LH846Casein kinases inhibitor CAS# 639052-78-1 |
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| Cas No. | 639052-78-1 | SDF | Download SDF |
| PubChem ID | 851474 | Appearance | Powder |
| Formula | C16H13ClN2OS | M.Wt | 316.81 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 45 mg/mL (142.04 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-(5-chloro-6-methyl-1,3-benzothiazol-2-yl)-2-phenylacetamide | ||
| SMILES | CC1=CC2=C(C=C1Cl)N=C(S2)NC(=O)CC3=CC=CC=C3 | ||
| Standard InChIKey | DYHAMRNAHTWYKY-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H13ClN2OS/c1-10-7-14-13(9-12(10)17)18-16(21-14)19-15(20)8-11-5-3-2-4-6-11/h2-7,9H,8H2,1H3,(H,18,19,20) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective inhibitor of casein kinase (CK) 1δ (IC50 values are 290 nM, 1.3 μM and 2.5 μM for CK1δ, ε and α); displays no inhibitory activity at CK2. Inhibits CK1δ-dependent phosphorylation and degradation of PER1 protein. Shown to lengthen the circadian period in U2OS cells, with minimal effect on amplitude. |
LH846 Dilution Calculator
LH846 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1565 mL | 15.7823 mL | 31.5647 mL | 63.1293 mL | 78.9117 mL |
| 5 mM | 0.6313 mL | 3.1565 mL | 6.3129 mL | 12.6259 mL | 15.7823 mL |
| 10 mM | 0.3156 mL | 1.5782 mL | 3.1565 mL | 6.3129 mL | 7.8912 mL |
| 50 mM | 0.0631 mL | 0.3156 mL | 0.6313 mL | 1.2626 mL | 1.5782 mL |
| 100 mM | 0.0316 mL | 0.1578 mL | 0.3156 mL | 0.6313 mL | 0.7891 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
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