Src Degrader

DAS-5-oCRBN is a PROTAC molecule with both c‑Src kinase inhibitory activity and target protein degradation activity, with an EC₅₀ of 45 nM for c‑Src binding. DAS-5-oCRBN binds non-covalently to Cereblon and mediates target protein degradation via the ubiquitin-proteasome pathway. DAS-5-oCRBN can catalytically deplete intracellular c‑Src protein, while blocking both the kinase catalytic function of c‑Src and the non-catalytic protein interactions mediated by its SH2 and SH3 domains. DAS-5-oCRBN inhibits tumor cell proliferation and exerts significant anti-proliferative effects on both c‑Src kinase activity-dependent MDA-MB-231 cells and c‑Src protein level-dependent CAL51 cells. DAS-5-oCRBN can be used in cancer-related research such as studies on triple-negative breast cancer and chronic myeloid leukemia.

BLK degrader 1 (compound 9) is a selective degrader of B-lymphoid tyrosine kinase (BLK). BLK degrader 1 shows anticancer activity in several B-lymphoid cell lines.

DB0662 is a multi-target kinase-directed PROTAC degrader, targeting kinases including PTK2B, MAPK9, BLK, CSK, LIMK1, etc.

SJ45566 a potent and orally active PROTAC-based LCK degrader, with a DC₅₀ of 1.21 nM. SJ45566 can be used in the research for T‑Cell Acute Lymphoblastic Leukemia.

PROTAC DDa-1 is a multi-targeted DCAF1-recruiting tyrosine kinase PROTAC degrader. PROTAC DDa-1 mediates the degradation of TNK2, CSK, LIMK2, TEC, and BTK, with a DC₅₀ of 90 nM for BTK. PROTAC DDa-1 reduces the viability of BTK-dependent diffuse large B-cell lymphoma cells. PROTAC DDa-1 can be used for the research of diffuse large B-cell lymphoma.

Lck degrader-1 (Compound 17) is a molecular glue degrader targeting lymphocyte-specific protein tyrosine kinase (LCK) (DC₅₀=23.1 nM). Lck degrader-1 is promising for research of T-cell acute lymphoblastic leukemia (T-ALL).