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Product Description
– (S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM[1]. (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Web ID
– HY-130654
Shipping
– Room temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C33H49N7O8S
References
– [1]Wang S, et al. Uncoupling of PARP1 trapping and inhibition using selective PARP1 degradation. Nat Chem Biol. 2019 Dec;15(12):1223-1231.
CAS Number
– 2597167-24-1
Molecular Weight
– 703.85
SMILES
– CC(C)([C@H](NC(CCOCCOCCOCCOCCN=[N+]=[N-])=O)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)=O)C
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– E3 Ligase Ligand-Linker Conjugates
Isoform
– von Hippel-Lindau (VHL)
Pathway
– PROTAC
Product type
– Reference compound
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