KIN1148

Category	Influenza Virus
CAS	1428729-56-9
Description	KIN1148, a small-molecule IRF3 agonist, associates with and activates recombinant RIG-I protein in cell-free assays. KIN1148 is a novel influenza vaccine adjuvant found to enhance flu vaccine efficacy.

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Product Information

Synonyms	KIN-1148; KIN 1148; KIN1148; N-([1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)naphthalene-2-carboxamide
IUPAC Name	N-([1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)naphthalene-2-carboxamide
Molecular Weight	361.44
Molecular Formula	C19H11N3OS2
Canonical SMILES	C1=CC=C2C=C(C=CC2=C1)C(=O)NC3=NC4=C(S3)C5=C(C=C4)SC=N5
InChI	1S/C19H11N3OS2/c23-18(13-6-5-11-3-1-2-4-12(11)9-13)22-19-21-14-7-8-15-16(17(14)25-19)20-10-24-15/h1-10H,(H,21,22,23)
InChIKey	YAISOECYKYATLL-UHFFFAOYSA-N
Purity	≥98% (HPLC)
Density	1.531±0.06 g/cm3
Solubility	DMSO: ≥100 mg/mL
Appearance	Light yellow to yellow (Solid)
Storage	Store in a cool and dry place (or refer to the Certificate of Analysis).
Animal Admin	The final liposomes prior to mixing with vaccine contained KIN1148 (5 mg/mL) and phospholipids (40 mg/mL) and are delivered intramuscularly (KIN1148 at 50 μg and phospholipid at 400 μg per dose). Blank liposomes are prepared without KIN1148 as vehicle control. KIN1148 liposome and blank liposome formulations are stable for at least 4 months at 4°C and are used for in vivo experiments within a month after preparation.
Complexity	519
Exact Mass	361.03435433
In Vitro	KIN1148 induces the dose-dependent nuclear translocation of IRF3 in PH5CH8 cells and specific activation of IRF3- responsive promoters. KIN1148 also elicits greater induction of endogenous IRF3-dependent ISG54 and OASL expression by PH5CH8 cells.
In Vivo	Prime-boost immunization of mice with a suboptimal dose of a monovalent pandemic influenza split virus H1N1 A/California/07/2009 vaccine plus KIN1148 protect against a lethal challenge with mouse-adapted influenza virus (A/California/04/2009) and induce an influenza virusspecific IL-10 and Th2 response by T cells derived from lung and lung-draining lymph nodes. Primeboost immunization with vaccine plus KIN1148, but not prime immunization alone, induce antibodies capable of inhibiting influenza virus hemagglutinin and neutralizing viral infectivity. Nevertheless, a single immunization with vaccine plus KIN1148 provide increased protection over vaccine alone and reduce viral load in the lungs after challenge.
Target	Influenza Virus
XLogP3-AA	5.3