2929304-05-0
Chemical Structure
UNC8732
- CAS No.: 2929304-05-0
- Formula:C35H39N5O5
- Molecular Weight:609.71
InChIKey: CSTHTJLTORVUST-UHFFFAOYSA-N
SMILES: O=C(N1)COC2=C1C=CC(C(N(C3CC3)CC4=CC=C(C(NC5=CC=C(CN(C(CCCCCN)=O)CC6)C6=C5)=O)C=C4)=O)=C2
Biological Activity: UNC8732 is an NSD2 degrader with a Kd value of 76 nM for NSD2, and achieves highly selective degradation of NSD2 across the detectable proteome. UNC8732 acts as a prodrug; its primary amine is metabolized to an aldehyde, which forms a reversible covalent interaction with Cys326 in the FIST_C domain of FBXO22, recruiting the SCFFBXO22 ubiquitin ligase complex to mediate polyubiquitination and proteasomal degradation of NSD2. UNC8732 serves as a chemical probe to investigate NSD2-associated disease phenotypes and study the functions of NSD2 in nuclear signaling and epigenetics. UNC8732 can be used in studies of acute lymphoblastic leukemia[1].
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UNC8732 | UNC8732 is an NSD2 degrader with a Kd value of 76 nM for NSD2, and achieves highly selective degradation of NSD2 across the detectable proteome. UNC8732 acts as a prodrug; its primary amine is metabolized to an aldehyde, which forms a reversible covalent interaction with Cys326 in the FIST_C domain of FBXO22, recruiting the SCFFBXO22 ubiquitin ligase complex to mediate polyubiquitination and proteasomal degradation of NSD2. UNC8732 serves as a chemical probe to investigate NSD2-associated disease phenotypes and study the functions of NSD2 in nuclear signaling and epigenetics. UNC8732 can be used in studies of acute lymphoblastic leukemia. | |||||||||||||||||||||
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Keywords
