946518-60-1 Usage
Description
LY2409881 trihydrochloride is a small molecule inhibitor of IkB-kinase (IKK2), which plays a crucial role in the regulation of the NF-κB signaling pathway. LY2409881 trihydrochloride has the potential to be developed as an anti-inflammatory drug candidate due to its ability to inhibit the activation of NF-κB pathways.
Uses
Used in Pharmaceutical Industry:
LY2409881 trihydrochloride is used as an anti-inflammatory drug candidate for its ability to inhibit the IkB-kinase (IKK2) and NF-κB pathways. This inhibition can help in reducing inflammation and treating various inflammatory diseases by modulating the immune response.
Used in Research Applications:
LY2409881 trihydrochloride is used as a research tool for studying the role of IkB-kinase (IKK2) and NF-κB pathways in various cellular processes and diseases. LY2409881 trihydrochloride can help researchers understand the molecular mechanisms underlying inflammation and identify potential therapeutic targets for the development of new anti-inflammatory drugs.
Biological Activity
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].
references
[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.
Check Digit Verification of cas no
The CAS Registry Mumber 946518-60-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,4,6,5,1 and 8 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 946518-60:
(8*9)+(7*4)+(6*6)+(5*5)+(4*1)+(3*8)+(2*6)+(1*0)=201
201 % 10 = 1
So 946518-60-1 is a valid CAS Registry Number.
946518-60-1Relevant articles and documents
[4-(Benzo[B]Thiophen-2-Yl) Pyrimidin-2-Yl]-Amine Derivatives As Ikk-Beta Inhibitors For The Treatment Of Cancer And Inflammatory Diseases
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Page/Page column 19, (2009/01/20)
The present invention provides compounds of Formula I: useful in the treatment of cancer and inflammatory diseases.
