selleck inhibitor catalog--june

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1un.20ll1un.20llScreening LibrariesProteins/PeptidesAPIssiRNAsSelleck pre-defined or custom siRNA libraries in human and mouse are available in any of our three market-leading siRNA technologies for screens with efficient, specific and guaranteed knockdown.Selleck compound libraries contain over 1000 unique and diverse bioactive compounds suitable for high-throughput screening, cell based high-content screening and chemicalbiology applications.Selleck provides about 400 kinds of fine Active Pharmaceutical Ingredients (APIs) and 120 kinds of natural products for global customers.Selleck produces over 300 grow factors, enzymes, cytokines and chemokines. We also specialize in both peptide synthesis and peptide modifications.Selleck provides high purity small molecule inhibitors on signaling pathways such as Apoptosis, Akt, MAPK, angiogenesis etc.AntibodiesSelleck offers a broad selection of monoclonal and polyclonal antibodies to human proteins for various applications, including Western blot, immunohistochemistry, immunofluores-cence, flow cytometry and more.InhibitorsWhats in it for me?Selleck is one of the world leading suppliers of high-performance life-science products. We have over 8,000 products which consist of inhibitors, antibodies, RNAis, proteins and peptides those which focus on signaling pathways such as MAPK, PI3K/Akt, and apoptosis. Furthermore, compound libraries for high-throughput screening and high-content screening are also available.QualitySelleck pays great attention to the purity, stability and activity of the products. Not only could Selleck provides the chemical test data, such as HNMR, LC-MS and HPLC, but also provides the reviews overall evaluations of the products from the customers who have used our products. Western Blot, MTT, RT-PCR, ICH photos and figures provide double guarantee for the biological activities of our products in life-science research. If our products have any quality prob-lems, we will unconditionally refund or replace the products .SupportSelleck has been leading the way in biology, medical and pharmaceutical science researches, and its reagents and services have been helping scientists world-wide to make successful discoveries. Our team is dedicated to customer satis-faction and our technical experts provide professional support to ensure the best results.Worldwide RelationSelleck has established long-term and stable relationships with more than 10,000 customers from pharmaceutical and biotech companies, universities and research institutions. Selleck has headquarters in United States,Asia and Europe, and also has 38 distributors worldwide. We provide overnight delivery in North America and Europe.Our goalOur goal is to provide scientists worldwide an easy access to the most innovative life science reagents, and to help them make more significant discoveries.Welcome to'PMMPXUIF0OMJOF1VSDIBTJOH'MPX$IBSUBOENBLFBOFBTZPSEFSPG4FMMFDLQSPEVDUTJOTUPDLOrder OnlineOnline orders can be paid by credit card or debit card.Order offlineTel: +1-832-582-8158 (Phone orders can be placed in 1 min)Fax: +1-832-582-8590Email: [email protected] Follow the Online Purchasing Flow Chart and place orders easily.Ordering InformationOnline Payment with High Safety Guarantee:To ensure safety of your online payments, Selleck has upgraded system to Verisign SSL and is accredited by BBB. Verisign SSL is the leader in providing Secure Socket Layers for e-commerce websites.3FHJTUFS4JHOJO BEEQSPEVDUTUPTIPQQJOHDBSUDIPPTFQBZNFOUNFUIPET1BZOPXPS1BZMBUFSSecure ShoppingUse of Research ProductsSelleck products are applied only for laboratory research and analytical use, and not for any human or veterinary use. They should be used only by technically-qualified individuals or under their direct supervision. 1. Delivery will be done within 24 hours if items you ordered are in stock and the shipment will normally take 2-3 working days. 2. For orders that are out of stock, we will arrange replenishment within 24 hours and will keep you informed of the delivery status via email or phone. 3. The shipping and handling fee is 40USD in US and 28EUR in Europe.4. Orders will be shipped directly to you via UPS, TNT or FedEx. 5. Packages and products should be inspected immediately upon receipt. Notification of damage, shortages or defects should be given to us immediately. by e-mail or fax.Overnight Delivery1. Selleck has well-established warehouse system in America, Europe and Asia and could guarantee of 90% orders overnight delivery. 2. Purchase orders should be placed before 2:30 p.m. for overnight delivery.3. The overnight delivery is subject to the stock status. We appreciate your kind understanding.Return is Easy1. Selleck has 365-day Free Return policy. If you are not satisfied with your purchase, either for protocol-related problems or for product-related problems, you may return items at anytime for free within 365 days from the purchase date.2. All requests for returns must have prior authorization and must be shipped back to Selleck in the original packaging, and the items are in the same condition. 3. Please have on hand the invoice number, purchase order number or air bil number.4. Once your return is received and inspected by the QC center (usually within 72 hours of receipt), your refund will be processed and a credit will be automatically applied to your credit card or original method of payment within 7 days.Free delivery is quatified when the total value of your order exceeds 500USD/EUR/GBP (for US,Europe and UK respectively).DeliveryFree DeliveryTable of ContentsEGFR VEGFR/PDGFR FGFR Src-Bcl-Abl IGF-IRHER2 c-Kit c-Met FLT-3 ALK Vascular Disrupting AgentETA receptorHIFSyk Tie21 Angiogenesis/Tyrosine Kinase Pathway361111131314141516161616 17 17Cell Cycle/Checkpoint Pathway18ROCKPLKCDKTopoisomeraseMicrotubuleAntimetabolitesTelomeraseDNA/RNACheckpointDihydrofolate reductase20202022222425252626HDAC SignalingHDACSir2-like family deacetylase272731ApoptosisBcl-2 TNF-alpha p53 Survivin 3234353535PARPPARP3638KspAurora KinaseAurora Kinase404244MAPK SignalingMEK p38 MAPK B-Raf JNK 4547 4850 50PI3K/Akt SignalingPI3KmTORDNA-PKGSK-3PDK-1ATMAkt5153565757575858HormoneAndrogen ReceptorEstrogen receptor Aromatase5-alpha-reductaseGPR596060616262Proteases/HSP90/HSP70 PathwayProteasomeHSP-70 DPP-4HSP-90AminopeptidaseHCV protease66686869697070Wnt/Hedgehog/Notch PathwayHedgehog WntVHFUHWDVH71727272Jak/Stat PathwayStatJak737474Ca/cAMP/Lipid SignalingPKC7576Neuro Signaling PathwayCGRPCOX7778787*)6PDG6LJQDOLQJ7*) 7980Integrase/CCR5 PathwayCCR5Integrase636565GPCR PathwayVasopressin receptor Angiotensin receptorCB1 receptor UHFHSWRUSerotonin receptorSmooth henedmGluR2/mGlu3 81 82 83 83 83 828283Ion ChannelCFTRCalcium channelProton pump 84 85 85 86Cytochrome P45014a-demethylase 87 88OthersFactor Xa S1P ReceptorsPLA2P-glycoprotein Reverse transcriptase Xanthine oxidase Serotonin reuptake Phosphodiesterase AcetylcholinesteraseAdrenergic receptor HistamineGABA 90 91 91 91 91 92 93 93 94 95 96 97 98Peptide InhibitorsCDKBcl-2p38 MAPK JNK Oxytocin receptor Glycoprotein receptor Vasopressin receptor LHRHR/GnRHR PTHR Melanocortin-1 receptor PKCSNAPR NKRBDKR/KORTRH receptor CRF receptor GRF-R Ghrelin receptor Tachykinin NK1 receptor Angiotensin receptor Secretin receptor SSTR GCGRGHSR 99100100100100100101101101102103103103103103104104104104105105105105105106 Angiogenesis/Tyrosine Kinase0rcoderesardArd|oderes|s:3|dra||rdT|ree-0|rers|ora|Turor0roWl|. Janusz Rak, Joanne L Yu et al. J Investig Dermatol Symp Proc. 2000(5):2433.Tumor growth is dependent on the perpetual recruitment of host blood vessels to the tumor site. This recruitment process (mainly via angiogenesis) is thought to be triggered by the very same set of genetic alterations as those responsible for other aspects of malignant transformation. Potent oncogenes are able to deregulate expression of both angiogenesis stimulators and inhibitors in cancer cells. For example, mutant ras expression is associated with increased production of VEGF and downregulation of TSP-1. Upregulation of VEGF and angiogenesis can also be induced by constitutive activation of other oncogenic proteins (e.g., EGFR, Raf, MEK, PI3K) acting at various levels on the Ras signaling pathway. The mode and the magnitude of such pro-angiogenic influences can be significantly modified by cell type (fibroblastic or epithelial origin), epigenetic factors (hypoxia, changes in cell density), and/or presence of additional genetic lesions. Activated oncogenes (e.g. ras, src, HER-2) induce co-expression of angiogenic prop-erties concomitantly with several highly selectable traits (increased mitogen-esis, resistance to apoptosis). On the other hand oncogene-induced reduction in growth requirements may also endow tumor cells with a diminished dependence on proximity to blood vessels. Angiogenesis can be simultaneously suppressed by effective use of the specific oncogene antagonists and signal transduction inhibitors.l2S1010 BIBF1120(Vargatef)Inhibition of Lck enhances glucocorticoid sensitivity and apoptosis in lymphoid cell lines and in chronic lymphocytic leukemiaMW Harr, PF Caimi, KS et al. Cell Death & Differentiation. 2010(17):1381-1391.S1012 BMS-536924 PTK6 Regulates IGF-1-Induced Anchorage-Independent SurvivalIrie HY, Shrestha Y et al. PLoS ONE. 2010;5(7): e11729.S1014 Bosutinib(SKI-606) Inhibition of ser/thr phosphatases induces capacitation-associated signaling in the presence of Src kinase inhibitorsKrapf D, Arcelay E et al. J. Biol. Chem. 2010(285): 7977-7985. S1019 CI-1033(Canertinib)The fibroblast-derived paracrine factor neuregulin-1 has a novel role in regulating the constitutive color and melanocyte function in human skinWonseon Choi, Rainer Wolber et al. J Cell Sci. 2010(123): 3102-3111.S1021 Dasatinib Anti-leukemic activity of Dasatinib in both p53wild-type and p53 mutated B malignant cells Raffaella Bosco, Marco Rabusin et al. Invest New Drugs 2010.S1021 Dasatinib/ S1026 Imatinib MesylateMolecular Characterization of c-Abl/c-Src Kinase Inhibitors Targeted against Murine Tumour Progenitor Cells that Express Stem Cell MarkersRaffaella Bosco, Marco Rabusin et al. Invest New Drugs 2010.S1023 Erlotinib Hydrochloride Dual specificity phosphatase 6(DUSP6) is an ETS-regulated negative feedback mediator of oncogenic ERK-signaling in lung cancer cells Zhenfeng Zhang, Susumu Kobayashi et al. Carcinogenesis 2010;31(4): 577-586 Mechanisms of myogenic tone of coronary arteriole: Role of down stream signaling of the EGFR tyrosine kinaseAli H. Amin, Zakaria Y et al. Microvascular Research 2011;81(1):135-142Papers Using Selleck ProductsEGFR (Epidermal growth factor receptor)EGFR Ard|oderes|s/Tvros|reK|rase3S1392 Pelitinib5mg25mg50mgNCNONHONHNClFSynonyms: EKB-569, WAY-EKB 569Size Price5mg10mg50mg5mg10mg25mg25mg50mg100mgNN HNNNNHS1486 AEE788AEE788 is a novel dual inhibitor of EGFR/ErbB2 and VEGFR tyrosine kinases (IC50s: EGFR=2 nM, ErbB2=6 nM, KDR=77 nM, and Flt-1=59 nM). AEE788 demonstrated antiproliferative activity against EGFR and ErbB2-overexpressing cell lines and inhibited the proliferation of human umbilical vein endothelial cells. Oral administration of AEE788 to mice resulted in high and persistent compound levels in tumor tissue.Size PriceSynonyms: NVP-AEE 788Produced Independently by our customer Dr.Zhang, Tianjin Medical UniversityS1011 BIBW2992FeedWestern blot analysis of extracts from EGF, BIBW2992 treated T47D breast denocarcinoma cell line using antibodies as indicated.S1011 BIBW2992FCl NHNNHNO ONOBIBW2992 shows potent activity against EGFR and HER2. BIBW2992 was effective in inhibiting survival of H1666 or NCI-H1975 EGFR, with IC50s below 100 nM . Assessed in a standard xenograft model of the epidermoid carcinoma cell line A431.Daily oral treatment with BIBW2992 at 20 mg/kg for 25 days resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. Synonyms: TovokSize PriceH1666 or NCI-H1975 EGFR, with IC50s below Nepidermoid carcinoma cell line A431.Daily oral tredramatic tumor regression with a cumulative treatP-EGFR0nM1nM0.1nM0.01nM0nM-+ + + +EGF(100ng/ml)BIBW2992EGFR S1028 Lapatinib Ditosylate Lapatinib have IC50 values against purified EGFR and HER2 of 10.2 and 9.8 nM, respectively. And IC50 >10000nM against c-Raf-1, MEK, ERK, CDK1, CDK2, p38 and VEGFR-2.The IC50s for inhibition of cell JURZWKE\KWUHDWPHQWZLWK*:DUH0IRU$0IRU+10IRU%70IRUN87. Lapatinib undergoes first-pass metabolism catalyzed by CYP3A4/5 and does not appear to be a substrate for P-glycoprotein.Synonyms: Tykerb, Tyverb, GW-572016Size PriceNNHN ClO FONHSO OS OHOOS OHOO1 10 100 1000 10000050100lapatiniblapatinib+7839Lapatinib conc (nM)% control cell growthEGF (100ng/ml) + -beta-ActinTotal Aktp-Akt (Ser.473)p-Erk1/2 (Thr.202/Tyr.204)p-ErbB2 (Tyr.1221/1222)p-TyrosineTotal Erk1/2+ + +Lapatinib 0M 0M5M0.5M0.05MGrowing- SKBR3 cells were starved for 4h in serum-free medium and treated as indicated; or left growing in complete medium (last lane).Sheddase inhibition improves the ability of lapatinib to inhibit BT-474 cell growth.Provided from our customer Carl Uli Bialucha,Cold Spring Harbor Laboratory ,NY,USAS1028 LapatinibFeed25mg50mg100mgS1025 GefitinibThe monolayer growth of these EGF-driven untransformed cells such as MCF10A is inhibited by ZD1839 with an IC50 of 20 nM, similar to its IC50 in vitro for EGFR and consistent with effective inhibition of EGFR in vivo. Cell line characteristics and sensitivity to Gefitinib at 1uM are 59% inhibition for MDA-MB-231, 74% inhibition for A431, 81% inhibition for SKBr3,60% inhibition for SKOV3, 33% inhibition for BT474,52% inhibition for MCF-7, 28% inhibition for T47D, respectively.Synonyms: ZD-1839, IressaSize PriceNNHN ClFOO NOData from Oncogene (2010), 114 using our product.Data provided by our customerVicky TinThe University of Hong Kong.Effects of shRNA-mediated RECK depletion on EGFR signaling in MEFs. (a) Immunoblotting (IB) of the indicated proteins in wild-type MEFs transduced with the indicated shRNAs and cultured for 48 h in the presence of 0.1% dimethyl sulfoxide(DMSO; vehicle) or 1 mM gefitinib (S1025, Selleck Chemicals,Houston, TX, USA). (b) Immunoprecipitation from whole lysates of cells from panel a with an anti-phosphorylated tyrosine (pTyr) antibody. Precipitates from 500 mg protein in whole cell lysates (upper) or 20 mg protein in whole cell lysates (lower) were analyzed by IB with anti-EGFR antibody.MTT assay result. 0-500nM Gefitinib (Selleck S1025) treated with H1299, H358, H25 and HCC827 cell lines by 72h, Proliferation rate was tested.S1025 GefitinibFeedPelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. Pelitinib irreversibly binds covalently to EGFR, ErbB-1, -2 and -4, thereby inhibiting receptor phosphorylation and signal transduction and resulting in apoptosis and suppression of proliferation in tumor cells that overexpress these receptors. Pelitinib inhibits EGF-induced phosphorylation of EGF-R and the growth of tumors that overexpress EGF-R in animal models.Toll Free:(877)796-6397 www.selleckchem.com [email protected]:+1-832-582-8158---USA and Canada only---\l"S2192 AZD8931AZD8931 is a novel potent reversible small molecule epidermal growth factor receptor, ErbB2 (HER2) and ErbB3 inhibitor with an IC50 of 4, 3, 4 nM, respectively. It has a unique pharmacologic profile providing equipotent inhibition of EGFR, ErbB2, and ErbB3 signaling and showing greater antitumor activity than agents with a narrower spectrum of erbB receptor inhibition in specific preclinical models.Size PriceS1194 CUDC-101CUDC-101 has novel structure incorporating HDAC (IC50 4.4 nM) inhibitory functionality into the pharmacophore of the EGFR C50 2.4 nM) and HER2 (IC50 15.7 nM) inhibitors. CUDC-101 exhibits efficient antiproliferative activity with greater potency than vorinostat (SAHA), erlotinib, lapatinib. CUDC-101 inhibition in various cancer xenograft models including NSCLC, liver, breast, head and neck, colon, and pancreatic cancers.Size PriceNNHNOOHNOHOData from our customer Dr Meng Xiangbing, The University of Iowa.Effect of CUDC101 on the viability was detected by WST-1 method after 3 daystreatment in endometrial cancer cell line Hec50 and Ishikawa and ovarian cancer cell line SKOV3, Caov3 and PA1. S1023 Erlotinib HClErlotinib Hydrochloride inhibit activity against isolated tyrosine kinase(IC50, 2 nmol/L), to reduce HER1/EGFR autophosphorylation in intact human tumor cells in vitro (IC50, 20 nmol/L), and to inhibit the EGF-dependent proliferation of cells. It acts by inducing the expression of the cell-cycle inhibitor p27, and suppressing the expression of the cell-cycle promoter cyclin D1, thereby blocking cell-cycle progression at the G1 phase. Synonyms: Tarceva, CP-358774, OSI-774, NSC 718781Size PriceHNNN OOOOHClPC9 cellTime(hr)P-ERKT-ERKDUISP6GAPDH0E D Er3h 6hE D Er9hE D ErTime(hr) 0D T U3h 6hD T U9hD T UHCC827 cellP-EGFRVY-1068T-EGFRP-ERKT-ERKETS1DUSP6GAPDHBreast cancer cells were starved for 16 hrs, 100ng/ml EGF for 15 min with the indicated concentrationsProduced Independently by our customer Dr.Zhang, Tianjin Medical UniversityDownregulation of DUSP6 is directly dependent on inhibition of P-ERK/ETS1 signaling and only indirectly on inhibition of EGFR activity as demonstrated by DUSP6 expression in PC9 cells correlating closely with p-ERK activity.Data form Carcinogenesis Advance Access Published online on Jan. 2010 using our inhibitorDUSP6 is regulated by EGFR/ERK inhibition in NSCLC cell lines. Protein expression levels were assayed by immunoblot for phosphor-EGFR at indicated tyrosine sites, total-EGFR, phosphor-ERK, total-ERK, ETS1, DUSP6 and GAPDH demonstrating suppression of DUSP6 following inhibition of activated ERK (P-ERK) and ETS1 levels in the presence of appropriate drug for each of the following cell lines: HCC827 cells treated with erlotinibS1143 AG-490HOHONNHOAG490 is a member of the tyrphostin family of tyrosine kinase inhibitors. The most-studied targets of AG490 are the Janus kinases (JAKs: JAK-2, JAK3/STAT, JAK3/AP-1, and JAK3/MAPK), a family of tyrosine kinases that phosphorylate and thus activate the STAT transcription factors. AG490 inhibits the proliferation of several cell types including leukemia cells and fibroblasts. AG490 is also selective inhibitor of EGFR tyrosine kinase ,&YDOXHVDUHDQG0IRU(*)5DQG(UE%UHVSHFWLYHO\Synonyms: Tyrphostin AG490 Size PriceNNOONFHNNHOClS1194 CUDC-101FeedS1023 Erlotinib HydrochlorideFeedSynonyms: ZM 252868, AG 1517, Tyrphostin AG 1517 S1079 PD153035 HClPD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGFR stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2.NNHNOOBrHClData from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.Inhibition of orthopoxvirus replication and spreading correlates with blocking of(*)5VLJQDOLQJE\3'9DQGHWDQLEDQG*HWLQL:HVWHUQEORWRIFHOOlysates obtained from VACVplaque reduction tests for analysis of EGFR-ERK1/2signaling and VACV proteins. As an indicative band for VACV a 30KD a protein was depicted from detection of total VACV proteins by apolyclonal antibody in cell lysates of infected Hep2 cells.PD153035 Vandetanib Gefitinib Synonyms: ZM 252868, AG 1517, Tyrphostin AG 1517, SU 5271, PD 153035S2150 Neratinib Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Neratinib also inhibits the EGFR kinase and the proliferation of EGFR-dependent cells.N OHNON HN ClONNSynonyms: HKI-272Size PriceSize PriceS1079 PD153035 HydrochlorideFeedArd|oderes|s/Tvros|reK|raseSolutions to Signal Transduction Research4EGFRAcetyl-H3H3Breast Cancer Cell line MDA-MB-231CUDC101(M) 0 0.01 0. 1 1.0 10.0 20.05mg10mg25mg50mg100mg500mg25mg100mg200mg10mg50mg200mg5mg25mg100mg10mg50mg200mg EGFR Ard|oderes|s/Tvros|reK|rase5NNNH NN ClO NHOS1170 WZ3146WZ3146 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wildtype EGFR, than quinazoline-based EGFR inhibitors (HKI-272 and CL-387,785) in vitro. WZ3146 has a 300-fold lower half-maximum inhibitory concentration (IC50 100-fold selective with respect to PLk2, PLK3, and 48 other kinases tested.Size PriceONNHNHO NNN ON\l"NNNNSONH2OFF FCDK (Cyclin-dependent kinase)S1485 HMN-214HMN-214 is a potent PLK1 inhibitor (an average cell IC50 of 118 nM). HMN-176 interferes with PLK1, but does not appear to directly inhibit PLK1. Instead, it alters its spatial distribution, resulting in cell cycle arrest at the G2M phase, with destruction of the spindle polar bodies followed by DNA fragmentation. Drug-resistant cell lines showed low crossresistance to HMN-176. In human tumor xenografts, there was a broad spectrum of antitumor activity.Size PriceSynonyms: IVX-214S1362 ON-01910ON-01910 is a non-ATP-competitive small molecule Plk1 inhibitor with an IC50 of 9 nM. It induces mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis. In vivo, this compound did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a variety of xenograft models. ON01910 showed strong synergy with several chemotherapeutic agents, often inducing complete regression of tumors.Size PriceSynonyms: EstybonN NSOOOOOOO OSO OONHONaO S1524 AT7519 AT7519 is a novel small molecule multi-cyclin-dependent kinase inhibitor. It selectively binds to and inhibits CDKs, which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are serine/theronine kinases involved in regulation of the cell cycle and may be overexpressed in some types of cancer cells.Synonyms: AT 7519 Size Price Size PriceCl ClNH OHN NONHNHCe||Cvc|e/C|ec|po|rlSolutions to Signal Transduction Research20ROCK / PLK / CDK 10mg50mg100mg2mg50mg10mg50mg200mg5mg10mg50mg10mg50mg200mg10mg50mg200mg10mg50mg200mg5mg10mg25mgS1153 RoscovitineRoscovitine is a potent and selective inhibitor of CDKS. Roscovitine inhibits p34 cdc2/cyclin B (IC50 = 0.65 M), p33 CDK2/cyclin A (IC50 = 0.70 M), p33 CDK2/cyclin E (IC50 = 0.70 M), and p33 cdk2/p35(IC50 = 0.20 M) by competing for the ATP binding domain of these kinases. Roscovitine exhibits very low sensitivity towards related kinases, such as Erk1 and Erk2 (IC50 = 34 M and 14 M, respectively). Roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle.Synonyms: CYC202, SeliciclibSize PriceNNNNNHHOHNS1572 BS-181 HClBS-181 is a selective cyclin-dependent kinase inhibitor with an IC50 of 21 nM for the inhibition of CDK-activating kinase. Testing of other CDKs as well as another 69 kinases showed that BS-181 only LQKLELWHG&'.DWFRQFHQWUDWLRQVORZHUWKDQ0ZLWK&'.EHLQJLQKLELWHGIROGOHVVSRWHQWO\,&nM) than CDK7. In MCF-7 cells, BS-181 inhibited the phosphorylation of CDK7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.Size PriceNN NNHH2NHNHCl S2386 Indirubin ,QGLUXELQLVDSRWHQWF\FOLQGHSHQGHQWNLQDVHVDQG*6.LQKLELWRUZLWK,&RIDERXWQ0DQG0,WLQKLELWV&'.DQG*6.PHGLDWHGWDXSKRVSKRU\ODWLRQ$OVRLQKLELWV$03./&.DQG6*.,QGXFHVFHOOF\FOHDUUHVWDQGLQKLELWVFHOOSUROLIHUDWLRQ,QGLUXELQDOVRVXSSUHVVHGWKH1)%DFWLYDWLRQLQGXFHGE\YDULRXVinflammatory agents and carcinogens.Size PriceHNOHNO\l" S1230 FlavopiridolFlavopiridol inhibited rhabdoid cell growth (IC50-200nmol/L) , induced G1 and G2 arrest, and apoptosis in vitro in a concentration-dependent manner. These effects were correlated with the down-modulation of cyclin D1, up-regulation of p21, and induction of caspase 3/7 activities. Flavopiridol (at 7.5 mg/kg) significantly inhibited the growth of xenografted rhabdoid tumors, and its effect was correlated with the induction of p21 and down-modulation of cyclin D1.Synonyms: HMR-1275, Alvocidib, L868275Size PriceS1249 JNJ-7706621 JNJ-7706621 blocked proliferation of cancer cells regardless of their p53, retinoblastoma or P-glycoprotein status and induced cell death by activating apoptosis; delayed progression through G1 and arrested the cell cycle at the G2/M phase; decreased CDK1 kinase activity, altered CDK1 phosphorylation status and blocked signaling to downstream substrates of CDKs; reduced histone H3 phosphorylation; inhibited Aurora kinase. In YLWURFHOOSUROLIHUDWLRQDVVD\V,&PRO/+H/D,&+&7,&3&,&Size Price S1116 PD0332991 PD0332991 is an orally available pyridopyrimidine-derived CDK inhibitor with potential antineoplastic activity. 7KLVFRPSRXQGLVDKLJKO\VSHFLILFLQKLELWRURI&'.,&PRO/DQG&'.,&PRO/having no activity against a panel of 36 additional protein kinases. Therapeutic doses of PD0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and downregulation of genes under the transcriptional control of E2F.Size Price S1487 PHA-793887 PHA-793887 is a novel pan-cdk inhibitor, including CDK1, CDKT2, CDK4, CDK5, CDK7, and CDK9 with IC50 in the 5 to 140 nM range. It is inactive against other 34 kinases representative of all kinase families, in particular c-Abl, c-Kit, lck, and TRKA with IC5010 mM. It shows anti-proliferative activity against several solid tumor cell lines, with IC501 mM. In these cells, it is able to inhibit Rb phosphorylation and expression of S-phase cyclins, such as cyclin A.Size PriceOO OHHONHHOClHNNNNH NNN OOHNNNNOHNOData provided by our customer Pierre Roger,IRIBHM,ULB,BRUSSELS(Belgium).SH2NOONHN NNH2NFFOS1249 JNJ-7706621FeedProduced Independently by our customer Dr.Zhang, Tianjin Medical UniversityWestern blot analysis of p-Histone H3, Histone H3, p-Aurora A/B/C, $XURUD$0-1-ZDVDGGHGS1116 PD-0332991FeedSerum-deprived T98G glioma cells are restimulated with VHUXP)%6ZLWKRUZLWKRXW06HOOHFN3'CDK4/6 inhibitor.CDK Ce||Cvc|e/C|ec|po|rl2lHistone H3p-Histone H3Aurora Ap-Aurora A/B/C0M10M0.001M0.01M0.1M1M JNJ-770662110mg25mg50mg5mg25mg100mg10mg25mg50mg1mg5mg10mg5mg10mg25mg5mg10mg50mg10mg25mg50mgToll Free:(877)796-6397 www.selleckchem.com [email protected]:+1-832-582-8158---USA and Canada only---TopoisomeraseS1145 SNS-032SNS-032 is a small-molecule CDK inhibitor for the treatment of B-cell malignancies and advanced solid tumors. SNS-032 is a specific and potent inhibitor of CDK2, 7 and 9 which induces cell cycle arrest and apoptosis in tumor cell lines. It was shown to inhibit in vitro angiogenesis and prostaglandin E2 (PGE2) production, both strongly associated with tumorigenesis. Phase I clinical trials support the safety and tolerability of SNS-032 as evaluated in dose-escalation studies.Size PriceSynonyms: BMS-387032NOSNS HNONH S1208 Adriamycin Adriamycin is an anthracycline antibiotic and is used in cancer chemotherapy. It inhibits the progression of the enzyme topoisomerase II, which relaxes supercoils in DNA for transcription. Doxorubicin stabilizes the topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix from being resealed and thereby stopping the process of replication. It has an inhibitory effect on MCF-7 and 0'$0%ZLWK,&RIDQG0UHVSHFWLYHO\Synonyms: Doxorubicin, RubexSize Price S1288 Camptothecine Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I). It was isolated from the bark and stem of Camptotheca acuminata, a tree native in China. Two CPT analogues have been approved and are used in cancer chemotherapytoday, topotecan and irinotecan.Size Price S2217 Irinotecan HCl Trihydrate ,ULQRWHFDQK\GURFKORULGHWULK\GUDWHLVDWRSRLVRPHUDVH,LQKLELWRUZLWK,&RIDQG0IRU/R9RFHOOVand HT-29 cells, respectively. As a Topo I inhibitor, Irinotecan inhibits the religation step of the enzymes normal action, inducing single stranded DNA breaks. Irinotecan is activated by esterases to produce the activated metabolite and has been reported to be associated with cleavage of PARP in colon carcinoma cells.Synonyms: CPT 11, Camptosar, Campto, IrinotecanSize PriceO OOOHOHOOHOHNH2OHOOH.HClO NOOHO NN NOONNOOOOHH2OH2O H2OHCl\l"Microtubule S2209 Vinflunine Tartrate Vinflunine Tartrate is a new microtubule inhibitor with IC50 of 18.8 nM. Vinflunine suppressed the rate of WUHDGPLOOLQJ,& 02WKHUHIIHFWVVXFKDVLQGXFWLRQRIFHOOF\FOHDUUHVWDW*0GLVUXSWLRQRIWKHmicrotubular network of interphase cells and formation of paracrystals, generally required 3- to 17-fold higher concentrations of vinflunine than the other vinca alkaloids.Size PriceNNHHOHOOOOONHNFFOOHOOC COOHOHOH\l"\l" S1225 EtoposideEtoposide caused an increase in the mean fluorescence intensity of FasR in both subclones, and an induction of FasL in the ES subclone. However, no change in the numbers of apoptotic cells induced by etoposide was observed when FasR was blocked by an antagonist anti-Fas antibody, nor was an agonist anti-Fas antibody alone cytotoxic to the subclones or enhanced the cytotoxic effect of etoposide.Synonyms: Eposin, Vepesid, VP-16, ToposarSize PriceOOOOHOOHOHO OHOHOHOOHH S1198 Irinotecan Irinotecan is an inhibitor of topoisomerase I and is activated by hydrolysis to SN-38. The inhibition of topoisomerase I by the active metabolite SN-38 eventually leads to inhibition of both DNA replication and transcription. Its main use is in colon cancer, particularly in combination with other chemotherapy agents. The F\WRWR[LFLW\RILULQRWHFDQDQG61LQWKHWZRFHOOOLQHVZDVDVIROORZHGLULQRWHFDQ,&YDOXHVZHUH0IRU/R9RFHOOVDQG0IRU+7FHOOV61,&YDOXHVZHUHQ0IRU/R9RFHOOVDQGQ0IRUHT-29 cells.Synonyms: CamptosarSize Price S2485 Mitoxantrone Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 M, 0.42 mM for HepG2 and MCF-7/wt cells, respectively. It disrupts DNA synthesis and DNA repair in both healthy cells and cancer cells. It is used in the treatment of certain types of cancer, mostly metastatic breast cancer, acute myeloid leukemia, and non-Hodgkins lymphoma. It was also shown to improve the survival of children suffering from first relapse of acute lymphoblastic leukaemia.Size PriceN NOO NNOOOHOS1231 Topotecan HClTopotecan hydrochloride is a chemotherapy agent that is a topoisomerase I inhibitor. It is the water-soluble derivative of camptothecin. It is used to treat ovarian cancer and lung cancer, as well as other cancer types.Synonyms: Hycamtin, NSC 609699Size PriceNNOHNOOOHOHClOHOHOOHNHNHNOHNHOH Ce||Cvc|e/C|ec|po|rlSolutions to Signal Transduction Research22CDK / Topoisomerase / IicroIubule 25mg100mg200mg5mg10mg50mg500mg1g5g100mg200mg1g25mg100mg500mg100mg200mg1g100mg200mg250mg50mg100mg200mg10mg50mg200mg S2195 CYT997 CYT997, a synthetic small molecule optimized for antiproliferative activity in a panel of cell-based assays, in which the compound shows an IC50 of between 1 and 100 nmol/L across a panel of cancer cell lines. The FRPSRXQG LQKLELWV WKH SRO\PHUL]DWLRQ RI WXEXOLQ ZLWK DQ ,& RI PRO/ &