Compound class:
Synthetic organic
Comment: EG-001's chemical structure was derived from that of the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib [1], but it does not inhibit BTK or any other kinase. It has potent anti-proliferative and anti-tumour effects in vivo, against a wide range of lymphomas and leukaemias. A preprint has reported the molecular mechanism of EG-001 [2]; it acts to convert the auto-inhibited (closed) form of the Wiskott-Aldrich syndrome protein (WASp; WAS; P42768) to its activated allosteric conformation. WASp is one of a family of actin/cytoskeleton-regulating proteins that is expressed only in cells of haematopoietic origin. Activated WASp increases actin polymerisation (via interactions with the Arp2/3 complex), induces cytoskeleton reorganisation, and promotes cell death.
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Classification | |
Compound class | Synthetic organic |
IUPAC Name |
1-[(4-phenoxyphenyl)methyl]-3-(1-prop-2-enoylpiperidin-3-yl)pyrido[3,2-d]pyrimidine-2,4-dione |
Database Links | |
GtoPdb PubChem SID | 479821106 |
PubChem CID | 139552342 |
Search Google for chemical match using the InChIKey | JBKILBGEQHFIOB-UHFFFAOYSA-N |
Search Google for chemicals with the same backbone | JBKILBGEQHFIOB |
UniChem Compound Search for chemical match using the InChIKey | JBKILBGEQHFIOB-UHFFFAOYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | JBKILBGEQHFIOB-UHFFFAOYSA-N |