REV-ERB

REV-ERB is a member of the nuclear receptor superfamily consisting of two similar proteins: REV-ERBα and REV-ERBβ. REV-ERBα and REV-ERBβ, are encoded by Nr1d1 and Nr1d2, and link circadian rhythms and metabolism. REV-ERBs lack the canonical NR activation domain, and thus function as a transcriptional repressor. Like other NRs, REV-ERBs can be regulated by ligands, including naturally occurring heme (22, 23), which modulate their repressive activity. Two REV-ERB molecules, usually present as a dimer, compete with retinoic acid receptor-related orphan receptor (ROR) for the binding to the ROR response element DNA sequence (RORE) region. REV-ERB is involved in the regulation of many physiological processes, from circadian rhythm, to immune function and metabolism. Accordingly, REV-ERB has been considered as a promising, but difficult drug target for the treatment of numerous diseases.

REV-ERB Related Products (11):

By Effects:	Inhibitors (4) Agonists (2) Antagonist (1) Activator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-14415

SR8278	Antagonist	99.94%
SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC₅₀ of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease.

HY-148711

STL1267	Activator	99.86%
STL1267 is a potent and cross-the-blood-brain barrier REV-ERB agonist with a K_i value of 0.16 µM for REV-ERBα. STL1267 shows no cytotoxicity. STL1267 inhibits the gene expression of BMAL1.

HY-14414

GSK4112	Inhibitor	99.87%
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.

HY-13421

SR1001	Inhibitor	99.89%
SR1001 is a selective ROR_α and ROR_γt inverse agonist with K_is 172 and 111 nM, respectively.

HY-16988

SR9011		99.78%
SR9011 is a REV-ERBα/β agonist with IC₅₀s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

HY-117516

SR10067	Agonist	≥99.0%
SR10067 is a potent, selective and brain penetrant REV-ERB agonist. SR10067 has high affinity for Rev-Erbβ and Rev-Erbα with IC₅₀ values of 160 nM and 170 nM, respectively. SR10067 can be used for the research of metabolic diseases and neuropsychiatric disorders.

HY-148103

SR12418		99.93%
SR12418 is a REV-ERB-specific synthetic ligand with IC₅₀s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research.

HY-16988A

SR9011 hydrochloride		99.39%
SR9011 hydrochloride is a REV-ERBα/β agonist with IC₅₀s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

HY-156458

SR-29065	Agonist
SR-29065 is a selective REV-ERBα agonist, can be used for autoimmune disorders research.

HY-163136A

Autophagy/REV-ERB-IN-1 hydrochloride	Inhibitor
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.

HY-163136

Autophagy/REV-ERB-IN-1	Inhibitor
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.

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