LH 846 | CAS#639052-78-1 | casein kinase inhibitor

MedKoo Cat#: 531198 | Name: LH846

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

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: 316.80

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
10mg	USD 110.00	Ready to ship
25mg	USD 220.00	Ready to ship
50mg	USD 350.00	Ready to ship
100mg	USD 600.00	Ready to ship
200mg	USD 1,050.00	Ready to ship
500mg	USD 1,950.00	Ready to ship
1g	USD 2,950.00	2 Weeks
2g	USD 4,450.00	2 weeks

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Related CAS #

No Data

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

More Info

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.

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#XPR70221

QC Data

View QC data: current batch, Lot#XPR70221

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

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

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	38.0	119.95

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 316.80 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.

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:

In vivo protocol:

TBD

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.