GW3965

Agonist of NR1H2, NR1H3

Structure

Information

Protein target names: NR1H2, NR1H3

Mechanism of action: Agonist

In Vitro Validations

Uniprot ID: P55055
Target Class: NHR
Target SubClass: NR1 Subfamily
Potency: IC 50
Potency Value: 125 nM
Potency Assay: LXRalpha/SRC1 LiSA.
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: Yes some, see J Med Chem paper.
Target aliases:
Oxysterols receptor LXR-beta, UNR, NER, LXRB, NR1H ...

DOI Reference: 10.1021/jm0255116

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

Comments:

GW3965 has been widely used as a chemical probe for the liver X receptors, alpha and beta. GW3965 is commonly employed in parallel with another LXR agonist such as T1317. T1317 is approximately 10-fold more potent in agonizing the LXRs in cells but suffers from the liability of activity at a handful of other nuclear receptors, notably PXR. GW3965 has properties amenable for in vivo usage.

(last updated: 4 Aug 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

This appears to be a robust and credible probe for the investigation of LXR biology, though the primary literature reference is somewhat sparse in terms of utilization and limitation. It will be important for the community to report new findings using this probe to fully validate its applicability.

(last updated: 11 Aug 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

GW3965 is a selective non-steroidal agonist for the LXRa and LXRb receptors. GW3965 is suitable for in vivo use in mouse models where a 10mg/kg oral dose exceeds the LXR EC50. A complementary, structurally orthogonal tool is LXR-623, which could be used in parallel to confirm outcomes.

(last updated: 18 Aug 2017 )

SERP Ratings

Comments:

A 2020 publication shows that T0901317 exert unspecific effects on pancreatic β-cell function DOI: 10.1007/s12020-020-02241-4

(last updated: 9 Jul 2020 )