1. Signaling Pathways
  2. Antibody-drug Conjugate/ADC Related
  3. Drug-Linker Conjugates for ADC
  4. Pyrrolobenzodiazepines Isoform

Pyrrolobenzodiazepines

Pyrrolobenzodiazepines (PBDs) are sequence-selective DNA minor-groove binding agents that covalently attach to guanine bases and create durable DNA damage[1]. Mechanistically, PBD dimers form non-distorting interstrand cross-links, while SJG-136 reacts with guanine bases in the 5′-GATC-3′ sequence and shows higher cytotoxicity than melphalan in CHO repair models[2][3]. In cancer research, PBDs have progressed from natural products to synthetic monomers, hybrids, dimers, and antibody-drug conjugate (ADC) payloads[1][4]. Compared with related DNA-binding systems, PBD activity differs from duocarmycin or CC-1065 analogs that alkylate adenine-rich minor-groove sites, and PBDs show insignificant affinity for most DNA G-quadruplexes without large C8 substituents[5][6]. For experimental applications, linker length and guanine spacing shape PBD dimer adduct patterns, supporting rational design of sequence-selective DNA cross-linking agents and ADC payloads[7][8].

Pyrrolobenzodiazepines Related Products (4):

Cat. No. Product Name Effect Purity
  • HY-128952
    Tesirine
    98.31%
    Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity.
  • HY-101162
    SGD-1910
    SGD-1910 is a agent-linker conjugate for ADC by using the antitumor antibiotic, pyrrolobenzodiazepine (PBD, a cytotoxic DNA crosslinking), linked via the cleavable linker MC-Val-Ala.
  • HY-126685
    Mal-PEG4-VA-PBD
    Mal-PEG4-VA-PBD is a agent-linker conjugate for ADC by using the antitumor antibiotic, Pyrrolobenzodiazepine (PBD), linked via Mal-PEG4-VA.
  • HY-128952G
    Tesirine (GMP)
    Tesirine (GMP) (SG3249 (GMP)) is Tesirine (HY-128952) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity.