1. PROTAC
    Epigenetics
  2. PROTAC
    Epigenetic Reader Domain
  3. SIM1

SIM1 

Cat. No.: HY-141438
Handling Instructions

SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity.

For research use only. We do not sell to patients.

SIM1 Chemical Structure

SIM1 Chemical Structure

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Description

SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity[1].

IC50 & Target

BRD2

1.1 nM (IC50)

BRD2

186 nM (Kd)

BRD3

 

BRD4

 

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 1 nM
Incubation Time: 30 hours
Result: Resulted in measurable cellular death after 6 hours.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 1 µM
Incubation Time: 4 hours
Result: Degraded BET proteins.
Molecular Weight

1618.81

Formula

C₇₉H₉₈Cl₂N₁₄O₁₃S₃

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Product Name:
SIM1
Cat. No.:
HY-141438
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