2-(1-(Thiophen-2-yl)ethylidene)hydrazinecarbothioamide is an antimicrobial agent.{58140} It is active against the Gram-negative bacteria E. coli, P. aeruginosa, and S. marcescens (MICs = 64, 100, and 70 μg/ml, respectively), the Gram-positive bacteria S. aureus, M. luteus, and B. cereus (MICs = 130, 100, and 50 μg/ml, respectively), and the fungi C. albicans, G. candidum, T. rubrum, F. oxysporum, A. flavus, and S. brevicaulis (MICs = 69-120 μg/ml). 2-(1-(Thiophen-2-yl)ethylidene)hydrazinecarbothioamide is also a precursor in the synthesis of other antimicrobial agents, as well as compounds with anticancer activity.{58140,58141}
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An antimicrobial agent; active against Gram-negative bacteria (MICs = 64-100 μg/ml), Gram-positive bacteria (MICs = 50-130 μg/ml), and fungi (MICs = 69-120 μg/ml); a precursor in the synthesis of other antimicrobial agents, as well as compounds with anticancer activity
Formal name: 2-[1-(2-thienyl)ethylidene]-hydrazinecarbothioamide
Synonyms: 1-(Thiophen-2-yl)ethanone thiosemicarbazone|NSC 707
Molecular weight: 199.3
CAS: 5351-71-3
Purity: ≥95%
Formulation: A crystalline solid
The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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