REV-ERB Inhibitor

GSK4112 (SR6452) is a Rev-erbα agonist with an EC₅₀ value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways.

SR1001 is a selective ROR_α and ROR_γt inverse agonist with K_is 172 and 111 nM, respectively.

(R)-SR-29065 is a selective REV-ERBα inhibitor with a IC₅₀ of 10 nM. (R)-SR-29065 is applicable to research related to autoimmune diseases.

GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC₅₀s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.

GSK1362 is a selective inverse agonist of REV-ERB. GSK1362disrupts the interaction of REV-ERBα with repressive co-modulators (NCoR1, SMRT2, RIP140). GSK1362 exerts an inverse agonist effect by increasing the transcription of BMAL1 to relieve BMAL1 repression by endogenous REV-ERB ligands. GSK1362 suppresses LPS (HY-D1056)-induced inflammatory cytokine expression, inhibits IL-1β-induced Cxcl5 transcription in cells. GSK1362 can be used for the study of inflammatory diseases.

Autophagy/REV-ERB-IN-1 hydrochloride (Compound 24) is a dual autophagy and REV-ERB inhibitor with anticancer activity. Autophagy/REV-ERB-IN-1 (hydrochloride) has improved potency in blocking autophagy, enhanced toxicity against cancer cells. Autophagy/REV-ERB-IN-1 (hydrochloride) can be used for the research for melanoma.

Autophagy/REV-ERB-IN-1 (compound 24) is a dual inhibitor of autophagy and REV-ERB. Autophagy/REV-ERB-IN-1 has anti-tumor activity with a CC₅₀ value of 2.3 μM on BTB-474 cells.

ARN5187 trihydrochloride (Standard) is the analytical standard of ARN5187 trihydrochloride (HY-103691A). This product is intended for research and analytical applications. ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis.

SR1001 (Standard) is the analytical standard of SR1001. This product is intended for research and analytical applications. SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.