SJG-136

SJG-136 is a rationally designed, sequence-selective DNA minor groove binding agent belonging to the pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimer class. It covalently binds to purine-GATC-pyrimidine sequences in the minor groove of DNA, forming interstrand cross-links by targeting the N2 positions of guanines on opposite strands. This cross-linking inhibits both DNA replication and gene transcription, leading to potent antitumor activity and apoptosis in cancer cells. Notably, its cytotoxicity is not diminished by p53 mutations or prior treatment history in B-cell chronic lymphocytic leukemia (B-CLL) cells and appears resistant to p53-mediated excision repair mechanisms. SJG-136 has been investigated primarily for hematologic malignancies such as acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), myelodysplastic syndromes (MDS), as well as solid tumors like recurrent ovarian epithelial cancer and fallopian tube cancer[2][3][4][5][6].

Other names

DNA minor groove binding agent SG2000