0.8 mM CHAPS, 0.05 mg/mL BSA). Fluorescent signal is detected on a Spectramax microplate reader (485/530 nm)[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay [1]
Cells are seeded into 96 well plates at 200-400 cells per well and treated with GSK 2830371 dilution series on day 1. After 7 d, we used the CellTiter-Glo cell viability assay to determine effects on cell growth. Luminescent signal is detected on an EnVision 2104. For clonogenic assays, cells are seeded in 12-well tissue culture plates at 2,000 cells per well. Cells are treated with a compound dilution series on day 1 and again on day 7. After 14 d, cells are washed with 1× PBS, stained with 1 mL of Coomassie Brilliant Blue R-250, and colonies are quantitated with the Optomax Sorcerer colony counter[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [1]
Mice[1] Female SCID mice are subcutaneously inoculated with 1×107 DOHH2 cells and tumor growth is monitored with electronic calipers. When tumors reached 100-200 mm3, animals are treated orally twice (BID) or thrice (TID) daily with vehicle (2% DMSO and 40% Captisol, pH 4.0) or GSK 2830371. For efficacy studies, eight mice per group are administered with GSK 2830371 at 75 or 150 mg per kg body weight BID or 150 mg per kg body weight TID. Tumor growth inhibition (% difference in tumor growth compared to control) is calculated when tumors for vehicle-control mice exceeded 1,000 mm3 (day 11). For pharmacodynamic biomarker analysis, DOHH2 tumors from three mice are harvested 2 or 4 h after final dose following 14 d of treatment with either vehicle or GSK 2830371 at 75 or 150 mg per kg body weight, BID; tumors are frozen in liquid nitrogen for subsequent lysis and western blot analysis.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Gilmartin AG, et al. Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat Chem Biol. 2014 Mar;10(3):181-7.
[2]. Esfandiari A, et al. Chemical Inhibition of Wild-Type p53-Induced Phosphatase 1 (WIP1/PPM1D) by GSK2830371 Potentiates the Sensitivity to MDM2 Inhibitors in a p53-Dependent Manner. Mol Cancer Ther. 2016 Mar;15(3):379-91.
![(Glu8·9)-Helodermin 编码 [209340-47-6]](http://www.fluoroprobe.com/wp-content/uploads/2022/10/20221006_633e58593f848.png)
![(Glu8·9)-Helodermin 编码 [209340-47-6]](http://www.fluoroprobe.com/wp-content/uploads/2022/10/20221006_633e5859910e4.jpg)
![[Lys(Ac)382]-p53 (361-393), biotin labeled 编码](http://www.fluoroprobe.com/wp-content/uploads/2022/10/20221013_63489227a1b97.png)
![[Lys(Ac)382]-p53 (361-393), biotin labeled 编码](http://www.fluoroprobe.com/wp-content/uploads/2022/10/20221013_634892280732d.jpg)
