CLK8

COA

CAS编号: 898920-65-5
分子式: C₂₉H₂₆N₂O₆
分子量: 498.53
PubChem编号: 4869040

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货号 (SKU)	包装规格	是否现货
C647919-5mg	5mg	期货
C647919-10mg	10mg	期货
C647919-25mg	25mg	期货
C647919-50mg	50mg	期货

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Cryptochrome (1) Metabolic Enzyme/Protease (4889) Nucleic Acid Metabolism (949)

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基本描述

英文名称	CLK8
生化机理	CLK8 是一种强效的特异性 CLOCK 抑制剂，可破坏 CLOCK 与 BMAL1 之间的相互作用，并干扰 CLOCK 的核转位。CLK8 可用于研究与昼夜节律受阻有关的疾病。
储存温度	2-8°C储存,避光,干燥
运输条件	冰袋运输
作用类型	抑制剂
产品介绍	CLK8 is a potent and specific CLOCK inhibitor that can disrupt the interaction between CLOCK and BMAL1 and interfere with nuclear translocation of CLOCK. CLK8 can be used for the research of disorders associated with dampened circadian rhythms In Vitro CLK8 (10-40 μM; 4-6 d) enhances the amplitude of the Bmal1-dLuc signal in U2OS and NIH 3T3 cells in a dose-dependent manner with no period change. CLK8 (10-40 μM) reduces BMAL1-CLOCK interaction, whereas the interaction between CLOCK-F80A, K220A and BMAL1 is not affected in HEK293T cells. CLK8 (20 μM; 2 d) reduces nuclear localization of CLOCK in U2OS cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CLK8 (25 mg/kg; a single i.p.) decreases CLOCK levels in whole cell lysates of the mouse livers, whereas the levels of BMAL1 and CRY1 are unaltered . CLK8 (5-1000 mg/kg; i.p.) exhibits no mortality or clinical signs (dyspnea, hyporeflexia, reduced locomotor activity, piloerection, hunched posture, and corneal opacity) at the doses of 5 and 25 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J mice (8 weeks, 18-24 g) Dosage: 25 mg/kg Administration: A single i.p. Result: A decrease in CLOCK levels was detected in whole cell lysates of the mouse livers, whereas the levels of BMAL1 and CRY1 were unaltered. Decreased the abundance of CLOCK in the nucleus. The abundances of cytosolic and nuclear BMAL1 and CRY1 were unaltered. Decreased Cry1 transcriptional level. Form:Solid IC50& Target:CLOCK

名称和识别符

IIUPAC Name	2-[[2-[(8,8-dimethyl-2-oxo-4-phenyl-9,10-dihydropyrano[2,3-h]chromen-5-yl)oxy]acetyl]amino]benzamide
INCHI	1S/C29H26N2O6/c1-29(2)13-12-19-22(37-29)15-23(35-16-24(32)31-21-11-7-6-10-18(21)28(30)34)26-20(14-25(33)36-27(19)26)17-8-4-3-5-9-17/h3-11,14-15H,12-13,16H2,1-2H3,(H2,30,34)(H,31,32)
InChi Key	SVELPNHVEDZZRQ-UHFFFAOYSA-N
Smiles	CC1(CCC2=C3C(=C(C=C2O1)OCC(=O)NC4=CC=CC=C4C(=O)N)C(=CC(=O)O3)C5=CC=CC=C5)C
Isomeric SMILES	CC1(CCC2=C3C(=C(C=C2O1)OCC(=O)NC4=CC=CC=C4C(=O)N)C(=CC(=O)O3)C5=CC=CC=C5)C
PubChem CID	4869040
分子量	498.53

化学和物理性质

溶解性	DMSO : 50 mg/mL (100.29 mM; Need ultrasonic)
分子量	498.500 g/mol
XLogP3	4.400
氢键供体数Hydrogen Bond Donor Count	2
氢键受体数Hydrogen Bond Acceptor Count	6
可旋转键计数Rotatable Bond Count	6
精确质量Exact Mass	498.179 Da
单同位素质量Monoisotopic Mass	498.179 Da
拓扑极表面积Topological Polar Surface Area	117.000 Å²
重原子数Heavy Atom Count	37
形式电荷Formal Charge	0
复杂度Complexity	910.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

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