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 ; 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
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
BRD2; BRD3; BRD4
Frequently Asked Questions
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