500586

JQ1 Enantiomers Set

• Synonyme(s) : JQ1 Enantiomers Set, (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, 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
• Formule empirique (notation de Hill): C₂₃H₂₅ClN₄O₂S
• Poids moléculaire : 456.99
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥96% (for both enantiomers, HPLC)
• Niveau de qualité: 100
• Forme: solid
• Puissance: 50 nM K_i
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow-white
• Solubilité: DMSO: 50 mg/mL (Each compound is soluble)
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

A 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 (K_D = 128.4 nM for human BD1; ΔT_m^obs = 6.47 and 7.97 °C, respectively, for human BD1 and BD2), BRD3 (K_D = 59.5 and 82.0 nM, respectively, for human BD1 and BD2), BRD4 (K_D = 49.0 and 90.1 nM, respectively, for human BD1 and BD2), and BRD6/BRDT (K_D = 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 M) 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.

A 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 M) 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).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
BRD4

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Forme physique

Set contains 5 mg each of (S)-(+)-JQ1 enantiomer (540696-5MG) and (R)-(-) JQ1 enantiomer (500585-5MG)

Reconstitution

Following reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

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.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids