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Tocris Bioscience™ SIM1

Réf. : BL-RE-125770Réf. fabricant : 18769606 5 mg
407,12 € HT

Potent and selective trivalent BET Bromodomain Degrader (PROTAC™)

Nom chimique ou matériau
N,N'-(11-((2-((-1-((2 S,4 R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(2-(-4-(4-chlorophenyl)-2,3,9-tri
Quantité
5 mg
Cible
Active Degraders
Formule moléculaire
C79H98Cl2N14O13S3
Pureté
0.98
Marque
Tocris Bioscience

SIM1 is a potent and selective trivalent PROTAC™ Degrader based on BET bromodomain inhibitors linked to a Von Hippel Lindau (VHL) ligand via branched linkers. SIM1 degrades all BET family proteins with a preference for BRD2 (DC50 values = 0.7 nM, 1.1 nM and 3.3 nM for BRD4, BRD2 and BRD3, respectively). SIM1 degrades BRD2 more significantly and rapidly than BRD3 and BRD4, and degrades BET proteins with a higher potency than a bivalent degrader. SIM1 also decreases protein levels for Myc and HMOX1 and induces apoptosis in prostate cancer cells.

Caractéristiques techniques

MarqueTocris Bioscience
Réf. B-LABOBL-RE-125770
Réf. fabricant18769606
Nom chimique ou matériauN,N'-(11-((2-((-1-((2 S,4 R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(2-(-4-(4-chlorophenyl)-2,3,9-tri
Quantité5 mg
CibleActive Degraders
Formule moléculaireC<sub>79</sub>H<sub>98</sub>Cl<sub>2</sub>N<sub>14</sub>O<sub>13</sub>S<sub>3</sub>
Pureté0.98
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