| Identification | Back Directory | [Name]
2-[[2-[(8,8-dimethyl-2-oxo-4-phenyl-9,10-dihydropyrano[2,3-h]chromen-5-yl)oxy]acetyl]amino]benzamide | [CAS]
898920-65-5 | [Synonyms]
CLK8
2-[[2-[(8,8-dimethyl-2-oxo-4-phenyl-9,10-dihydropyrano[2,3-h]chromen-5-yl)oxy]acetyl]amino]benzamide
Benzamide, 2-[[2-[(9,10-dihydro-8,8-dimethyl-2-oxo-4-phenyl-2H,8H-benzo[1,2-b:3,4-b']dipyran-5-yl)oxy]acetyl]amino]- | [Molecular Formula]
C29H26N2O6 | [MDL Number]
MFCD06769505 | [MOL File]
898920-65-5.mol | [Molecular Weight]
498.53 |
| Chemical Properties | Back Directory | [Boiling point ]
788.9±60.0 °C(Predicted) | [density ]
1.326±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.50±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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[1].
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[1]. | Animal Model: | Male C57BL/6J mice (8 weeks, 18-24 g)[1] | | 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.
|
| [References]
[1] Doruk YU, et, al. A CLOCK-binding small molecule disrupts the interaction between CLOCK and BMAL1 and enhances circadian rhythm amplitude. J Biol Chem. 2020 Mar 13;295(11):3518-3531. DOI:10.1074/jbc.RA119.011332 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
|