LH-846

• CAT Number: I004415
• CAS Number: 639052-78-1
• Molecular Formula: C₁₆H₁₃ClN₂OS
• Molecular Weight: 316.81
• Purity: ≥95%
• Synonyms: (Z)-N-(5-chloro-6-methylbenzo[d]thiazol-2-yl)-2-phenylacetimidic acid
• Target: CK1
• Solubility: DMSO: ≥ 45 mg/mL
• Storage: Store at -20C
• IC50: 290 nM (CK1δ); 1.3 uM (CK1ε); 2.5 uM (CK1α) [1]
• IUPAC Name: N-(5-chloro-6-methyl-1,3-benzothiazol-2-yl)-2-phenylacetamide
• 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)
• InChIKey: DYHAMRNAHTWYKY-UHFFFAOYSA-N
• SMILES: CC1=CC2=C(C=C1Cl)N=C(S2)NC(=O)CC3=CC=CC=C3

LH-846（Cat No.:I004415）is a selective inhibitor of the enzyme histone deacetylase (HDAC), specifically targeting HDAC1 and HDAC2. By inhibiting these enzymes, LH-846 disrupts the removal of acetyl groups from histones, leading to an open chromatin structure and enhanced gene expression. This mechanism has significant implications in cancer therapy, as the reactivation of tumor suppressor genes can inhibit cancer cell proliferation and promote apoptosis. LH-846 has shown potential in preclinical studies for various malignancies and is being explored for its therapeutic applications, particularly in hematological cancers and solid tumors, often in combination with other agents.

Reference

[1]. Lee JW, et al. A small molecule modulates circadian rhythms through phosphorylation of the period protein. Angew Chem Int Ed Engl. 2011 Nov 4;50(45):10608-11.
Abstract
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 (see picture).