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PS-1145

Cat. No. M5338

PS-1145 Structure
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: PS-1145 blocks TNFalpha-induced NF-kappaB activation through inhibition of IkappaBalpha phosphorylation, and blocks the protective effect of IL-6 against Dex-induced apotosis. PS-1145 also inhibits paracrine MM cell growth and IL-6 secretion in BMSCs triggered by MM cell adherence. In human primary CD4(+) T cells, PS-1145 abrogates cell proliferation and impairs the activation of NF-κB and AP-1 transcription factors by engagement of CD3 and CD28 coreceptor. In vivo: In male Wistar rats with DMBA-induced skin tumor, PS-1145 (50 mg/kg, i.v.) enhances tumor cell apoptosis by up-regulating p53, activating caspases and down regulating NF-κB and VEGF factor, and thus induces the tumor progression.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 322.75
Formula C17H11ClN4O
CAS Number 431898-65-6
Purity >99%
Solubility 64 mg/mL in DMSO
Storage at -20°C
Chemical Name
References

Interleukin 6, a nuclear factor-kappaB target, predicts resistance to docetaxel in hormone-independent prostate cancer and nuclear factor-kappaB inhibition by PS-1145 enhances docetaxel antitumor activity.
Domingo-Domenech J, et al. Clin Cancer Res. 2006 Sep 15;12(18):5578-86. PMID: 17000695.

NF-kappaB as a target for the prevention of graft-versus-host disease: comparative efficacy of bortezomib and PS-1145.
Vodanovic-Jankovic S, et al. Blood. 2006 Jan 15;107(2):827-34. PMID: 16174760.

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  Catalog
Abmole Inhibitor Catalog 2015




Keywords: PS-1145 supplier, IκB/IKK, inhibitors

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