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salt-inducible kinase inhibitor GRN-300

An orally bioavailable small molecule inhibitor of the salt inducible kinases 2 (SIK2) and 3 (SIK3), with potential antineoplastic activity. Upon oral administration of SIK inhibitor GRN-300, this agent targets, binds to and blocks the activity of SIK2 and SIK3. This prevents SIK2/3-mediated signaling, blocks centrosome separation, and inhibits proliferation in SIK2/3-overexpressing tumor cells. GRN-300 may enhance tumor sensitivity to other chemotherapeutic agents. SIK2/3, serine/threonine centrosome kinase family members required for bipolar mitotic spindle formation, are overexpressed in a variety of tumor cell types.
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Synonym:ARN3261
SIK inhibitor GRN-300
Code name:ARN 3261
GRN 300
GRN300
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