生物活性小分子化合物库_Medchemexpress_(MCE中国)
CCK8检测操作手册 - 细胞技术_MedChemExpress
WST-8 是 MTT 的一种升级替代产品，和 MTT 或其它 MTT 类似产品，如 XTT 、MTS 等相比有明显的优点。
第一，MTT 被线粒体内的一些脱氢酶还原生成的 formazan 不是水溶性的，需要有特定的溶剂来溶解；而 WST-8 和 XTT 、MTS 产生的 formazan 都是水溶性的，可以省去后续的溶解步骤。
第二，WST-8 产生的 formazan 比 XTT 和 MTS 产生的 formazan 更易溶解。
第三，WST-8 比 XTT 和 MTS 更加稳定，使实验结果更可靠。
第四，WST-8 和 MTT 、XTT 等相比线性范围更宽，灵敏度更高，并且更加稳定。
WST-8 对细胞无明显毒性。
加入 CCK-8 溶液显色后，可以在不同时间反复用酶标仪读板，检测时间更加灵活，便于确定最佳测定时间。
产品编号HY-K0301-100T HY-K0301-500T HY-K0301-3000T HY-K0301-12000T包装1 mL 5 mL 5 mL × 6(5 mL × 6) × 4产品名称Cell Counting Kit-8Cell Counting Kit-8Cell Counting Kit-8Cell Counting Kit-8Cell Counting Kit-81包装清单产品概述Cell Counting Kit-8，简称 CCK-8 试剂盒，是一种基于 WST-8 而广泛应用于细胞增殖和细胞毒性的快速、高灵敏度、无放射性的比色检测试剂盒。
CCK-8 溶液可以直接加入到细胞样品中，不需要预配各种成分。
WST-8 在电子耦合试剂存在的情况下，可以被线粒体内的一些脱氢酶还原生成橙黄色的formazan (参考图1) 。
细胞增殖越多越快，则颜色越深；细胞毒性越大，则颜色越浅。
对于同样的细胞，颜色的深浅 (生成的 formazan 量) 和细胞数目呈线性关系 (图2) 。
cck8做标准曲线-细胞技术_MedChemExpress
WST-8 是 MTT 的一种升级替代产品，和 MTT 或其它 MTT 类似产品，如 XTT 、MTS 等相比有明显的优点。
第一，MTT 被线粒体内的一些脱氢酶还原生成的 formazan 不是水溶性的，需要有特定的溶剂来溶解；而 WST-8 和 XTT 、MTS 产生的 formazan 都是水溶性的，可以省去后续的溶解步骤。
第二，WST-8 产生的 formazan 比 XTT 和 MTS 产生的 formazan 更易溶解。
第三，WST-8 比 XTT 和 MTS 更加稳定，使实验结果更可靠。
第四，WST-8 和 MTT 、XTT 等相比线性范围更宽，灵敏度更高，并且更加稳定。
WST-8 对细胞无明显毒性。
加入 CCK-8 溶液显色后，可以在不同时间反复用酶标仪读板，检测时间更加灵活，便于确定最佳测定时间。
产品编号HY-K0301-100T HY-K0301-500T HY-K0301-3000T HY-K0301-12000T包装1 mL 5 mL 5 mL × 6(5 mL × 6) × 4产品名称Cell Counting Kit-8Cell Counting Kit-8Cell Counting Kit-8Cell Counting Kit-8Cell Counting Kit-81包装清单产品概述Cell Counting Kit-8，简称 CCK-8 试剂盒，是一种基于 WST-8 而广泛应用于细胞增殖和细胞毒性的快速、高灵敏度、无放射性的比色检测试剂盒。
CCK-8 溶液可以直接加入到细胞样品中，不需要预配各种成分。
WST-8 在电子耦合试剂存在的情况下，可以被线粒体内的一些脱氢酶还原生成橙黄色的formazan (参考图1) 。
细胞增殖越多越快，则颜色越深；细胞毒性越大，则颜色越浅。
对于同样的细胞，颜色的深浅 (生成的 formazan 量) 和细胞数目呈线性关系 (图2) 。
PHA-680632-DataSheet-MedChemExpress
PHA-680632TGI without signs of toxicity in the HL60 human acute myelogenous leukemia xenograft model. PHA-680632treatment at 60 mg/kg i.v. b.i.d. for 5 days results in 78% of TGI without signs of toxicity in the A2780 human ovariancarcinoma model[1]. PHA680632 in association with radiation leads to an additive effect in cancer cells, especially inthe p53-deficient cells, but does not act as a radiosensitiser[2].PROTOCOLKinase Assay [1]Inhibition of kinase activity by PHA-680632 is assessed using a scintillation proximity assay format. In this assay, the biotinylated substrate is transphosphorylated by the kinase in presence of ATP traced with γ33-ATP. Thephosphorylated substrate is then captured using streptavidin-coated scintillation proximity assay beads and theextent of phosphorylation is evaluated by β-counter after a 4-hour rest for the floatation of the beads on a dense 5 MCsCl solution. In particular a peptide derived from the Chocktide sequence (LRRWSLGL) is used as substrate forAurora A, whereas the optimized peptide Auroratide1 is employed for Aurora B and C. The assay is run in a robotizedformat on 96-well plates. The potency of the compound toward Aurora kinases and 29 additional kinases belongingto our Kinase Selectivity Screening panel is evaluated and the relevant IC50s are determined[1].MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay [1]Cells are seeded at different densities ranging from 5,000 to 15,000 cm2 in 24-well plate with the appropriate complete medium. After 24 hours, plates are treated with PHA-680632 and incubated for 72 hours at 37°C in 5% CO2atmosphere. At the end of incubation time, cells are detached from each plate and counted using a cell counter. IC50sare calculated using percentage of growth versus untreated control[1].MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration [2]Mice: Tumour xenograft mice are randomly allocated into four groups (six mice per group): A, control; B, IR alone, 8 Gy in 1 day; C, PHA-680632 alone, 40 mg/kg, b.i.d., for 4 days; D, same dose of PHA-680632 combined with IR (24 h after the first administration of PHA680632, similar schedule as IR alone) for 4 days. Drug or vehicle control (same volume of 20% Tween-80 in 5% glucose solution) is administered intraperitoneally (i.p.). The tumour size is measured twice a week using an electronic caliper. Follow-up of individual mice is conducted. The tumour volume is estimated from 2D tumour measurements[2].MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES[1]. Soncini C, et al. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res. 2006 Jul 1;12(13):4080-9.[2]. Tao Y, et al. Enhancement of radiation response by inhibition of Aurora-A kinase using siRNA or a selective Aurora kinase inhibitor PHA680632 in p53-deficient cancer cells. Br J Cancer. 2007 Dec 17;97(12):1664-72.Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
Indoleamine_2,3-Dioxygenase(IDO抑制剂_激动剂_MCE
Cat. No.: HY-79531
Bioactivity: IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM, shows activity in Hela cell (IC50=12 nM).
Cat. No.: HY-16724
Bioactivity: Indoximod is an IDO pathway inhibitor, and reverses IDO-mediated immune suppression.
Purity:
>98%
Clinical Data: Phase 1, Phase 2
Purity:
>98%
Clinical Data:
Size:
10mM x 1mL in DMSO,
5 mg, 10 mg, 50 mg
Purity:
>98%
Clinical Data:
Size:
10mM x 1mL in DMSO,
5 mg, 10 mg, 50 mg
INCB 024360
(Epacadostat)
NLG919
(NLGБайду номын сангаас919)
Cat. No.: HY-13983
Bioactivity: NLG919 is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM.
Purity:
Purity:
>98%
Clinical Data:
MK-1775_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:MK–1775 is a potent Wee1 inhibitor with IC 50 of 5.2 nM.IC50 & Target: IC50: 5.2 nM (Wee1)In Vitro: MK–1775 enhances the cytotoxic effects of 5–FU in p53–deficient human colon cancer cells. MK–1775 inhibits CDC2 Y15phosphorylation in cells, abrogates DNA damaged checkpoints induced by 5–FU treatment, and causes premature entry of mitosis determined by induction of Histone H3 phosphorylation [1]. MK–1775 abrogates the radiation–induced G2 block in p53–defective cells but not in p53 wild–type lines [2]. The combination of gemcitabine with MK–1775 produces robust anti–tumor activity and remarkably enhances tumor regression response (4.01 fold) compared to gemcitabine treatment in p53–deficient tumors [3]. In Vivo: In vivo, MK–1775 potentiates the anti–tumor efficacy of 5–FU or its prodrug, capecitabine, at tolerable doses [1]. MK–1775(60 mg/kg twice daily, p.o.) enhances H1299 xenograft tumor response to fractionated radiotherapy [2]. MK–1775 (30 mg/kg. p.o.)regresses tumor growth in PANC198, PANC215 and PANC185 as compared to GEM treated mice [3]. PROTOCOL (Extracted from published papers and Only for reference)Cell Assay:[2]Total protein is extracted from the cell pellet using a lysis solution containing 50 mM HEPES (pH 7.9), 0.4 mol/L NaCl, and 1 mM EDTA and fortified with 10 μL/mL phosphatase inhibitor cocktail 1, 10 μL/mL phosphatase inhibitor cocktail 2, 10 μL/mLprotease inhibitor, and 1% NP–40. Protein concentration of the lysates is determined by the Bio–Rad protein assay. Equal amounts of protein are separated by 12% SDS–PAGE and transferred to an Immobilon membrane. Nonspecific binding sites on the membrane are blocked in 5% nonfat dry milk in Tris (20 mM)–buffered saline (150 mM, pH 7.4) with 0.1% Tween (TBS–T). Protein signals are detected by incubating the membrane in primary antibody in 5% nonfat dry milk overnight at 4°C, followed by a 45–min incubation in theappropriate peroxidase–conjugated secondary antibody. The membrane is then developed by enhanced chemiluminescence with ECL plus Western Blotting Detection Reagents on a Typhoon 9400 scanner.Animal Administration:[2]Tumor xenografts are produced in the leg by im inoculation of 1×106 Calu–6 cells in 10 μL. Irradiation and MK–1775 treatment are started when tumors reach 8 mm diameter and continue for 5 days. Gamma–rays are deliveredlocally to the tumor–bearing legs of unanesthetized mice using a small–animal irradiator consisting of two parallel–opposed 137Cs sources, at a dose rate of 5 Gy/min. Tumors are irradiated twice daily separated by 6 h. MK–1775 is given by gavage in 0.1 mL volumes 1 h before and 2 h after the first daily radiation dose.References:[1]. Hirai H, et al. MK–1775, a small molecule Wee1 inhibitor, enhances anti–tumor efficacy of various DNA–damaging agents, including 5–fluorouracil Cancer Biol Ther. 2010 Apr;9(7):514–22.Product Name:MK–1775Cat. No.:HY-10993CAS No.:955365-80-7Molecular Formula:C 27H 32N 8O 2Molecular Weight:500.60Target:Wee1Pathway:Cell Cycle/DNA Damage Solubility:10 mM in DMSO[2]. Bridges KA, et al. MK–1775, a novel Wee1 kinase inhibitor, radiosensitizes p53–defective human tumor cells. Clin Cancer Res. 2011 Sep 1;17(17):5638–48. Epub 2011 Jul 28.[3]. Rajeshkumar NV, et al. MK–1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53–deficient pancreatic cancer xenografts.Clin Cancer Res. 2011 May 1;17(9):2799–806. Epub 2011 Mar 9.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
小分子化合物库高通量筛选
MedChem ExpressInhibitors, Agonists, Screening LibrariesMedChemExpress USACompound Screening LibraryHandling InstructionsLockedTel: 609-228-6898Tech E-mail:tech@ Fax: 609-228-5909 Sale E-mail: sales@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USARecognize Me!96-Well Format Racks for Sample Storage TubesLidLockOur sample rack uses a LidLock lever to secure the top of the rack. The LidLock can prevent the tubes in racks from falling out if the rack is inverted or dropped. Simply push the LidLock in the desired direction as marked by the arrows to open or lock the rack.RackCodeEach 96 sample-rack has a “RackCode ” linear barcode located on the side which can be used to easily distinguish different racks.Compound Technical Documents:Each compound library is shipped with a flash drive containing an Excel file that describes the detailed information of compounds in your library. The disk also contains the SDF , COA for every compound, this general handling instructions and compound layout for each screening library.The Excel file details the following information:RackCode, Cat. No., Product Name, Plate Location, VialCode, CAS No., M.Wt, Target, Saltdata, Information, Smiles, Solubility, Method of Analysis, Batch No., Quantity, URL and Pathway.Chemical structure information for each compound is contained in the relevant SDF files.If you have any questions, please contact our technical support via Email at: tech@ .VialCodeCompounds can be identified quickly by scanning the 2D barcode with an HD barcode scanner. Each 96-well format sample storage tube contains a "VialCode " 2D barcode located on the base of the vial. Using the 2D barcode, you can look up the corresponding compound information for the vial in electronic files or the provided hard copy.1 Can we centrifuge the whole rack?Yes. It is advised to centrifuge all of the samples before experimental use. This can prevent the compound from adhering to the tube wall or even the tube gap and can reduce experimental error.2 How can I use the 2D barcode on the bottom of vial?Use an HD barcode scanner to scan the barcode, and then find the corresponding compound information in the Excel or the provided hard copy.3 How do I dissolve my compounds (dry solid)?Add the relevant solvent (DMSO, Ethanol etc.) specified by your ordered format (100 μL or 250 μL) and dilute the solution to a concentration of 10 mM.4 What are the appropriate compound storage conditions?For dry solid compounds, store at 4°C.For solutions, store at -80°C.For some special compounds, specific handling instructions are provided.5 After receiving the compound library, the ice box has melted, will this affect the efficacy of the compound?MCE products are primarily chemical synthesis products which are not temperature sensitive. The ice boxes inside of the packages are used to prevent the occurrence of extreme temperatures during the process of transportation, and a melted icebox will not affect the reagent quality. After transit, the icebox is no longer needed.Frequently Asked Questions:。
Cryptotanshinone-Cryptotanshinon-DataSheet-MedChemExpress
体内研究
Cryptotanshinone reverses the ovarian IR and significantly increases 2-deoxy-D-[1,2-3H]-glucose uptake in all examined tissues from the DEX-treated mice. Cryptotanshinone significantly reduces the ovulation rate and plasma E2 and P levels [2]. Cryptotanshinone administration significantly reduces the body weight and food intake of ob/ob mice (C57BL/6J-Lepob) and diet-induced obese (DIO) mice in a dose-dependent manner. Cryptotanshinone causes noticeably less fat in the adipose tissues, significant reductions of serum triglycerides and cholesterol levels, and 2.5- to 3-fold higher AMPK activity of the skeletal muscles than in the control mice. Oral administration of Cryptotanshinone at 600 mg/kg/day produces dramatic reductions in blood glucose levels of ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb), and ZDF rats, which occur after 3 days and persist over the entirety of the monitoring period [4].
TAME_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:TAME is a small molecule anaphase–promoting complex/cyclosome (APC) inhibitor.IC50 Value: 12 μM ( inhibits cyclin proteolysis in mitotic Xenopus egg extract)Target: APCin vitro: TAME at concentration of 1–200 μM arrests interphase extract treated with recombinant cyclin B1/Cdc2 complex in mitosis,with stable cyclin B1 and phosphorylated Cdc27. TAME at concentration of 200 μM dramaticly inhibits the ubiquitin ligase activity of the Anaphase–Promoting Complex (APC), accompanied by reduced binding of Cdh1 to APC. TAME addition to interphase extract reduces Cdc20 association with the APC in a dose–dependent manner partly by binding directly to APC, and the contribution motif is the C–terminal isoleucine–arginine (IR) tail on APC. TAME is hydrolysed by trypsin with Km of 0.328 mM. TAME accelerates the ATP hydrolysis process about 12–fold. TAME interacts with β and γ phosphate and the adenine ring of ATP by the guanidinium group and the aromatic ring. TAME at concentration of 50 mM inhibits nutrient–induced germination and pressure–induced germination at 600MPa in Bacillus subtilis. TAME induces a concentration dependent contractile response on ileal strips with EC50 of 4.3 x 103 M.in vivo: N/AReferences:[1]. Zeng X et al. Pharmacologic inhibition of the anaphase–promoting complex induces a spindle checkpoint–dependent mitotic arrest in the absence of spindle damage. Cancer Cell. 2010 Oct 19;18(4):382–95.[2]. Paul VD, Rajagopalan SS, Sundarrajan S, George SE, Asrani JY, Pillai R, Chikkamadaiah R, Durgaiah M, Sriram B, Padmanabhan S.A novel bacteriophage Tail–Associated Muralytic Enzyme (TAME) from Phage K and its development into a potent antistaphylococcal protein.BMC Microbiol. 2011 Oct 11;11:226.Product Name:TAME Cat. No.:HY-13255CAS No.:901-47-3Molecular Formula:C 14H 22N 4O 4S Molecular Weight:342.41Target:APC Pathway:Cell Cycle/DNA Damage Solubility:10 mM in DMSOCaution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
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生物活性小分子化合物库- Medchemexpress （MCE）美国原装进口，现货供应，提供组合定制服务
品牌：Medchemexpress （MCE）
保存条件：-20℃
供应商：MCE中国
数量：大量
保质期：2年
Size：
Pre-dissolved DMSO/Solid（Or dry solid）
100 uL/well (10 mM solution)
200 uL/well (10 mM solution)
MedChemExpress (MCE)专注于各种抑制剂、调节剂、API、天然产物及化合物库，总部位于美国新泽西。
MCE经过十年努力已成为全球生物活性小分子领域的一流供应商。
MedChemExpress(MCE)产品涵盖近20个热门研究领域，1000多个细分靶点，超过3000个现货抑制剂、拮抗剂和激动剂。
相关的应用成果已发表于Nature、Cell等国际知名杂志，在全球20余个国家地区设有代理机构。
上海皓元生物医药科技有限公司(MCE 中国) 是MedChemExpress (MCE) 亚洲总代理。
货号：HY-L001
• A unique collection of 1428 bioactive compounds for high throughput screening (HTS) and high content screening (HCS).
• Bioactivity and safety confirmed by preclinical research and clinical trials.
• Some inhibitors have been approved by the FDA.
• Targets such as RTKs, PI3K, Aurora Kinase, CDK, and MAPK etc.
• Structurally diverse, medicinally active, and cell permeable.
• More detailed compound information with structure, IC50, and brief introduction.
• NMR and HPLC validated to ensure high purity and quality.
• All compounds are in stock.
/screening/Bioactive_Compound_Librar y.html
Formulation: A collection of 1428 bioactive compounds supplied as pre-dissolved DMSO solutions
Container: 96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode
Stability: 3 months -20°C in DMSO, 6 months -80°C in DMSO
Shipping: Blue ice Packaging: Inert gas。