LH846
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MedKoo CAT#: 531198

CAS#: 639052-78-1

Description: LH846 is a selective inhibitor of casein kinase. IC50 values of LH846 are 290 nM, 1.3 μM and 2.5 μM for CK1δ, ε and α). LH 846 has been shown to inhibit CK1δ-dependent phosphorylation and degradation of PER1 protein and to lengthen the circadian period in U2OS cells.


Chemical Structure

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LH846
CAS# 639052-78-1

Theoretical Analysis

MedKoo Cat#: 531198
Name: LH846
CAS#: 639052-78-1
Chemical Formula: C16H13ClN2OS
Exact Mass: 316.0437
Molecular Weight: 316.803
Elemental Analysis: C, 60.66; H, 4.14; Cl, 11.19; N, 8.84; O, 5.05; S, 10.12

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 Same day
25.0mg USD 250.0 Same day
50.0mg USD 450.0 Same day
100.0mg USD 650.0 Same day
200.0mg USD 1050.0 Same day
500.0mg USD 1950.0 Same day
1.0g USD 2950.0 Same day
2.0g USD 4450.0 2 Weeks
5.0g USD 6450.0 2 Weeks
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Synonym: LH846; LH-846; LH 846.

IUPAC/Chemical Name: N-(5-Chloro-6-methyl-2-benzothiazolyl)benzeneacetamide

InChi Key: DYHAMRNAHTWYKY-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(NC1=NC2=CC(Cl)=C(C)C=C2S1)CC3=CC=CC=C3

Appearance: Yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: 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.
In vitro activity: A high-throughput cell-based screen identified a benzothiazole analogue, LH846, which induces period lengthening of the circadian rhythm. Affinity chromatography coupled with mass spectrometry and genomic analysis identified protein kinase CKIδ as the biological target of LH846. The benzothiazole derivative LH846 (8 μM) lengthened the period (10 h) with minimal effect on the amplitude of both Per2-dLuc and Bmal1-dLuc rhythms in U2OS cells (Figure 1). In vitro kinase profiling against a panel of around 50 kinases revealed that LH846 strongly inhibited CKIδ and, with less potency CKIα and ROCK2 (see Table 2S in the Supporting Information). Determination of the half maximal inhibitory concentration (IC50) based on an in vitro assay revealed that LH846 inhibited CKIδ with an IC50 of 290 nM, CKIα with an IC50 of 2.5 μM, CKIε with an IC50 of 1.3 μM and had no effect on CK2 (see Figure 1S in the Supporting Information). Taken together, these results suggest that CKIδ is the biological target of LH846. Reference: Angew Chem Int Ed Engl. 2011 Nov 4; 50(45): 10608–10611. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3755734/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.0 119.95

Preparing Stock Solutions

The following data is based on the product molecular weight 316.803 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Lee JW, Hirota T, Peters EC, Garcia M, Gonzalez R, Cho CY, Wu X, Schultz PG, Kay SA. A small molecule modulates circadian rhythms through phosphorylation of the period protein. Angew Chem Int Ed Engl. 2011 Nov 4;50(45):10608-11. doi: 10.1002/anie.201103915. Epub 2011 Sep 26. PMID: 21954091; PMCID: PMC3755734.
In vitro protocol: 1. Lee JW, Hirota T, Peters EC, Garcia M, Gonzalez R, Cho CY, Wu X, Schultz PG, Kay SA. A small molecule modulates circadian rhythms through phosphorylation of the period protein. Angew Chem Int Ed Engl. 2011 Nov 4;50(45):10608-11. doi: 10.1002/anie.201103915. Epub 2011 Sep 26. PMID: 21954091; PMCID: PMC3755734.
In vivo protocol: TBD

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1: Lee JW, Hirota T, Peters EC, Garcia M, Gonzalez R, Cho CY, Wu X, Schultz PG,
Kay SA. A small molecule modulates circadian rhythms through phosphorylation of
the period protein. Angew Chem Int Ed Engl. 2011 Nov 4;50(45):10608-11. doi:
10.1002/anie.201103915. PubMed PMID: 21954091; PubMed Central PMCID: PMC3755734.

LH846

10.0mg / USD 150.0


Additional Information

Unlike the great majority of protein kinases, which are tightly regulated enzymes, CK2 is endowed with high constitutive activity, a feature that is suspected to underlie its oncogenic potential and possible implication in viral infections. This makes CK2 an attractive target for anti-neoplastic and antiviral drugs.