| Identification | Back Directory | [Name]
3-Ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-2-(2-pyridinylmethylene)-4-thiazolidinone | [CAS]
812647-88-4 | [Synonyms]
YM-08
YM-08, blood-brain barrier permeable Hsp70 inhibitor
3-Ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-2-(2-pyridinylmethylene)-4-thiazolidinone
4-Thiazolidinone, 3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-2-(2-pyridinylmethylene)- | [Molecular Formula]
C19H17N3OS2 | [MDL Number]
MFCD26961118 | [MOL File]
812647-88-4.mol | [Molecular Weight]
367.49 |
| Hazard Information | Back Directory | [Uses]
YM-08 (Compounds 7a) is a brain-penetrant inhibitors of SIRT2,with the IC50 of 19.9 μM. YM-08 also is inhibitor of Hsp70[1]. | [Biochem/physiol Actions]
YM-08 is a Heat Shock Protein 70 (Hsp70) inhibitor that is blood-brain barrier permeable. YM-08 is a neutral derivative of the Hsp70 inhibitor MKT-077. MKT-077 reduces tau levels in cellular models, but it doesn′t penetrate the blood brain barrier. Although YM-08 was somewhat less effective than MKT-077 in anti-tau and anticancer assays, it selectively reduced pathogenic tau in brain slices, which MKT-077 did not. Furthermore,YM-08 was not retained in the kidney leading one to speculate that it would not have the nephrotoxicity that was a problem for MKT-077 in clinical trials. | [IC 50]
HSP70 | [References]
[1] Abbotto E, et al. Novel Thiazole-Based SIRT2 Inhibitors Discovered via Molecular Modelling Studies and Enzymatic Assays. Pharmaceuticals (Basel). 2023;16(9):1316. Published 2023 Sep 18. DOI:10.3390/ph16091316 |
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