PS-1145

Alias: PS 1145; PS1145; PS-1145
Cat No.:V0753 Purity: ≥98%
PS-1145 (PS1145) is a novel, potent and specific IKK (IκB kinase) inhibitor with anticancer activity.
PS-1145 Chemical Structure CAS No.: 431898-65-6
Product category: IκB IKK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of PS-1145:

  • PS-1145 diHCl
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

PS-1145 (PS1145) is a novel, potent and specific IKK (IκB kinase) inhibitor with anticancer activity. With an IC50 of 88 NM, it inhibits IKK. In rats with DMBA-induced skin tumors, PS 1145 has excellent in vivo antitumor efficacy.

Biological Activity I Assay Protocols (From Reference)
Targets
IKK (IC50 = 88 nM)
ln Vitro
PS-1145 inhibits IkappaBalpha phosphorylation, which prevents TNFalpha from activating NF-kappaB, and it also prevents IL-6 from protecting against Dex-induced apotosis. Additionally, PS-1145 reduces IL-6 secretion from BMSCs stimulated by MM cell adhesion as well as paracrine MM cell growth. [1] By activating CD3 and CD28 coreceptors in human primary CD4(+) T cells, PS-1145 prevents cell proliferation and hinders the activation of NF-κB and AP-1 transcription factors. [2]
ln Vivo
PS-1145 (50 mg/kg, i.v.) promotes tumor cell apoptosis in male Wistar rats with DMBA-induced skin tumors by up-regulating p53, activating caspases, and down-regulating NF-κB and VEGF factor, and this promotes the growth of the tumor. [3]
Enzyme Assay
PS-1145 is dissolved in DMSO and kept at −20 °C until use. By measuring Km, ATP against changing fixed inhibitor concentrations, the Ki value of PS-1145 against the IKK complex is calculated. In a nutshell, the catalytic domain of MEKK1 expressed in sf9 is used to pre-activate the partially purified IKK complex obtained from unstimulated HeLa S3 cells. An ELISA format is used to measure kinase activity using a biotinylated IκBα peptide (250 μM, RHDSGLDSMKD,Km,peptide = 30 M,K m, ATP = 10 μM) and phospho-[Ser32]-phosphoantibodies.
Cell Assay
By measuring the cells' MTT dye absorbance, the inhibitory effect of PS-1145 on MM growth is determined. For the final 4 hours of 48-h cultures, cells from 48-h cultures are pulsed with 10 μL of 5 mg/ml MTT to each well, and then 100 l of isopropanol containing 0.04N HCl. Using a spectrophotometer, absorbance is measured at 570 nm.
Animal Protocol
Mice: The mice used are C57BL/6 (B6), B10.BR, and B6.SJL. Regular mouse food and acidified tap water are freely given to mice. PS-1145 is given intraperitoneally at a dose of 50 mg/kg, whereas animals receive bortezomib intravenously at a dose of 1 mg/kg. Before conditioning with total body irradiation (TBI), the first dose of each agent is given.
Rats: Male Wistar rats weighing between 320 and 350 g are employed. For a 9-day research period, the HFD is consumed by four groups of rats (n=6/group). Three times per week, each group's animals receive two consecutive icv injections. All animals receive a pretreatment icv injection of either the IKK inhibitor PS1145 (10 g) or its vehicle (saline) just before receiving an icv injection of IL-4 (100 ng) or vehicle. Daily measurements of food intake and body weight are taken. On days 0 and 8, body composition analysis is performed as described above. Animals are put to death and samples are taken on day nine.
References

[1]. J Biol Chem . 2002 May 10;277(19):16639-47.

[2]. J Immunol . 2012 Mar 15;188(6):2545-55.

[3]. Cell Biol Int . 2015 Nov;39(11):1317-28.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H11CLN4O
Molecular Weight
322.75
Exact Mass
322.750
Elemental Analysis
C, 63.26; H, 3.44; Cl, 10.98; N, 17.36; O, 4.96
CAS #
431898-65-6
Appearance
Yellow solid powder
SMILES
C1=CC(=CN=C1)C(=O)NC2=CC(=CC3=C2NC4=C3C=CN=C4)Cl
InChi Key
JZRMBDHPALEPDM-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H11ClN4O/c18-11-6-13-12-3-5-20-9-15(12)21-16(13)14(7-11)22-17(23)10-2-1-4-19-8-10/h1-9,21H,(H,22,23)
Chemical Name
N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)pyridine-3-carboxamide
Synonyms
PS 1145; PS1145; PS-1145
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~64 mg/mL (~198.3 mM)
Water: <1 mg/mL
Ethanol: ~2 mg/mL warmed (~6.2 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0984 mL 15.4919 mL 30.9837 mL
5 mM 0.6197 mL 3.0984 mL 6.1967 mL
10 mM 0.3098 mL 1.5492 mL 3.0984 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • PS-1145

    PS-1145 blocks phosphorylation and degradation of IκBα triggered by TNFα.J Biol Chem.2002 May 10;277(19):16639-47.
  • PS-1145

    Effect of PS-1145 on DNA synthesis, cell cycle profile, and signaling cascades triggered by IL-6.J Biol Chem.2002 May 10;277(19):16639-47.
  • PS-1145

    Dex up-regulates IκBα protein and enhances the inhibitory effect of PS-1145 on NF-κB activation.J Biol Chem.2002 May 10;277(19):16639-47.
  • PS-1145

    PS-1145 inhibits growth and blocks the protective effect of IL-6 against Dex - and IMiD3-induced growth inhibition.J Biol Chem.2002 May 10;277(19):16639-47.
  • PS-1145

    PS-1145 inhibits TNFα-induced ICAM-1 expression and triggers TNFα-induced apoptosis in MM cells.J Biol Chem.2002 May 10;277(19):16639-47.
  • PS-1145

    PS-1145 inhibits paracrine MM cell growth and IL-6 secretion in BMSCs triggered by MM cell adherence.J Biol Chem.2002 May 10;277(19):16639-47.
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