500586 | JQ1 Enantiomers Set - Calbiochem

500586
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      500586-1SET
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service

          Glass bottle 1 set
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          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®
          Synonyms(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, BRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          Data Sheet

          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
          Synonyms(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, BRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I
          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 -20°C
          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.
          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.