LH846 |
| カタログ番号GC17466 |
LH846 は、CKIδ の選択的阻害剤であり、IC50 は 290 nM であり、CKIα および CKIε を阻害する効果は低く、IC50 はそれぞれ 2.5 μM および 1.3 μM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 639052-78-1
Sample solution is provided at 25 µL, 10mM.
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LH846 is an inhibitor of casein kinases with IC50 values of 290nM, 2.5μM and 1.3μM against CKIδ, CKIα and CKIε, respectively [1].
As a small inhibitor of casein kinase, LH846 is developed for the treatment of the diseases that have an underlying circadian disorder. LH846 is previously screened out from a cell-based assay using human U2OS cells. It affects the circadian rhythm and lengthens the period (10h) at concentration of 8μM. LH846 can inhibit the activity of CKIδ, CKIα and CKIε with IC50 values of 290nM, 2.5μM and 1.3μM, respectively. The specific target of it is CKIδ. When treated with a panel of about 50 kinases, LH846 exerts potent inhibition against CKIδ and less potent effects on CKIα and ROCK2. CK2 is not sensitive to LH846 [1].
References:
[1] Lee J W, Hirota T, Peters E C, et al. A small molecule modulates circadian rhythms through phosphorylation of the period protein. Angewandte Chemie, 2011, 123(45): 10796-10799.
| Cas No. | 639052-78-1 | SDF | |
| Chemical Name | (Z)-N-(5-chloro-6-methylbenzo[d]thiazol-2-yl)-2-phenylacetimidic acid | ||
| Canonical SMILES | CC1=CC(S2)=C(N=C2/N=C(O)/CC3=CC=CC=C3)C=C1Cl | ||
| Formula | C16H13ClN2OS | M.Wt | 316.81 |
| 溶解度 | DMF: 5 mg/mL,DMSO: 5 mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1565 mL | 15.7823 mL | 31.5647 mL |
| 5 mM | 0.6313 mL | 3.1565 mL | 6.3129 mL |
| 10 mM | 0.3156 mL | 1.5782 mL | 3.1565 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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