circadian

KL001 是一流的隐花色素蛋白 (CRY)稳定剂，可与 CRY1 和 CRY2 特异性相互作用。其中CRY 是一种对蓝光敏感的黄素蛋白，参与调节动植物的昼夜节律。KL001能够防止泛素依赖性 CRY 降解，从而延长了昼夜节律周期，具有控制空腹激素诱导的糖异生的潜力。

Tasimelteon (BMS-214778) 是一种褪黑激素受体激动剂，用于治疗盲人的非 24 小时睡眠-觉醒障碍。

KL201 是一种昼夜节律调制器，是 CRY1选择性的 稳定剂， 对 CRY2 没有稳定作用。KL201 延长了细胞和组织中的昼夜节律周期。

Prolylleucine (((Benzyloxy)carbonyl)-L-prolyl-D-leucine) 是一种二肽，含有支链氨基酸，可以影响动物的昼夜节律和行为。

(E Z)-GO289 是一种选择性酪蛋白激酶 2 抑制剂，IC50值为 7 nM。它可显着延长昼夜节律周期，表现出与细胞时钟功能相关的癌细胞生长的细胞类型依赖性抑制。

Betaine chloride (Betaine hydrochloride) 是一种天然化合物，在许多食物中能够发现，也是能够维持正常 DNA 甲基化模式的特性甲基供体。

1A-116 是 Rac1的抑制剂，对几种类型的癌症具有抗肿瘤和抗转移作用，如乳腺癌。

Hesperin (6-MSITC) 是从橙皮中分离得到的黄酮化合物，是植物中的昼夜节律去烯化酶，抑制 3T3-L1 和 RAW264.7 细胞中脂质积累和活性氧和活性氮的产生。

TIK-301 is a chlorinated melatonin derivative and a potent, high-affinity, and orally active melatonin MT1 and MT2 receptors agonist (Kis: 0.081 nM and 0.042 nM, respectively). TIK-301 is also a 5-HT2B 5-HT2C receptor antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

E3 Ligase Ligand-linker Conjugate 163 是 AH078 的 E3 连接酶配体 (E3 Ligase Ligand 58)-连接子偶联物。AH078 是一种 PROTAC，旨在靶向降解 CK1δ 和 CK1ε，可用于研究昼夜节律失调相关的疾病。

GR 196429, a melatonin receptor agonist, exhibits selectivity for the MT1 subtype. This compound not only promotes sleep and alters circadian rhythms but also stimulates melatonin release in mice.

LY2033298 是毒蕈碱 M4 受体的正变构调节剂，可增强奥昔莫林对仓鼠昼夜节律活动中光诱导的相移的抑制作用，可用于与神经系统相关的疾病。

KL044 是一种隐花色素 1（CRY1） 激活剂，可延长昼夜节律并抑制 PER2 的活性。 KL044 通过抑制cAMP PKA CREB 通路来抑制黑色素生成。

Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.4References1. Khavinson, V.K., and Myl'nikov, S.V. Effect of epithalone on the age-specific changes in the time course of lipid peroxidation in Drosophila melanogaster. Bull. Exp. Biol. Med. 130(11), 1116-1119 (2000).2. Anisimov, V.N., Khavinson, V.K., Popovich, I.G., et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology 4(4), 193-202 (2003).3. Kossoy, G., Anisimov, V.N., Ben-Hur, H., et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H He mice. In Vivo 20(2), 253-257 (2006).4. Khavinson, V., Goncharova, N., and Lapin, B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro. Endocrinol. Lett. 22(4), 251-254 (2001). Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.4 References1. Khavinson, V.K., and Myl'nikov, S.V. Effect of epithalone on the age-specific changes in the time course of lipid peroxidation in Drosophila melanogaster. Bull. Exp. Biol. Med. 130(11), 1116-1119 (2000).2. Anisimov, V.N., Khavinson, V.K., Popovich, I.G., et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology 4(4), 193-202 (2003).3. Kossoy, G., Anisimov, V.N., Ben-Hur, H., et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H He mice. In Vivo 20(2), 253-257 (2006).4. Khavinson, V., Goncharova, N., and Lapin, B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro. Endocrinol. Lett. 22(4), 251-254 (2001).

SR9009 (Stenabolic) 是一种REV-ERBα β激动剂，可增加由 REV-ERBα ERBβ 调节的基因的组成性抑制，IC50分别为 670 nM 和 800 nM。

KS15 is a chemical compound that acts as an inhibitor on the interactions between cryptochromes, specifically CRY1 and CRY2, and the CLOCK: BMAL1 heterodimer. This compound, with an EC50 value of 4.9 μM, hinders the feedback actions of CRYs on E-box-dependent transcription. The CLOCK: BMAL1 heterodimer is a vital transcriptional regulator for the mammalian circadian clock. In addition, KS15 exhibits significant anti-proliferative activity.

FT709 是选择性的USP9X 有效抑制剂 (IC50: 82 nM)。其中USP9X 与中心体功能、EGF 受体降解、有丝分裂期间的染色体排列、化学致敏和昼夜节律有关。

PF-05236216 hydrochloride is a brain penetrant, potent and selective inhibitor of casein kinase 1 delta epsilon (CK1δ ε) that modulates circadian rhythms in mice.

Brevicompanine B is a fungal metabolite that has plant growth and circadian rhythm regulatory activity. Brevicompanine B inhibits primary root growth in Arabidopsis seedlings and disrupts the transcription of various genes involved in the regulation of plant circadian rhythm. It is active against P. falciparum.

CLK8 是一种具有选择性的 CLOCK 抑制剂，可结合并干扰 CLOCK 活性，破坏 CLOCK 和 BMAL1 之间的相互作用，可调节昼夜节律振幅。CLK8 可用于研究与昼夜节律相关的疾病。

VU661, 一种吩嗪甲酰胺类化合物，作为昼夜节律调节剂能促使昼夜节律周期延长，该小分子具备氧化还原活性。

Delta (Phospho) Sleep Inducing Peptide (DSIP-P) 是促进睡眠效应持久的多肽，能诱导大鼠昼夜运动行为的改变。

Jujubosides have hypnotic effect on normal rats, may be influenced by circadian rhythm and the serotonergic system may involve in the hypnotic effect of jujubosides, jujubosides may be good source of lead compounds for novel hypnotics.

Potent, endogenous neuromedin U receptor agonist (EC50 values are 65 and 91 pM at NMU1 and NMU2 respectively). Induces phase shifts in the circadian rhythm of locomotor activity following i.c.v. administration. Potent endogenous anorexigenic peptide.