Free shipping on all orders over $ 500

PS-1145

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
Bulk Inquiry?

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
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.

Related IκB/IKK Products
LY2409881

LY2409881 is a novel selective inhibitor of IKK2 with IC50 of 30 nM; IC50 for IKK1 and other common kinases is at least one log higher.

Bardoxolone

Bardoxolone is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor.

Amlexanox

Amlexanox is a specific inhibitor of IKKε and TBK1.

PHA-408

PHA-408 is a highly selective and ATP-competitive IKK-2 inhibitor with IC50 of 40 nM.

IMD 0354

IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.