_-_-Talarozole_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Data SheetBIOLOGICAL ACTIVITY: Alpha–cyperone is associated with the down–regulation of COX–2,IL–6,Nck–2,Cdc42 and Rac1, resulting in reduction of inflammation.which would be highly beneficial for treatment of inflammatory diseases such as AD.In vitro: The anti–inflammatory activity of alpha–cyperone is associated with the down–regulation of COX–2 and IL–6 via the negativeregulation of the NFκB pathway in LPS–stimulated RAW 264.7 cells.[1] Alpha–Cyperone binds and interacts with tubulin and is capableof distinctly destabilizing microtubule polymerization. The effect of this interaction could result in reduction of inflammation whichwould be highly beneficial for treatment of inflammatory diseases such as AD. One microliter of alpha–Cyperone was dissolved inDMSO (1:1 v/v) and it was further diluted in double distilled water (ddH2O) to a final volume of 20 microliter. [2]References: [1]. Jung, S. H. et al. alpha–Cyperone, isolated from the rhizomes of Cyperus rotundus, inhibits LPS–induced COX–2 expression and PGE2 production throughthe negative regulation of NFkappaB signalling in RAW 264.7 cells. Journal of ethnopharmacology 147, 208–214, doi:10.1016/j.jep.2013.02.034 (2013).[2]. Azimi, A. et al. alpha–Cyperone of Cyperus rotundus is an effective candidate for reduction of inflammation by destabilization of microtubule fibers inbrain. Journal of ethnopharmacology, doi:10.1016/j.jep.2016.06.058 (2016).Product Name:alpha–CyperoneCat. No.:HY-N0710CAS No.:473-08-5Molecular Formula:C15H22OMolecular Weight:218.33Target:OthersPathway:OthersSolubility: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,

Inhibitors, Agonists, Screening

Safety Data SheetRevision Date:Sep.-22-2017Print Date:Sep.-22-2017

1. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :Fadrozole

Catalog No. :HY-14247A

CAS No. :102676-47-11.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USA

Tel:609-228-6898

Fax:609-228-5909

E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-6898

2. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.

Inhibitors, Agonists, Screening Data Sheet

BIOLOGICAL ACTIVITY: Tamoxifen Citrate is an antiestrogen by inhibiting the binding of estrogen to estrogen receptors.IC50 & Target: Estrogen receptor[1]In Vitro: Tamoxifen shows strong inhibition of MCF–7 cells (EC50=1.41 μM) and to a lesser extent the T47D cells (EC50=2.5 μM) butdoes not affect the MDA–MB–231 cells[2]. In Vivo: The Tamoxifen–inducible gene knockout strategy has clear advantages in that expression of a gene can be ablated in adultmice at will in a tissue specific manner. To study the role of Med1 in adult heart, 7–week old TmcsMed1–/– mice are given a dailyIintraperitoneal injection of Tamoxifen at a dose of 65 mg/kg for 5 days and killed at selected intervals thereafter. qPCR analysis ofRNA shows that the Med1 expression begin to decrease after 3 days of Tamoxifen injection (about 70% decrease), and by 5 days ofinjection, Med1 expression is almost non–detectable in the heart. Tamoxifen–inducible cardiac–specific disruption of Med1(TmcsMed1–/–) in adult mice causes dilated cardiomyopathy[3].PROTOCOL (Extracted from published papers and Only for reference) Animal Administration: Tamoxifen is dissolved in DMSO and diluted with PBS before use (Mice)[3].[3]Mice[3]Seven–week old TmcsMed1–/– mice and the wild–type littermates are then administered Tamoxifen intraperitoneally at a daily doseof 65 mg/kg body weight for 5 days and then killed at selected intervals after initiation of Tamoxifen treatment. For eachexperiment 3 to 5 mice for control and csMed1–/– are used. To obtain survival curve 41 csMed1–/– and 41 csMed1fl/fl mice areused. Thirteen TmcsMed–/– mice and the same number of littermates are used for the survival curve experiments using Tamoxifeninducible model. The specific criteria for animal euthanasia included absence of food or water intake, slow or no mobility, weak orabsence of heart beat, absence of palpitation of the chest as well as absence of respiratory movement. Mice are euthanized byintraperitoneal pentobarbital injection at the dose of 150mg/kg body weight to minimize suffering.References: [1]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609–18.[2]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth–inhibitory effects of styrylpyrone derivative (SPD) and assessment ofits antiestrogenicity. Anticancer Res. 1998 Nov–Dec;18(6A):4383–6.[3]. Jia Y, et al. Cardiomyocyte–Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016Aug 22;11(8):e0160755.Product Name:Tamoxifen (Citrate)Cat. No.:HY-13757CAS No.:54965-24-1Molecular Formula:C32H37NO8Molecular Weight:563.64Target:Autophagy; Estrogen Receptor/ERRPathway:Autophagy; OthersSolubility:DMSO: ≥ 570 mg/mL

Inhibitors, Agonists, Screening Data SheetBIOLOGICAL ACTIVITY: Clofarabine(Clolar; Clofarex) inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.IC50 Value: 65 nMTarget:in vitro: Clofarabine is a second generation purine nucleoside analog with antineoplastic activity. It is phosphorylated intracellularly,which inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase, resulting in inhibition of DNArepair and synthesis of DNA and RNA. This nucleoside analog also disrupts mitochondrial function and membrane integrity, resultingin the release of pre–apoptotic factors, including cytochrome C and apoptotic–inducing factor, which activate apoptosis.in vivo: Clofarabine is used for treating relapsed or refractory acute lymphoblastic leukaemia (ALL) in children, after at least two othertypes of treatment have failed.References: [1]. Bonate et al Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat.Rev.Drug Discov. (2006)5 855.[2]. Ghanem H, Kantarjian H, Ohanian M, Jabbour E.The Role of Clofarabine in Acute Myeloid Leukemia.Leuk Lymphoma. 2012 Sep 7.[3]. Abd Elmoneim A, Gore L, Ricklis RM, Boklan J, Cooper T, Narendran A, Rolla K, Scott T, Arceci RJ.Phase I dose–escalation trial of clofarabine followed byescalating doses of fractionated cyclophosphamide in children with relapsed or refractory acute leukemias.Pediatr Blood Cancer. 2012 Aug 8. doi:10.1002/pbc.24264.[4]. Thudium KE, Ghoshal S, Fetterly GJ, Haese JP, Karpf AR, Wetzler M.Synergism between clofarabine and decitabine through p53R2: A pharmacodynamicdrug–drug interaction modeling.Leuk Res. 2012 Aug 9.[5]. Aye Y, Brignole EJ, Long MJ, Chittuluru J, Drennan CL, Asturias FJ, Stubbe J.Clofarabine Targets the Large Subunit (α) of Human Ribonucleotide Reductasein Live Cells by Assembly into Persistent Hexamers.Chem Biol. 2012 Jul 27;19(7):799–805.Product Name:ClofarabineCat. No.:HY-A0005CAS No.:123318-82-1Molecular Formula:C10H11ClFN5O3Molecular Weight:303.68Target:Nucleoside Antimetabolite/Analog; AutophagyPathway:Cell Cycle/DNA Damage; AutophagySolubility:10 mM in DMSO