- 商品介绍
- 规格参数
- 包装参数
Application
SIM1 is suitable for use to study intracellular degradation of BET proteins, and to produce a trivalent PROTAC with enhanced target degradation.
Biochem/physiol Actions
SIM1, a PROTAC degrader, is a highly potent bromo and extra terminal (BET) protein degrader (BRD2/3/4 Dmax50 = 57.3/413.9/96.3 pM post 22h using HEK293 expressing respective BRD; BRD2/3/4 λmax/h = 2.8/1.2/1.9 nM) that corresponds to a trivalent chimera composed of a Von Hippel Lindau (VHL) E3 ligase-targeting ligand linked to two molecules of BET inhibitor (+)-(S)-JQ1. Compared to bivalent degraders, SIM1 shows higher and more sustained degradation efficacy by simultaneously engaging two BET bromodomains with high avidity in a cis intramolecular fashion, exhibiting positive cooperativity, leading to more potent anticancer activity (MV4;11 AML viability IC50 = 1.1 nM/SIM1 vs 11.3 nM/MZ1 post 48h treatment). SIM1 is found to interact with the BD2 and BD1 bromodomains of BRD4, creating a ternary complex with VHL and BRD4. This interaction increases target binding valency and extends the duration of specific molecular interactions with the target.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| 长度(mm) | |
| 宽度(mm) | |
| 高度(mm) | |
| 重量(kg) |
-
询价
-
¥ 1148.92
-
¥ 1451.54
-
询价
-
询价
-
询价
-
询价
-
¥ 8520.40
-
¥ 8135.09
-
询价
-
询价
-
¥ 15214.65
-
¥ 3319.60
-
询价
-
¥ 1564.00
-
¥ 1156.91
-
¥ 8137.12
-
¥ 2406.69
-
¥ 954.17
-
¥ 10685.48
微信小程序
7X24小时在线咨询