- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 431898-65-6] PS-1145
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18008 |
| Brand: | MCE |
| CAS: | 431898-65-6 |
Overview
| MDL | MFCD18089825 |
|---|---|
| Molecular Weight | 322.75 |
| Molecular Formula | C17H11ClN4O |
| SMILES | O=C(C1=CC=CN=C1)NC2=CC(Cl)=CC3=C2NC4=C3C=CN=C4 |
2 Publications Citing Use of MCE
Summary
PS-1145 is an IκB kinase ( IKK ) inhibitor with an IC 50 of 88 nM.
IC50 & Target
|
IKK 88 nM (IC 50 ) |
In Vitro
PS-1145 blocks TNFα-induced NF-κB activation in a dose- and time-dependent fashion in MM cells through inhibition of IκBα phosphorylation. Dexamethasone (Dex), which up-regulates IκBα protein, enhances blockade of NF-κB activation by PS-1145. PS-1145 blocks the protective effect of IL-6 against Dex-induced apotosis. TNFα-induced intracellular adhesion molecule (ICAM)-1 expression on both RPMI8226 and MM.1S cells is also inhibited by PS-1145. Moreover, PS-1145 inhibits both IL-6 secretion from bone marrow stromal cells (BMSCs) triggered by MM cell adhesion and proliferation of MM cells adherent to BMSCs [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Administration of either Bortezomib or PS-1145 (50 mg/kg) results in a significant decrease in serum levels of all 3 cytokines that is nonsignificantly different from those in mice that underwent transplantation with TCD BM alone [2] . PS1145 is injected intracerebroventricular (icv) as a pretreatment to block hypothalamic inflammation induced by IL-4 in adult male Wistar rats consuming a high-fat diet (HFD) over an 11-day period. The four groups of rats according to icv pretreatment/treatment condition are Veh/Veh, Veh/IL-4, PS1145/Veh, and PS1145/IL-4. Rats in the Veh/IL-4 group display increased weight gain on the HFD compared with the Veh/Veh group (P<0.05 on days 6-9). Importantly, the effect of icv IL-4 administration to increase body fat mass during high-fat (HF) feeding is completely blocked by icv PS1145 pretreatment at a dose that has no independent effect on body composition (on day 8: P<0.001, PS1145/Veh vs. PS1145/IL-4; P=not significant, PS1145/Veh vs. Veh/Veh). In PS1145/IL-4 injected rats, IL-1β mRNA content is decreased by ~75% compared with that of Veh/IL-4-injected rats [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 20.83 mg/mL ( 64.54 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.44 mM); Clear solution
References
- [1] Hideshima T, et al. NF-kappa B as a therapeutic target in multiple myeloma. J Biol Chem. 2002 May 10;277(19):16639-47.
- [2] Vodanovic-Jankovic S, et al. NF-kappaB as a target for the prevention of graft-versus-host disease: comparative efficacy of bortezomib and PS-1145. Blood. 2006 Jan 15;107(2):827-34.
- [3] Oh-I S, et al. Central administration of interleukin-4 exacerbates hypothalamic inflammation and weight gain during high-fat feeding. Am J Physiol Endocrinol Metab. 2010 Jul;299(1):E47-53.
Synonyms
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.