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 相关产品（3）

货号	产品名	Cas	产品描述
PL10976	SR10067	1380548-02-6	SR10067 是一种强效、选择性和脑渗透性 REV-ERB 激动剂。SR10067 对 Rev-Erbβ 和 Rev-Erbα 具有高亲和力， IC50 值分别为 160 nM 和 170 nM。 SR10067 可用于代谢疾病和神经精神疾病的研究。
PL10975	SR9011 hydrochloride	2070014-94-5	SR9011 hydrochloride 是一种 REV-ERBα/β 激动剂，作用于 REV-ERBα 和 REV-ERBβ，IC50s 分别为 790 nM 和 560 nM。
PL10974	STL1267	1429024-58-7	STL1267 是一种有效的可穿过血脑屏障的 REV-ERB 激动剂，对 REV-ERBα 的Ki 值为 0.16 µM。STL1267 没有表现出细胞毒性。STL1267 抑制 BMAL1 的基因表达。