IKK 16
IKK 16 Basic information
- Product Name:
- IKK 16
- Synonyms:
-
- IKK Inhibitor
- [4-[(4-Benzo[b]thien-2-yl-2-pyriMidinyl)aMino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-Methanone
- IKK Inhibitor VII
- Methanone, [4-[(4-benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-
- 1-[4-[(4-Benzo[b]thien-2-yl-2-pyrimidinyl)amino]benzoyl]-4-(1-pyrrolidinyl)piperidine IKK-16 (IKK Inhibitor VII)
- 1-[4-[(4-Benzo[b]thien-2-yl-2-pyrimidinyl)amino]benzoyl]-4-(1-pyrrolidinyl)piperidine
- IKK16;IKK-16;IKK INHIBITOR VII
- CS-1847
- CAS:
- 873225-46-8
- MF:
- C28H29N5OS
- MW:
- 483.63
- Product Categories:
-
- NF-kB
- IκB/IKK
- Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds
- Inhibitors
- Mol File:
- 873225-46-8.mol
IKK 16 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- ≥23.05 mg/mL in DMSO; ≥11.3 mg/mL in EtOH with ultrasonic; insoluble in H2O
- form
- solid
- color
- White to yellow
- InChIKey
- BWZJBXAPRCVCKQ-UHFFFAOYSA-N
- SMILES
- C(C1=CC=C(NC2=NC=CC(C3SC4=CC=CC=C4C=3)=N2)C=C1)(N1CCC(N2CCCC2)CC1)=O
IKK 16 Usage And Synthesis
Uses
IKK-16 is a potential novel IκB kinase 2 (IKK2) inhibitor used in the treatment of various immune/inflammatory disorders.
Definition
ChEBI: [4-[[4-(1-benzothiophen-2-yl)-2-pyrimidinyl]amino]phenyl]-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone is a N-acylpiperidine and a member of benzamides.
Biological Activity
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].
in vivo
IKK 16 also demonstrates significant in vivo activity in an acute model of cytokine release. Both routes of administration of IKK 16 (30 mg/kg, sc) or orally (30 mg/kg, p.o) at the indicated dose results in a significant inhibition of 86% (sc) and 75% (p.o.). IKK 16(10 mg/kg, sc) is also active in the thioglycollate-induced peritonitis model in the mouse. The maximal inhibition of neutrophil extravasation in this model is about 50%[1]. Treatment of septic mice with IKK 16 (1 mg/kg body weight i.v.) results in a significantly increased degree of phosphorylation (P<0.05) of serine residues on Akt and eNOS in the liver[3].
target
IKK-2
IC 50
IKK2: 40 nM (IC50); IKK1: 200 nM (IC50); IKK: 70 nM (IC50); LRRK2: 50 nM (IC50)
References
[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.
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