Bay 11-7821 (BAY 11-7082)
Bay 11-7821 (also known as BAY 11-7082; CAS 19542-67-7) is a selective inhibitor of IκB kinase (IKK), exhibiting an IC50 of 10 μM. It suppresses TNFα-mediated phosphorylation of IκB-α, thereby blocking NF-κB activation and subsequent expression of adhesion molecules including E-selectin, VCAM-1, and ICAM-1. Independent of NF-κB inhibition, Bay 11-7821 can induce cell death in B-cell lymphoma and leukemic T cells, and suppresses the NALP3 inflammasome activation in macrophages. Thus, it serves as an important tool for studies on inflammatory signaling pathways and apoptosis regulation.
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| Storage | Store at -20°C |
| M.Wt | 207.25 |
| Cas No. | 19542-67-7 |
| Formula | C10H9NO2S |
| Solubility | insoluble in H2O; ≥64 mg/mL in DMSO; ≥10.64 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | (E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)C=CC#N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Non-small cell lung cancer cell line NCI-H1703 |
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Reaction Conditions |
0 ~ 8 μM Bay 11-7821 for 12 h incubation |
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Applications |
Bay 11-7821 (< 8 μM) was able to effectively inhibit both basal and TNFα stimulated NF-κB luciferase activity in a dose dependent manner. Bay 11-7821 (8 μM) strongly inhibited the rate of proliferation in NCI-H1703 cells. |
| Animal experiment:[2] | |
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Animal models |
Mice xenografted with human gastric cancer HGC27 cells |
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Dosage form |
2.5 or 5 mg/kg Twice-weekly intratumoral injection of Bay 11-7821, for 21 days |
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Applications |
Treatment of Bay 11-7821 significantly suppressed tumor growth in a dose-dependent manner. Furthermore, Bay 11-7821 dose-dependently induced cellular apoptosis and inhibited proliferation in tumor xenografts. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Gastonguay A, Berg T, Hauser AD, et al. The role of Rac1 in the regulation of NF-κB activity, cell proliferation, and cell migration in non-small cell lung carcinoma. Cancer Biology & Therapy, 2012, 13(8): 647-656. 2. Chen L, Ruan Y, Wang X, et al. BAY 11-7082, a nuclear factor-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells. Journal of Gastroenterology, 2014, 49(5): 864-874. |
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| Description | Bay 11-7821 is an inhibitor of E2 ubiquitin (Ub) conjugating enzyme and NF-κB. | |||||
| Targets | E2 ubiquitin conjugating enzyme | NF-κB | ||||
| IC50 | 10 μM | |||||
Quality Control & MSDS
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