Colibactin 742 

Colibactin 742 is a covalently binding DNA-damaging agent targeting DNA, with an IC₅₀ of 5.2 μM against human cervical cancer cells (HeLa). Colibactin 742 covalently binds to DNA, forming interstrand crosslinks (ICLs), activating the Fanconi anemia DNA repair pathway, inducing γH2AX and FANCD2 foci formation and cell cycle arrest, while exacerbating mismatch repair deficiency (MMRd)-related mutations. Colibactin 742 can mimic the genotoxicity of natural Colibactin while avoiding its instability, and is mainly used in colorectal cancer (CRC) related research, including microbial tumorigenesis mechanisms, DNA damage repair pathways, and mutation signature analysis^[1][2][3].

Colibactin 742 (100 nM-100 μM; 1.5 hours) induces stable DNA interstrand crosslinks (ICLs) using linearized pUC19 DNA as a substrate at both pH 5.0 and pH 7.0, and its activity is superior to Colibactin 770 (3a) at pH 5.0^[1].
Colibactin 742 (1-100 μM; 4 hours treatment followed by 20 hours incubation) increases the number of FANCD2 and γH2AX foci-positive cells by 4 times at 11 μM in HeLa cells, and induces cell death at >33 μM^[1].
Colibactin 742 (24 nM-100 μM; 72 hours) is cytotoxic to HeLa cells with an IC₅₀ of 5.2 μM^[1].
Colibactin 742 (10 μM, 100 μM; 4 hours, 12 hours) activates the p53 signaling pathway and induces cell cycle arrest, senescence, ER stress, and the IL-1 inflammatory pathway in FHC cells, upregulating the expression of genes such as CDKN1A, BTG2, and FAS^[2].
Colibactin 742 (20 μM; 48 hours/10 times, with 48-96 hour intervals) upregulates BRCA1 and Fanconi in HCT 116 cells." Anemia, mismatch repair (MMR), and IFNL1-related pathway gene expression increase T>N ??single-base substitutions (SBS) and short insertion-deletion (Indel) mutations^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Colibactin 742 (7.42 μg/larva, approximately 30 mg/kg; i.p.; single dose; 24 hours) increases the degree of cuticle melanization in normal Galleria mellonella larvae, leading to DNA damage in larval intestinal epithelial cells, with increased DNA strand breaks observed in the comet assay^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

742.91

C₃₇H₄₂N₈O₅S₂

2916559-62-9

O=C(NCC1=NC(CCC2=NC(C3(O)CNC(C3C4=C(C5=N[C@@H](C)CC5)C(N[C@]46CC6)=O)=O)=CS2)=CS1)CC([C@@]7(CC7)N8)=C(C9=N[C@@H](C)CC9)C8=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wernke KM, et al. Probing Microbiome Genotoxicity: A Stable Colibactin Provides Insight into Structure-Activity Relationships and Facilitates Mechanism of Action Studies. J Am Chem Soc. 2021 Sep 29;143(38):15824-15833.  [Content Brief]

  [2]. Dougherty MW, et al. The microbial genotoxin colibactin exacerbates mismatch repair mutations in colorectal tumors. Neoplasia. 2023 Sep;43:100918.  [Content Brief]

  [3]. Agrawal R, et al. Colibactin Exerts Androgen-dependent and -independent Effects on Prostate Cancer. Eur Urol Oncol. 2025 Jun;8(3):716-730.  [Content Brief]