LH846

Casein kinases inhibitor CAS# 639052-78-1

LH846

Catalog No. BCC4246----Order now to get a substantial discount!

Product Name & Size Price Stock
LH846: 5mg $58 In Stock
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Chemical structure

LH846

3D structure

Chemical Properties of LH846

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.
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.
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.

Biological Activity of LH846

DescriptionSelective 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

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LH846 Molarity Calculator

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Preparing Stock Solutions of LH846

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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Background on LH846

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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Description

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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