2. NF-κB
  3. IKK
  4. LY2409881

LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.

For research use only. We do not sell to patients.

LY2409881 Chemical Structure

LY2409881 Chemical Structure

CAS No. : 946518-61-2

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IKK-α IKK-β IKK IKKε TBK1

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Description

LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.

IC50 & Target[1]

IKK2

30 nM (IC50)

In Vitro

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.

LY2409881 Related Antibodies
In Vivo

A well-established xenograft model of DLBCL is used to confirm the activity of LY2409881 in vivo. SCID-beige mice implanted with LY10 cell-derived tumors are given intraperitoneal injections of LY2409881 twice weekly at three different doses: 50, 100, and 200 mg/kg. The treatments are well tolerated, resulting in no death or severe morbidity of the mice. The average tumor volume is graphed as a function of time for each treatment group. The rates of tumor volume growth of the treatment groups are all significantly slower than the untreated control group (P≤0.01)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

485.04

Formula

C24H29ClN6OS
CAS No.
SMILES

O=C(C1=C(C=C(C2=NC(NCCCN3CCN(C)CC3)=NC=C2Cl)S4)C4=CC=C1)NC5CC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0617 mL 10.3084 mL 20.6169 mL
5 mM 0.4123 mL 2.0617 mL 4.1234 mL
View the Complete Stock Solution Preparation Table

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Purity & Documentation
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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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LY2409881 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY2409881946518-61-2LY 2409881LY-2409881IKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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