PROTAC BRD4 Degrader-39 

PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC₅₀ value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer^[1]. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))

PROTAC BRD4 Degrader-39 (Compound NG-2) (0.01-10 μM, 3-48 h) degrades BRD4 in a concentration- and time-dependent manner in MDA-MB-231 cells^[1].
PROTAC BRD4 Degrader-39 degrades BRD4 depending on GLUTs and proteasome in MDA-MB-231 cells^[1].
PROTAC BRD4 Degrader-39 (5-5000 nM, 3 h) degrades BRD4 in MDA-MB-157, MCF-7, T-47D and BEAS-2B cells^[1].
PROTAC BRD4 Degrader-39 is difficult to be recognized by P-gp, thereby effectively evading the efflux effect in Caco-2 cells^[1].

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

PROTAC BRD4 Degrader-39 (Compound NG-2) (2.5 mg/kg, i.p., every other day for 14 times) inhibits tumor growth in MDA-MB-231 tumor mice models^[1].

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

1410.10

C₆₃H₈₁ClN₁₂O₁₅S₄

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Room temperature in continental US; may vary elsewhere.

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

• [1]. Gao Y, et al. GLUTs-Facilitated Targeting BRD4 Degradation in Breast Cancer through Carbohydrate-Conjugated PROTACs. J Med Chem. 2025 Aug 28;68(16):17046-17064.