Salt-inducible Kinase Inhibitor GRN-300

Preferred Label : Salt-inducible Kinase Inhibitor GRN-300;

NCIt synonyms : ARN3261; SIK Inhibitor GRN-300;

NCIt definition : 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.;

Molecule name : ARN 3261; ARN-3261; GRN-300; GRN 300;

NCI Metathesaurus CUI : CL1643295;

Details

Origin ID

C177416;

UMLS CUI

C5447750;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
chemical_or_drug_has_mechanism_of_action
- Receptor Tyrosine Kinase Inhibition [NCIt concept]
chemical_or_drug_has_physiologic_effect
- Inhibition of Cell Proliferation [NCIt concept]
- Signal Transduction Inhibition [NCIt concept]
concept_is_in_subset
- CTRP Agent Terminology [NCIt concept]
- CTRP Terminology [NCIt concept]
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_target
- Serine/Threonine-Protein Kinase SIK2 [NCIt concept]

Keyword's position in hierarchy(ies) :

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