SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation ( IC 50 =1.1 nM; Kd =186 nM). SIM1 shows sustained anti-cancer activity
In Vitro
SIM1 (1 nM; 30 hours; MV4-11 cells) results in measurable cellular death after 6 hours. SIM1 (1 µM; 4 hours; HEK293 cells) degrades BET proteins. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MV4-11 cells Concentration: 1 nM Incubation Time: 30 hours Result: Resulted in measurable cellular death after 6 hours. Western Blot AnalysisCell Line: HEK293 cells Concentration: 1 µM Incubation Time: 4 hours Result: Degraded BET proteins.
SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation ( IC 50 =1.1 nM; Kd =186 nM). SIM1 shows sustained anti-cancer activity.
보관 조건
Protected from light,Store at -20°C,Argon charged
배송
Ice chest + Ice pads
이 제품은 콜드 체인 배송이 필요합니다.지상 및 기타 경제 서비스는 사용할 수 없습니다.
순수함
≥99%
이름과 식별자
분자량
1618.81
고급 데이터
인증서(CoA, COO, BSE/TSE 및 분석 차트)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
화학 및 물리적 특성
용해성
DMSO : 100 mg/mL (61.77 mM; Need ultrasonic)
솔루션 계산기
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.
Products are supplied to verified businesses, institutions, and qualified professionals for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
