Discoidin Domain Receptor Degrader

LLC355 is a discoidin domain receptor 1 (DDR1) ATTEC degrader with a DC₅₀ of 150.8 nM. LLC355 induces DDR1 protein degradation via lysosome-mediated autophagy. LLC355 inhibits the tumorigenicity, migration and invasion abilities of cancer cells, and induces apoptosis. LLC355 is applicable to research related to non-small cell lung cancer and pancreatic cancer.

PROTAC DDR1 degrader-1 is a potent and selective DDR1-targeting PROTAC degrader. PROTAC DDR1 degrader-1 selectively induces full-length DDR1 degradation via the ubiquitin proteasome system, blocking downstream signaling pathways. PROTAC DDR1 degrader-1 inhibits tumor cell migration and invasion. PROTAC DDR1 degrader-1 exhibits anti-tumor activity in mice. PROTAC DDR1 degrader-1 can be used for the research of DDR1-driven cancers.

SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC₅₀ of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)