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LY2409881

Catalog No.
B4986
potent and selective IKK2 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$103.00
In stock
25mg
$334.00
In stock
100mg
$698.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

LY2409881 is a potent and selective inhibitor of IKK2 with IC50 value of 30 nM [1].

IκB kinase β (IKK2) is an enzyme that serves as a subunit of IκB kinase, which is involved in the cytokine-activated immune responses. IKK2 activates nuclear factor kappa-B kinase (NF-κB).

LY2409881 is a selective IKK2 inhibitor and exhibited >10-fold selectivity over other common kinases and IKK1. In the ovarian cancer cell line SKOV3, LY2409881 showed moderate cytotoxicity. While coadministration of LY2409881 and TNFɑ significantly induced cells death, which suggested LY2409881 inhibited NF-κB mediated antiapoptotic signals in a TNFɑ-dependent way. In the DLBCL cell line LY10, LY2409881 (10 μM) inhibited TNFɑ-dependent phosphorylation of IκB. In the DLBCL cell line SUDHL2, LY2409881 (10 μM) inhibited the nuclear signals of p50 and NF-κB. Also, LY2409881 induced apoptosis in a concentration-dependent way [1].

In SCID-beige mice bearing LY10 cell-derived tumors, LY2409881 (50, 100 and 200 mg/kg) significantly inhibited tumor growth [1].

Reference:
[1].  Deng C, Lipstein M, Rodriguez R, et al. The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB. Clin Cancer Res, 2015, 21(1): 134-145.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt594.43
Cas No.946518-60-1
FormulaC24H32Cl4N6OS
Solubility≥59.4 mg/mL in DMSO with ultrasonic; insoluble in EtOH; insoluble in H2O
Chemical Name2-(5-chloro-2-((3-(4-methylpiperazin-1-yl)propyl)amino)pyrimidin-4-yl)-N-cyclopropylbenzo[b]thiophene-4-carboxamide
SDFDownload SDF
Canonical SMILESClC1=CN=C(NCCCN2CCN(C)CC2)N=C1C3=CC4=C(S3)C=CC=C4C(NC5CC5)=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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