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IKAM-1

Chemical Structure : IKAM-1

CAS No.: 2345648-37-3

IKAM-1 (Compound 39-100)

Catalog No.: PC-38626Not For Human Use, Lab Use Only.

IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM.
IKAM-1 (Compound 39-100) selectively binds to MAP3K1 and MAP3K12, inhibits MAP3K1 with IC50 of 4.2 uM, does not inhibit IKKβ but selectively inhibits MAP3K1 with micromolar potency in PANC1 cell lysates.
IKAM-1 (Compound 39-100) inhibits MAP3K1-mediated IKKβ phosphorylation and reduced levels of p-IKKβ in with an IC50 value of 2.3 uM, inhibits the growth of PC lines with lowmicromolar potencies.
IKAM-1 (Compound 39-100) reduces activated IKKβ levels, inhibits tumor growth, and reduces metastasis in mice pancreatic tumor models.

Physicochemical Properties

M.Wt 441.26
Formula C19H14BrFN6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(3-bromo-4-fluorophenyl)-3-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)urea

References

1. Napoleon JV, et al. Proc Natl Acad Sci U S A. 2022 May 3;119(18):e2115071119.

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