Inhibitor of ABCC8, KCNJ11



Protein target names: ABCC8 KCNJ11

Mechanism of action: Inhibitor

Primary References:

In Vitro Validations

Uniprot ID: Q09428
Target Class: Ion Channel
Target SubClass: Potassium channel
Potency: IC50
Potency Value: 106 nM
Potency Assay: In vitro assays with membranes from COS-1 cells expressing SUR-1. A KD of 50 nM was derived from the IC50 value. These data have been replicated in comparable experiments with HEK293 extracts (KD=0.4 nM) and BetaTC3 cells (KD=6.4 nM) using [3H]-labeled repaglinide.
PDB ID for probe-target interaction (3D structure): 6JB3 6JB1
Target aliases:
ATP-binding cassette sub-family C member 8, SUR1, ...

DOI Reference: 10.2337/diabetes.51.9.2789

In Cell Validations

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(last updated: 29 Apr 2020 )

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Repaglinide is a member of the meglitinide family of insulin secretagogues. Like the sulfonylurea class of anti-diabetes drugs, Repaglinide binds and inhibits the KATP (ATP-dependent potassium channel) in beta cells, causing membrane depolarization, calcium influx, and insulin secretion. The meglitinides, however, have slightly different biophysical interactions with the channel, and are more optimized for clinical use than for investigation as a probe in cell culture. If one is studying the KATP channel itself and insulin secretion in cells, the sulfonylureas seem to be quite good probes already, and would be preferable for use in the lab.

(last updated: 15 May 2020 )