GLPG3970, SIK2/3 inhibitor (TBI4446)

Description

Product Details

Formal Name: 8-Methoxy-6-[7-(2-morpholin-4-ylethoxy)imidazo[1,2-a]pyridin-3-yl]-2-(2,2,2-trifluoroethyl)-3,4-dihydroisoquinolin-1-one

Molecular Formula: C₂₅H₂₇F₃N₄O₄

Formula Weight: 504.5

CAS Number: 2403733-82-2

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 50 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

SIK2/3 inhibitor

Functions

Potent and selective (against a panel of 372 kinases) SIK2/3 inhibitor (IC₅₀s: SIK2 = 7.8 nM, SIK3 = 3.8 nM). It reduced THFα and increased IL-10 levels in an LPS challenge model in mice and displayed efficacy in a mouse model of colitis. GLPG3970 promoted reprogramming of human myeloid cells toward an anti-inflammatory phenotype, reprogrammed monocyte-dendritic differentiation toward stable tolerogenic phenotypes, and suppressed T-cell activation. It also displayed efficacy in mouse models of psoriasis and arthritis.

Application Procedures

First dissolved in DMSO (up to at least 50 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4446_GLPG3970_Datasheet

MSDS:

TBI4446_GLPG3970_MSDS

Research use only.