LY2409881
Based on 5 publication(s) in Google Scholar
LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.
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- CAS No.: 946518-61-2
- Formule: C24H29ClN6OS
- Masse moléculaire:485.04
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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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Publications Citing Use of MedChemExpress (MCE) LY2409881
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Activité biologique
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IKK2 30 nM (IC50) |
LY2409881 is an IKK2 inhibitor that inhibits TNFα-induced activation of NF-κB. By in vitro kinase assay, LY2409881 potently inhibits IKK2, with an IC50 of 30 nM. In contrast, the IC50 for IKK1 and other common kinases is at least one log higher. The specificity of LY2409881 for NF-κB signaling is further studied in a cell-based assay, by examining the effect of LY2409881 in the TNFα-dependent antiapoptosis function. TNFα is a well-characterized upstream stimulus of NF-κB. In the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity, whereas TNFα at 10 ng/mL does not cause any cytotoxicity. In contrast, coadministration of LY2409881 and TNFα results in markedly higher cell killing compared with LY2409881. This is because TNFα-dependent activation of antiapoptotic signals mediated by NF-κB is blocked by LY2409881, while the proapoptotic TNF receptor-associated death domain (TRADD) and FAS-associated death domain (FADD) cascade pathways activated by TNFα are not affected by LY2409881[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. 946518-61-2
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Masse moléculaire 485.04
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Formule C24H29ClN6OS
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SMILES
O=C(C1=C(C=C(C2=NC(NCCCN3CCN(C)CC3)=NC=C2Cl)S4)C4=CC=C1)NC5CC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
2026 Mar 11. PMID: 41813972 -
Clin Transl Med
Uterus globulin associated protein 1 (UGRP1) binds podoplanin (PDPN) to promote a novel inflammation pathway during Streptococcus pneumoniae infection. [Abstract]2022 Jun;12(6):e850. PMID: 35652821 -
Cell Rep
Polo-like kinase 2 promotes microglial activation via regulation of the HSP90α/IKKβ pathway. [Abstract]2024 Oct 8;43(10):114827. PMID: 39383034 -
Int J Mol Sci
Salicylate Sodium Suppresses Monocyte Chemoattractant Protein-1 Production by Directly Inhibiting Phosphodiesterase 3B in TNF-α-Stimulated Adipocytes. [Abstract]2022 Dec 24;24(1):320. PMID: 36613764 -
iScience
Pan-cancer analysis reveals Rho kinase addiction as a vulnerability of de-differentiated cancer cells. [Abstract]2026 Jun 2;29(6):116031. PMID: 42369662
Solvant et solubilité
DMSO : ≥ 37 mg/mL (76.28 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
OCI-Ly1, OCI-Ly7, and Su-DHL4 are GCB DLBCL cell lines; OCI-Ly3, OCI-Ly10, HBL1, and Su-DHL2 are ABC DLBCL lines. These cell lines are grown in Iscove Modified Dulbecco Medium with 10% FCS. Fresh medium is added every 2 to 3 days, and the cells are kept at a cell concentration of 0.1 to 1×106/mL. Cytotoxicity is evaluated using the CellTiter-Glo Reagent. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment (LY2409881; 0.01, 0.1, 1 and 10 μM) relative to the untreated control from the same experiment, as a function of time. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Mouse experiments are carried out. Five- to 7-week-old SCID beige mice are injected with 107 Ly10 cells mixed in Matrigel in the posterior flank subcutaneously. When the tumors approach 150 mm3, the mice are divided into four groups of 8 mice: (i) control group, which receive 5% dextrose in water; (ii) LY2409881 at 50 mg/kg in D5W; (iii) LY2409881 at 100 mg/kg in D5W; and (iv) LY2409881 at 200 mg/kg in D5W. LY2409881 or D5W is administered intraperitoneally on day 1 and 4 of every week for 4 weeks. The data are expressed as average tumor volume (mm3) per group as a function of time. Tumor volume is calculated.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
Références
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0617 mL | 10.3084 mL | 20.6169 mL | 51.5421 mL |
| 5 mM | 0.4123 mL | 2.0617 mL | 4.1234 mL | 10.3084 mL | |
| 10 mM | 0.2062 mL | 1.0308 mL | 2.0617 mL | 5.1542 mL | |
| 15 mM | 0.1374 mL | 0.6872 mL | 1.3745 mL | 3.4361 mL | |
| 20 mM | 0.1031 mL | 0.5154 mL | 1.0308 mL | 2.5771 mL | |
| 25 mM | 0.0825 mL | 0.4123 mL | 0.8247 mL | 2.0617 mL | |
| 30 mM | 0.0687 mL | 0.3436 mL | 0.6872 mL | 1.7181 mL | |
| 40 mM | 0.0515 mL | 0.2577 mL | 0.5154 mL | 1.2886 mL | |
| 50 mM | 0.0412 mL | 0.2062 mL | 0.4123 mL | 1.0308 mL | |
| 60 mM | 0.0344 mL | 0.1718 mL | 0.3436 mL | 0.8590 mL |
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