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Cat. No. M5338
PS-1145 Structure
Size Price Availability Quantity
5mg USD 95 In stock
10mg USD 165 In stock
50mg USD 625 In stock
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Quality Control
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.

Cell Experiment
Cell lines MM.1S, U266, and RPMI8226 cell lines
Preparation method The inhibitory effect of PS-1145 on MM growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-h cultures are pulsed with 10 μL of 5 mg/ml MTT to each well for the last 4 h of 48-h cultures, followed by 100 μl of isopropanol containing 0.04N HCl. Absorbance is measured at 570 nm using a spectrophotometer.
Concentrations ~50 μM
Incubation time 48 h
Animal Experiment
Animal models Male Wistar rats with DMBA-induced skin tumor
Formulation Dissolved at 0.4 mg/mL in DMSO and diluted with 0.9% NaCl
Dosages ~50 mg/kg
Administration i.v.
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 100.00%
Solubility 60 mg/mL in DMSO
Storage at -20°C

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

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