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500586 JQ1 Enantiomers Set - Calbiochem

JQ1 Enantiomers Set - Calbiochem: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: BRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I, (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate, SGCBD01

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      Übersicht

      Replacement Information
      Description
      OverviewA cell-permeable I-BET (Cat. No. 401010) class of thienodiazepine derivative whose (S)-(+), but not (R)-(-), enantiomer is shown to target both bromodomains (BD1 & BD2) of BET family members BRD2, BRD3, BRD4, and BRD6/BRDT in a Kac- (ε-N-acetylated lysine) competitive manner, exhibiting little affinity toward 23 other BD-containing proteins, BRD1 and BRD9, and little or no activity against a panel of more than 50 receptors, ion channels, and transporters. Effectively inhibits the oncogenic BRD4-NUT fusion-dependent NUT midline carcinoma and c-Myc oncoprotein-dependent multiple myeloma proliferation both in cultures (IC50 <1 µM) in vitro and in mice (50 mg/kg/day i.p.) in vivo. Also reported to cross the blood-testis boundary in male mice and effectively block BRDT-mediated spermatogenesis without affecting hormone levels. The set contains 5 mg of the active (S)-(+)-JQ1 (540696) and 5 mg of the inactive (R)-(-) enantiomer (500585).
      Catalogue Number500586
      Brand Family Calbiochem®
      SynonymsBRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I, (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate, SGCBD01
      References
      ReferencesMatzuk, M. M., et al. 2012. Cell. 150, 673.
      Delmore, J. E., et al. 2011 Cell. 146, 904.
      Filippakopoulos, P., et al. 2010. Nature. 468, 1067.
      Product Information
      FormYellowish white solid
      FormulationSet contains 5 mg each of (S)-(+)-JQ1 enantiomer (540696-5MG) and (R)-(-) JQ1 enantiomer (500585-5MG)
      Hill FormulaC₂₃H₂₅ClN₄O₂S
      Chemical formulaC₂₃H₂₅ClN₄O₂S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetBRD4
      Primary Target K<sub>i</sub>50 nM, IC₅₀
      Purity≥96% by HPLC for both enantiomers
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      500586 0

      Documentation

      JQ1 Enantiomers Set - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Matzuk, M. M., et al. 2012. Cell. 150, 673.
      Delmore, J. E., et al. 2011 Cell. 146, 904.
      Filippakopoulos, P., et al. 2010. Nature. 468, 1067.
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision31-October-2016 JSW
      SynonymsBRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I, (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate, SGCBD01
      DescriptionA cell-permeable I-BET (Cat. No. 401010) class of thienodiazepine derivative whose (S)-(+), but not (R)-(-), enantiomer is shown to target both bromodomains (BD1 & BD2) of BET (bromodomain and extra terminal) family members BRD2 (KD = 128.4 nM for human BD1; ΔTmobs = 6.47 and 7.97 °C, respectively, for human BD1 and BD2), BRD3 (KD = 59.5 and 82.0 nM, respectively, for human BD1 and BD2), BRD4 (KD = 49.0 and 90.1 nM, respectively, for human BD1 and BD2), and BRD6/BRDT (KD = 190.1, 44.1, 77.5, and 59.2 nM, respectively, for human BD1, human BD2, murine BD1, and murine BD2) in a Kac- (ε-N-acetylated lysine) competitive manner, exhibiting little affinity toward 23 other BD-containing proteins, including the single BD-containing BRD1 and BRD9, and little or no activity against a panel of more than 50 receptors, ion channels, and transporters. Effectively inhibits the oncogenic BRD4-NUT (Nuclear protein in testis) fusion protein-dependent NMC (NUT midline carcinoma) and c-Myc oncoprotein-dependent MM (multiple myeloma) proliferation both in cultures (IC50 <1 µM) in vitro and in mice (50 mg/kg/day i.p.) in vivo. Also reported to cross the blood-testis boundary in male mice and effectively reduce testis mass, sperm count and motility (50 mg/kg; b.i.d. i.p.) in a reversible manner by targeting BRDT-mediated spermatogenesis without interfering hormone levels.
      FormYellowish white solid
      FormulationSet contains 5 mg each of (S)-(+)-JQ1 enantiomer (540696-5MG) and (R)-(-) JQ1 enantiomer (500585-5MG)
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₃H₂₅ClN₄O₂S
      Structure formulaStructure formula
      Purity≥96% by HPLC for both enantiomers
      SolubilityEach compound is soluble at 50 mg/ml in DMSO.
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesMatzuk, M. M., et al. 2012. Cell. 150, 673.
      Delmore, J. E., et al. 2011 Cell. 146, 904.
      Filippakopoulos, P., et al. 2010. Nature. 468, 1067.