Chetomin, Chaetomium sp.

A cell-permeable antimicrobial that disrupts the CH1 domain structure of p300, an important mediator of tumor hypoxia adaptation. Prevents the association of p300 with CH1-interacting proteins, such as HIF-1α and STAT2. Shown to attenuate hypoxia-induced transcription in vitro (IC₅₀ = 20 nM and <10 nM in inhibiting secreted and cellular VEGF, respectively, in Hep38 cells) and inhibit tumor growth by inducing necrosis in vivo (1 mg/kg, i.v., daily in tumor xenografted NCr/Nude mice). Exhibits no effect on the transcriptional activity of PAR, SREBP2, or SRC-1, whose association with p300 is not mediated via CH1 domain.

A cell-permeable dithiodiketopiperazine antimicrobial agent that disrupts the CH1 domain structure of p300, an important mediator of tumor hypoxia adaptation, and prevents the association of p300 with CH1-interacting proteins, such as HIF-1α and STAT2. Shown to attenuate hypoxia-induced transcription in vitro (IC₅₀ = 20 nM and <10 nM in inhibiting secreted and cellular VEGF, respectively, in Hep38 cells) and inhibit tumor growth by inducing necrosis in vivo (1 mg/kg, i.v., daily in tumor xenografted NCr/Nude mice). Does not affect the transcriptional activity of PAR, SREBP2, or SRC-1, whose association with p300 is not mediated via CH1 domain.

A cell-permeable dithiodiketopiperazine antimicrobial agent that disrupts the CH1 domain structure of p300.

Toxicity: Toxic (F)

Following reconstitution in fresh, anhydrous DMSO, aliquot and freeze (-20°C). Stock solutions for up to 3 months at -20°C.

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Fujimoto, H., et al. 2004. J. Nat. Prod.67, 98.
Kung, A.L., et al. 2004. Cancer Cell6, 33.

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