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20

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9608	KL201	Others	Others
	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。
T14004	1A-116	Rho	Cell Cycle/Checkpoint
	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。
T22891	KL001 KL 001,KL-001	Others	Others
	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。
TP1264	Prolylleucine ((Benzyloxy)carbonyl)-L-prolyl-D-leucine	Others	Others
	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。
T9356	(E/Z)-GO289	Casein Kinase	Metabolism; Stem Cells
	(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。
T3495	Tasimelteon 他司美琼,VEC-162,BMS-214778	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	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。
T73573	CLK8	Others	Others
	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。
T32401	KL044 KL 044,KL-044	Others	Others
	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。
T27931	LY2033298 LY 2033298,LY-2033298	AChR	Neuroscience
	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。
T3685	SR9009 Stenabolic,REV-ERB Agonist II	Autophagy	Autophagy
	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。
TP1980	Neuromedin S(rat) Neuromedin S (rat)
	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.
T38433	KS15
	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.
T27430	GR 196429 GR-196429,GR 196,429,GR-196,429,GR196429,GR196,429
	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.
T70812	PF-05236216 hydrochloride
	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.
T80849	VU661
	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。
T82587	Delta (Phospho) Sleep Inducing Peptide DSIP-P
	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。
T17095	TIK-301 PD-6735,LY-156735	5-HT Receptor	GPCR/G Protein; Neuroscience
	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.
T63375	FT709
	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。
TP2194	Neuropeptide Y (scrambled)	Others	Others
	Neuropeptide Y (NPY) is a 36-amino acid neuropeptide that exerts its activity via G-protein-coupled receptors. NPY is widely distributed in the peripheral and central nervous systems. It modulates a variety of physiological processes, e.g. the central reg
T35993	Epitalon (acetate)
	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 melatoni...

化合物

Cat.No: T9608

Target: Others

Cat.No: T14004

Target: Rho

Cat.No: T22891

Synonym: KL 001,KL-001

Target: Others

Cat.No: TP1264

Synonym: ((Benzyloxy)carbonyl)-L-prolyl-D-leucine

Target: Others

Cat.No: T9356

Target: Casein Kinase

Cat.No: T3495

Synonym: 他司美琼,VEC-162,BMS-214778

Target: Melatonin Receptor, MT Receptor

Cat.No: T73573

Target: Others

Cat.No: T32401

Synonym: KL 044,KL-044

Target: Others

Cat.No: T27931

Synonym: LY 2033298,LY-2033298

Target: AChR

Cat.No: T3685

Synonym: Stenabolic,REV-ERB Agonist II

Target: Autophagy

Neuromedin S(rat)

Cat.No: TP1980

Synonym: Neuromedin S (rat)

Cat.No: T38433

Cat.No: T27430

Synonym: GR-196429,GR 196,429,GR-196,429,GR196429,GR196,429

PF-05236216 hydrochloride

Cat.No: T70812

Cat.No: T80849

Delta (Phospho) Sleep Inducing Peptide

Cat.No: T82587

Synonym: DSIP-P

Cat.No: T17095

Synonym: PD-6735,LY-156735

Target: 5-HT Receptor

Cat.No: T63375

Neuropeptide Y (scrambled)

Cat.No: TP2194

Target: Others

Epitalon (acetate)

Cat.No: T35993

Cat. No.	Product Name	Target	Signaling Pathways
T71896	Brevicompanine B
	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.
TN1812	Jujuboside B1 酸枣仁皂苷 B1	5-HT Receptor	GPCR/G Protein; Neuroscience
	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.

天然产物

Brevicompanine B

Cat.No: T71896

Cat.No: TN1812

Synonym: 酸枣仁皂苷 B1

Target: 5-HT Receptor

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