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500586 JQ1 Enantiomers Set - Calbiochem

JQ1 Enantiomers Set - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

500586
  
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Přehled

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®
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
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
Katalogové číslo GTIN
500586 0

Documentation

JQ1 Enantiomers Set - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Přehled odkazů
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 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.