IKK-16 (IKK Inhibitor VII)

IKK-16 (IKK Inhibitor VII)

Catalog Number:
L002370114APE
Mfr. No.:
APE-B1586
Price:
$292
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      • Overview
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          Background

          IKK-16 (IKK Inhibitor VII) is a novel inhibitor of IκB kinase (IKK) with the IC50 values of 0.04μM, 0.2μM and 0.07μM for IKK2, IKK1 and IKK complex, respectively [1].
          IKK-16 (IKK Inhibitor VII) is a 2-benzamido-pyrimidines and selective inhibitor of IκB kinase (IKK). IKK-16 has been reported to effectively inhibit TNFα release into plasma upon LPS-challenge in the rat. In addition, IKK-16 has been found to be active at thioglycollate-induced peritonitis model in the mouse. Furthermore, IKK-16 has revealed to be an orally bio-available in rats and mice, and have significant in vivo activity in an acute model of cytokine release [1].

          [1] Waelchli R1, Bollbuck B, Bruns C, Buhl T, Eder J, Feifel R, Hersperger R, Janser P, Revesz L, Zerwes HG, Schlapbach A.Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. Epub 2005 Oct 19.

      • Properties
        • Alternative Name
          [4-[[4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino]phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone
          CAS Number
          873225-46-8
          Molecular Formula
          C28H29N5OS
          Molecular Weight
          483.63
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥23.05 mg/mL in DMSO; ≥11.3 mg/mL in EtOH with ultrasonic; insoluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Robeson AC, Lindblom KR, et al. "Dimer-specific immunoprecipitation of active caspase-2 identifies TRAF proteins as novel activators." EMBO J. 2018 Jun 6. pii: e97072. PMID:29875129

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