BMS-345541
Based on 38 publication(s) in Google Scholar
BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.79%
- CAS No.: 445430-58-0
- Formule: C14H17N5
- Masse moléculaire:255.32
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Stockage: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
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BMS-345541
More- Cancer Cell. 2015 Mar 9;27(3):409-25. [Abstract]
- Cell Res. 2019 Mar;29(3):193-205. [Abstract]
- Nat Metab. 2023 Mar;5(3):481-494. [Abstract]
- Sci Transl Med. 2021 Jan 27;13(578):eaba7308. [Abstract]
- Interdiscip Med. 2026 May 18.
- Mol Biomed. 2026 Jun 23;7(1):94. [Abstract]
- J Immunother Cancer. 2026 Jun 3;14(6):e014253. [Abstract]
- Phytomedicine. 2026 Feb:151:157795. [Abstract]
- Am J Hematol. 2024 Jul;99(7):1326-1337. [Abstract]
- J Hazard Mater Adv. 2026 Mar 7.
- Int J Biol Macromol. 2025 Dec;334(Pt 1):149021. [Abstract]
- EMBO Mol Med. 2025 Nov 26. [Abstract]
- EMBO Mol Med. 2025 Apr;17(4):645-678. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Dent Res. 2019 Jul;98(8):896-903. [Abstract]
- Cancer Metab. 2024 Jul 8;12(1):20. [Abstract]
- Front Microbiol. 2021 Feb 2;12:607451. [Abstract]
- Int Immunopharmacol. 2021 Dec;101(Pt A):108264. [Abstract]
- Molecules. 2025 May 2;30(9):2025. [Abstract]
- J Mol Med (Berl). 2020 Oct;98(10):1479-1491. [Abstract]
- Cancer Sci. 2025 Nov 14. [Abstract]
- PLoS Pathog. 2025 Oct 24;21(10):e1013646. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- Antiviral Res. 2026 May:249:106391. [Abstract]
- Am J Physiol Endocrinol Metab. 2021 Apr 1;320(4):E732-E746. [Abstract]
- J Virol. 2019 Nov 26;93(24):e01499-19. [Abstract]
- PLoS Comput Biol. 2020 Jun 26;16(6):e1007901. [Abstract]
- J Pharmacol Sci. 2023 Dec;153(4):188-196. [Abstract]
- Biochem Biophys Res Commun. 2023 Nov 5:680:127-134. [Abstract]
- J Vet Sci. 2023 Sep;24(5):e72. [Abstract]
- Photobiomodul Photomed Laser Surg. 2025 Jul 24. [Abstract]
- University of Pittsburgh. 2026.
- bioRxiv. 2026 Apr 22:2026.04.19.719504. [Abstract]
- bioRxiv. 2025 Oct 25.
- bioRxiv. 2025 Aug 13:2025.08.11.669793. [Abstract]
- Research Square Print. October 27th, 2022.
- Aging (Albany NY). 2021 Aug 10;13(15):19088-19107. [Abstract]
- Biomed Pharmacother. 2020 Jul:127:110116. [Abstract]
Customer Validation & Images
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WB
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Cell Migration/Invasion Assay
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RT-PCR
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Flow Cytometry
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IF
Activité biologique
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IKK-2 0.3 μM (IC50) |
IKK-1 4 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
5.6 μM
Compound: BMS345541
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Cytotoxicity against human A549 cells measured after 72 hrs by MTT assay
Cytotoxicity against human A549 cells measured after 72 hrs by MTT assay
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[PMID: 27886548] |
| A549 | IC50 |
8.6 μM
Compound: BMS345541
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Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 29655083] |
| Jurkat | CC50 |
100 μM
Compound: 1
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Cytotoxicity against Jurkat cells by Alamar blue assay
Cytotoxicity against Jurkat cells by Alamar blue assay
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[PMID: 17540562] |
| Jurkat | EC50 |
13.3 μM
Compound: 1
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Inhibition of LPS-induced TNFalpha production in Jurkat cells
Inhibition of LPS-induced TNFalpha production in Jurkat cells
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[PMID: 17540562] |
| L02 | IC50 |
15.3 μM
Compound: BMS345541
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Cytotoxicity against human HL7702 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HL7702 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 29655083] |
| Lewis lung carcinoma cell line | IC50 |
4.8 μM
Compound: BMS345541
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Cytotoxicity against mouse LLC cells measured after 72 hrs by MTT assay
Cytotoxicity against mouse LLC cells measured after 72 hrs by MTT assay
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[PMID: 27886548] |
| NCI-H1650 | IC50 |
19.9 μM
Compound: BMS345541
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Cytotoxicity against human NCI-H1650 cells measured after 72 hrs by MTT assay
Cytotoxicity against human NCI-H1650 cells measured after 72 hrs by MTT assay
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[PMID: 27886548] |
| NCI-H1650 | IC50 |
9.3 μM
Compound: BMS345541
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Cytotoxicity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 29655083] |
| NCI-H1975 | IC50 |
8 μM
Compound: BMS345541
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Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 29655083] |
| NCI-H460 | IC50 |
2.8 μM
Compound: BMS345541
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Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 29655083] |
| PBMC | EC50 |
0.8 μM
Compound: 1
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Inhibition of LPS-induced TNFalpha production in PBMC
Inhibition of LPS-induced TNFalpha production in PBMC
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[PMID: 17540562] |
| PBMC | IC50 |
1 μM
Compound: 1, BMS-345541
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Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release treated for 5 mins before LPS challenge measured after 6 hrs by ELISA
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release treated for 5 mins before LPS challenge measured after 6 hrs by ELISA
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[PMID: 21087862] |
| THP-1 | IC50 |
1 μM
Compound: Chemical probe : BMS-345541
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Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in IL-1beta cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by enzyme immunoassay
Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in IL-1beta cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by enzyme immunoassay
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[PMID: 12403772] |
| THP-1 | IC50 |
1 μM
Compound: Chemical probe : BMS-345541
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Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in IL-6 cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 24 hrs by enzyme immunoassay
Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in IL-6 cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 24 hrs by enzyme immunoassay
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[PMID: 12403772] |
| THP-1 | IC50 |
1 μM
Compound: Chemical probe : BMS-345541
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Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in IL-8 cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by enzyme immunoassay
Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in IL-8 cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by enzyme immunoassay
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[PMID: 12403772] |
| THP-1 | IC50 |
1 μM
Compound: Chemical probe : BMS-345541
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Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in TNFalpha cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by enzyme immunoassay
Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in TNFalpha cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by enzyme immunoassay
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[PMID: 12403772] |
BMS-345541 selectively inhibits the stimulated phosphorylation of IκBα in cells (IC50=4 μM). Consistent with the role of IKK/NF-κB in the regulation of cytokine transcription, BMS-345541 inhibits lipopolysaccharide-stimulated tumor necrosis factor α, interleukin-1β, interleukin-8, and interleukin-6 in THP-1 cells with IC50 values in the 1 to 5 μM range[1]. BMS-345541 treatment results in a concentration-dependent inhibition of melanoma cell proliferation in SK-MEL-5, A375, and Hs 294T cells. BMS-345541 (0, 100 μM) shows apoptotic features as revealed by TUNEL staining and nuclear condensation[2].
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. 445430-58-0
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Appearance Solid
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Masse moléculaire 255.32
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Formule C14H17N5
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Color White to off-white
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SMILES
CC1=CN=C2C(NCCN)=NC3=CC=C(C)C=C3N21
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (38)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Self-enforcing feedback activation between BCL6 and pre-B cell receptor signaling defines a distinct subtype of acute lymphoblastic leukemia. [Abstract]2015 Mar 9;27(3):409-25. PMID: 25759025
BMS-345541 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2015 Mar 9;27(3):409-25. [Abstract]
pre-BCR+ ALL cells, pre-BCR- ALL cells and mature B cell lymphoma cells were treated with BMS-345541 hydrochloride (1-64 μM) and cell viability was measured by CCK-8 at different dose levels.
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Cell Res
Virus-induced accumulation of intracellular bile acids activates the TGR5-β-arrestin-SRC axis to enable innate antiviral immunity. [Abstract]2019 Mar;29(3):193-205. PMID: 30651583 -
Nat Metab
2023 Mar;5(3):481-494. PMID: 36879120
BMS-345541 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2023 Mar;5(3):481-494. [Abstract]
Mt2gene expression in beige adipocytes treated with indicated compounds (50 ng/mL TNF, 2 μM BMS345541, 1 μM SCH772984, 5 μM SB202190 and 5 μM SP600125; n = 4 biological independent samples).
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Sci Transl Med
A chimeric antigen receptor with antigen-independent OX40 signaling mediates potent antitumor activity. [Abstract]2021 Jan 27;13(578):eaba7308. PMID: 33504651 -
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Mol Biomed
Death-associated protein kinase 2 (DAPK2) propagates endoplasmic reticulum stress in macrophages to worsen sepsis through HSPA5-IRE1α axis. [Abstract]2026 Jun 23;7(1):94. PMID: 42334722 -
J Immunother Cancer
Chemotherapy induces an IL1β-dependent neutrophil recruitment and activation that promote chemoresistance in metastatic ovarian cancer. [Abstract]2026 Jun 3;14(6):e014253. PMID: 42236112 -
Phytomedicine
Complementary roles and synergy of the Ephedra-Glycyrrhiza herb pair across murine models of respiratory symptoms and poly(I:C)-induced pneumonia. [Abstract]2026 Feb:151:157795. PMID: 41539102 -
Am J Hematol
miR-146a-/- mice model reveals that NF-κB inhibition reverts inflammation-driven myelofibrosis-like phenotype. [Abstract]2024 Jul;99(7):1326-1337. PMID: 38646919 -
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Int J Biol Macromol
Lipocalin 2 deficiency attenuates NLRP3 inflammasome activation through glycolysis impairment and MGST1-mediated mitochondrial ROS reduction. [Abstract]2025 Dec;334(Pt 1):149021. PMID: 41260431 -
EMBO Mol Med
Isomeranzin activates Gnas-AMPK signaling to drive white adipose browning and curb obesity in mice. [Abstract]2025 Nov 26. PMID: 41299101 -
EMBO Mol Med
Targeting cIAP2 in a novel senolytic strategy prevents glioblastoma recurrence after radiotherapy. [Abstract]2025 Apr;17(4):645-678. PMID: 39972068 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
J Dent Res
2019 Jul;98(8):896-903. PMID: 31189369
BMS-345541 purchased from MedChemExpress. Usage Cited in: J Dent Res. 2019 Jul;98(8):896-903. [Abstract]
A223 and FaDu cells were treated with 5 µM BMS345541 for 18 h, and wb was detected.
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Cancer Metab
Subclinical dose irradiation triggers human breast cancer migration via mitochondrial reactive oxygen species. [Abstract]2024 Jul 8;12(1):20. PMID: 38978126
BMS-345541 purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2024 Jul 8;12(1):20. [Abstract]
The migratory activity of MCF7 or MDA-MB-231 cells was assessed 24 h after treatment ± NF-κB inhibitor BMS-345541 (10 µM).
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Front Microbiol
Cellular CARD11 Inhibits the Fusogenic Activity of Newcastle Disease Virus via CBM Signalosome-Mediated Furin Reduction in Chicken Fibroblasts. [Abstract]2021 Feb 2;12:607451. PMID: 33603723
BMS-345541 purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 Feb 2;12:607451. [Abstract]
BAY 11-7082, BMS-345541 (0.1-10 μM), and MI-2 at different concentrations for 24 h. These cells were observed and harvested to detect cell survival using flow cytometry. Scale bar = 50 μm.
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Int Immunopharmacol
Topoisomerase 2 inhibitor etoposide promotes interleukin-10 production in LPS-induced macrophages via upregulating transcription factor Maf and activating PI3K/Akt pathway. [Abstract]2021 Dec;101(Pt A):108264. PMID: 34715493 -
Molecules
Investigating Natural Product Inhibitors of IKKα: Insights from Integrative In Silico and Experimental Validation. [Abstract]2025 May 2;30(9):2025. PMID: 40363830 -
J Mol Med (Berl)
Chemically modified curcumin (CMC2.24) alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis. [Abstract]2020 Oct;98(10):1479-1491. PMID: 32860098
BMS-345541 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2020 Oct;98(10):1479-1491. [Abstract]
BMS-345541 (5 μM; 2 h) greatly enhanced CMC2.24-mediated decrease in the translocation of p65 subunits to the nuclei of chondrocytes.
BMS-345541 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2020 Oct;98(10):1479-1491. [Abstract]
BMS-345541 (5 μM) remarkably enhanced CMC2.24-mediated decrease in MMP-3, cleaved caspase-3, VEGF, RUNX2, p-p65, p-IκB-α, and Hif-2α expression, and increase in Col2a1 and Bcl-2 expression in chondrocytes.
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Cancer Sci
NF-κB Is a Potential Therapeutic Target for Histone Deacetylase Inhibitor-Resistant Cutaneous T-Cell Lymphoma. [Abstract]2025 Nov 14. PMID: 41236113 -
PLoS Pathog
Influenza virus infection reprograms cholesterol biosynthesis to facilitate virus replication by the TAK1-RORγ axis. [Abstract]2025 Oct 24;21(10):e1013646. PMID: 41134862
BMS-345541 purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2025 Oct 24;21(10):e1013646. [Abstract]
NL20 cells were infected with 0.1 MOI of H5N1 (SY) virus and then treated with the indicated concentrations of the JNK inhibitor (SP600125, SP), the IKK inhibitor (BMS345541, BMS, 0-10 μM) and the TAK1 inhibitor (5Z-oxzeneonal, 5Z) for 24 h. Cell lysates were prepared and analyzed for the levels of the PB2 and NP proteins by Western blots. GAPDH was detected as a loading control.
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iScience
Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]2024 May 16;27(6):110011. PMID: 38868181 -
Antiviral Res
Porcine epidemic diarrhea virus infection activates SREBP2 and induces RORγ expression to enhance cholesterol biosynthesis and virus replication. [Abstract]2026 May:249:106391. PMID: 41796918 -
Am J Physiol Endocrinol Metab
1,25-Dihydroxyvitamin D deficiency accelerates male reproductive senescence in aging mice and 1,25(OH)2D3 alleviates oxidative stress via NF-κB/SOD. [Abstract]2021 Apr 1;320(4):E732-E746. PMID: 33586492 -
J Virol
Host CARD11 Inhibits Newcastle Disease Virus Replication by Suppressing Viral Polymerase Activity in Neurons. [Abstract]2019 Nov 26;93(24):e01499-19. PMID: 31554683 -
PLoS Comput Biol
A systematic approach to decipher crosstalk in the p53 signaling pathway using single cell dynamics. [Abstract]2020 Jun 26;16(6):e1007901. PMID: 32589666 -
J Pharmacol Sci
Regulatory action of PGRMC1 on cyclic AMP-mediated COX2 expression in human endometrial cells. [Abstract]2023 Dec;153(4):188-196. PMID: 37973216 -
Biochem Biophys Res Commun
Engrailed 2 triggers the activation of multiple phosphorylation-induced signaling pathways in both transcription-dependent and -independent manners. [Abstract]2023 Nov 5:680:127-134. PMID: 37738902 -
J Vet Sci
Subcutaneous Streptococcus dysgalactiae GAPDH vaccine in mice induces a proficient innate immune response. [Abstract]2023 Sep;24(5):e72. PMID: 38031651 -
Photobiomodul Photomed Laser Surg
Photobiomodulation Promotes Odontoblast-Like Cell Activity via Reactive Oxygen Species and NF-κB: Implications for Dentin Regeneration. [Abstract]2025 Jul 24. PMID: 40711932 -
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bioRxiv
CDK4/6 inhibition sensitizes breast cancer to NK cell therapy by inducing immune-interactive surface proteins. [Abstract]2026 Apr 22:2026.04.19.719504. PMID: 42079201 -
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bioRxiv
2025 Aug 13:2025.08.11.669793. PMID: 40832193 -
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Aging (Albany NY)
2021 Aug 10;13(15):19088-19107. PMID: 34375950 -
Biomed Pharmacother
2020 Jul:127:110116. PMID: 32428833
BMS-345541 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Jul:127:110116. [Abstract]
Relative NFκB, p-NFκB, p-IKBα and t-IKBα protein levels in spheres in the control, TNFα, TNFα + BMS-345541 and TNFα + resveratrol groups.
Solvant et solubilité
DMSO : 10 mg/mL (39.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2.5 mg/mL (9.79 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 1 mg/mL (3.92 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (3.92 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Protocole
Assays measuring the enzyme-catalyzed phosphorylation of GST-IκBα are performed by adding enzyme (IKK-2, IKK-1, or IKK-ε, typically to a final concentration of 0.5 μg/mL) at 30°C to solutions of 100 μg/mL GST-IκBα and 5 μM [33P]ATP in 40 mM Tris-HCl, pH 7.5, containing 4 mM MgCl2, 34 mM sodium phosphate, 3 mM NaCl, 0.6 mM potassium phosphate, 1 mM KCl, 1 mM dithiothreitol, 3% (w/v) glycerol, and 250 μg/mL bovine serum albumin. The specific activity of [33P]ATP used in the assay is 100 Ci/mmol. After 5 min, the kinase reactions are stopped by the addition of 2× LaemmLi sample buffer and heat-treated at 90°C for 1 min. The samples are then loaded on to NuPAGE 10% BisTris gels. After completion of SDS-PAGE, gels are dried on a slab gel dryer. The bands are then detected using a 445Si PhosphorImager, and the radioactivity is quantified using ImageQuant software. Under these conditions, the degree of phosphorylation of GST-IκBα is linear with time and concentration of enzyme[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SK-MEL-5 cells are treated with BMS-345541 at different concentrations (0, 1.0, 10, and 100 μM) for different time periods. The cells are collected by trypsinization, fixed in 70% ethanol for 2 hours on ice and stained with PI solution (PBS containing 2 μg/mL PI, 0.1% Triton X-100, and 125 units/mL RNase A) at 37°C for 30 minutes. Cell fluorescence is measured by flow cytometry with 488 nm excitation and 620 nm emission filters and resulting data are analyzed using the software program MultiCycle[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
BMS-345541 is administered either by intravenous tail vein injection or by peroral gavage to groups of three 18-22 g female BALB/c mice. BMS-345541 is formulated as a 2 mg/mL solution in 3% Tween 80, water. Mice receive either a 2 mg/kg (1 mL/kg) intravenous bolus or a 10 mg/kg (5 mL/kg) peroral gavage. Whole blood samples are taken from individual mice by orbital bleed and cardiac puncture at 0, 0.05, 0.25, 0.5, 1.0, 3.0, 6.0, and 8.0 h after dosing. Whole blood is centrifuged at 20×103×g for 5 min. Serum is stored at -20°C until analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Burke JR, et al. BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice. J Biol Chem, 2003, 278(3), 1450-1456. [Content Brief]
[2]. Yang J, et al. BMS-345541 targets inhibitor of kappaB kinase and induces apoptosis in melanoma: involvement of nuclear factor kappaB and mitochondria pathways. Clin Cancer Res, 2006, 12(3 Pt 1), 950-960. [Content Brief]
[3]. MacMaster JF, et al. An inhibitor of IkappaB kinase, BMS-345541, blocks endothelial cell adhesion molecule expression and reduces the severity of dextran sulfate sodium-induced colitis in mice. Inflamm Res, 2003, 52(12), 508-511. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.9167 mL | 19.5833 mL | 39.1665 mL | 97.9163 mL |
| 5 mM | 0.7833 mL | 3.9167 mL | 7.8333 mL | 19.5833 mL | |
| DMSO | 10 mM | 0.3917 mL | 1.9583 mL | 3.9167 mL | 9.7916 mL |
| 15 mM | 0.2611 mL | 1.3056 mL | 2.6111 mL | 6.5278 mL | |
| 20 mM | 0.1958 mL | 0.9792 mL | 1.9583 mL | 4.8958 mL | |
| 25 mM | 0.1567 mL | 0.7833 mL | 1.5667 mL | 3.9167 mL | |
| 30 mM | 0.1306 mL | 0.6528 mL | 1.3056 mL | 3.2639 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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