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AB3067

AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM[1]. (Pink: ligand for target protein (HY-131633A) ; Black: linker (HY-170391) ; Blue: ligand for E3 ligase VHL (HY-112078) and CRBN (HY-W998346) )

Product Specifications

UNSPSC

12352005

Target

Epigenetic Reader Domain; PROTACs

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C(OCCOCCOCCOCC(C)(COCCOCCOCCNC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1F)COCC(N[C@H](C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)C(C)(C)C)=O)C[C@H]7C8=NN=C(C)N8C9=C(C(C)=C(C)S9)C(C%10=CC=C(Cl)C=C%10)=N7

Molecular Formula

C74H91ClFN11O17S2

Molecular Weight

1525.16

References & Citations

[1]Bond AG, et al., Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera. J Am Chem Soc. 2024 Dec 11;146 (49) :33675-33711.

Shipping Conditions

Room temperature

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-170390/

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

BRD2; BRD3; BRD4

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