PS-1145
Based on 5 publication(s) in Google Scholar
PS-1145 is an IκB kinase (IKK) inhibitor with an IC50 of 88 nM.
For research use only. We do not sell to patients.
- Purity: 99.67%
- CAS No.: 431898-65-6
- Formula: C17H11ClN4O
- Molecular Weight:322.75
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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NF-κB Signaling Compound Library
HY-L014
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Stem Cell Signaling Compound Library
HY-L017
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Differentiation Inducing Compound Library
HY-L038
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Pyroptosis Compound Library
HY-L059
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HY-L099
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Cell Death Library
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MCE Bioactive Compound Library
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Protein Kinase Compound Library
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
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Mass Spectrometry Human Metabolite Library
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Posttranslational Modification Library
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Lactylation Compound Library
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Publications Citing Use of MedChemExpress (MCE) PS-1145
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Biological Activity
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IKK 88 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
5 μM
Compound: 26
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Inhibition of GST-IkB phosphorylation by TNF-alpha stimulated HeLa cell lysate (IP-IKKgamma)
Inhibition of GST-IkB phosphorylation by TNF-alpha stimulated HeLa cell lysate (IP-IKKgamma)
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[PMID: 12824047] |
| HeLa | IC50 |
0.1 μM
Compound: 26
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Inhibitory activity against IkappaB kinase(IKK) isolated from HeLa cells activated with recombinant MEEK1 in an ELISA phosphorylation assay.
Inhibitory activity against IkappaB kinase(IKK) isolated from HeLa cells activated with recombinant MEEK1 in an ELISA phosphorylation assay.
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[PMID: 12824047] |
| HeLa | IC50 |
150 nM
Compound: 26
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Inhibition of IkBalpha phosphorylation in TNFalpha stimulated HeLa cells
Inhibition of IkBalpha phosphorylation in TNFalpha stimulated HeLa cells
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[PMID: 12824047] |
| MDA-MB-231 | IC50 |
>100 μM
Compound: PS-1145
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Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTox green assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTox green assay
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[PMID: 30108896] |
| MDA-MB-231 | IC50 |
0.9 μM
Compound: PS-1145
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Antiproliferative activity against human MDA-MB-231 cells assessed as DNA content after 72 hrs by Hoechst 33258 staining based fluorescence assay
Antiproliferative activity against human MDA-MB-231 cells assessed as DNA content after 72 hrs by Hoechst 33258 staining based fluorescence assay
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[PMID: 30108896] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 431898-65-6
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Appearance Solid
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Molecular Weight 322.75
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Formula C17H11ClN4O
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Color Off-white to light yellow
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SMILES
O=C(C1=CC=CN=C1)NC2=CC(Cl)=CC3=C2NC4=C3C=CN=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Bone Joint Res
Kaempferol suppresses fibroblast-like synoviocyte proliferation in rheumatoid arthritis by targeting glutamate-cysteine ligase modifier subunit to inhibit ferroptosis resistance. [Abstract]2026 May 8;15(5):482-496. PMID: 42097618 -
Exp Cell Res
Continuous NF-κB pathway inhibition promotes expansion of human phenotypical hematopoietic stem/progenitor cells through metabolism regulation. [Abstract]2021 Feb 15;399(2):112468. PMID: 33428903 -
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Solvent & Solubility
DMSO : 20.83 mg/mL (64.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (6.44 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The inhibitory effect of PS-1145 on MM growth is assessed by measuring MTT dye absorbance of the cells. MM.1S cells are cultured for 48 h with 0.2 and 1 ng/mL TNFα, in the absence or presence of 2.5 μM, 5 μM, and 10 μM PS-1145. Cell viability is assessed by MTT assay. 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
C57BL/6 (B6), B10.BR, and B6.SJL mice are used. Mice receive regular mouse chow and acidified tap water ad libitum. Bortezomib is administered intravenously to animals at a dose of 1 mg/kg, whereas PS-1145 is given intraperitoneally at a dose of 50 mg/kg. The first dose of each agent is administered before conditioning with total body irradiation (TBI).
Rats[3]
Weight-matched male Wistar rats (320-350 g) are used. Four groups of rats (n=6/group) consume the HFD for a 9-day study period. Animals in each group receive two consecutive icv injections three times/wk. Immediately prior to icv injection of IL-4 (100 ng) or vehicle, all animals receive a pretreatment icv injection of either the IKKβ inhibitor PS1145 (10 μg) or its vehicle (saline). Food intake and body weight are measured daily. Body composition analysis is conducted as above on days 0 and 8. On day 9, animals are euthanized and samples collected.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0984 mL | 15.4919 mL | 30.9837 mL | 77.4593 mL |
| 5 mM | 0.6197 mL | 3.0984 mL | 6.1967 mL | 15.4919 mL | |
| 10 mM | 0.3098 mL | 1.5492 mL | 3.0984 mL | 7.7459 mL | |
| 15 mM | 0.2066 mL | 1.0328 mL | 2.0656 mL | 5.1640 mL | |
| 20 mM | 0.1549 mL | 0.7746 mL | 1.5492 mL | 3.8730 mL | |
| 25 mM | 0.1239 mL | 0.6197 mL | 1.2393 mL | 3.0984 mL | |
| 30 mM | 0.1033 mL | 0.5164 mL | 1.0328 mL | 2.5820 mL | |
| 40 mM | 0.0775 mL | 0.3873 mL | 0.7746 mL | 1.9365 mL | |
| 50 mM | 0.0620 mL | 0.3098 mL | 0.6197 mL | 1.5492 mL | |
| 60 mM | 0.0516 mL | 0.2582 mL | 0.5164 mL | 1.2910 mL |
PS-1145 Related Classifications
HY-18008 Related Classifications
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