SIM1 is a potentvon Hippel-Lindau(VHL)-based trivalentPROTACcapable of degradation for allBETfamily members, with preference forBRD2degradation (IC₅₀=1.1 nM;Kd=186 nM). SIM1 shows sustained anti-cancer activity^[1].

SIM1 (1 nM; 30 hours; MV4-11 cells) results in measurable cellular death after 6 hours^[1].
SIM1 (1 μM; 4 hours; HEK293 cells) degrades BET proteins^[1].
SIM1 induces conformational changes upon binding to the BET protein to simultaneously engage with high avidity both its bromodomains in a cis intramolecular fashion. SIM1 engages BD1 and BD2 intramolecularly and forms a 1:1:1 ternary complex with VHL and BRD4^[1].

1618.81

Solid

C₇₉H₉₈Cl₂N₁₄O₁₃S₃

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

DMSO : 100 mg/mL(61.77 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。