267654-00-2

Usage

Uses

Used in Pharmaceutical Industry:
BML-259 is used as a research tool for studying the role of Cdk5/p25 and Cdk2 in cell cycle regulation and their involvement in various diseases, including neurodegenerative disorders and cancer.
Used in Neurodegenerative Disease Research:
BML-259 is used as a therapeutic agent for the treatment of neurodegenerative diseases, such as Alzheimer's disease, where the inhibition of Cdk5/p25 has been shown to protect neurons from degeneration and improve cognitive function.
Used in Cancer Therapy:
BML-259 is used as a potential anticancer drug, targeting the Cdk2 activity, which plays a critical role in cell cycle progression and is often dysregulated in various types of cancer. By inhibiting Cdk2, BML-259 can potentially arrest the cell cycle and induce apoptosis in cancer cells, leading to the suppression of tumor growth.
Used in Drug Discovery and Development:
BML-259 serves as a lead compound for the development of novel Cdks inhibitors with improved potency, selectivity, and pharmacokinetic properties. It can be further optimized and modified to develop more effective drugs for the treatment of various diseases, including neurodegenerative disorders and cancer.

References

1) Helal et al. (2004) Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease; Bioorg. Med. Chem. Lett. 14 5521

Upstream product

• 590-86-3 isovaleraldehyde 
• 64932-36-1 2-bromo-3-methyl-butyraldehyde 
• 103-82-2 phenylacetic acid 
• 101080-15-3 5-isopropylthiazol-2-amine 

Relevant academic research and scientific papers

2-AMINO-THIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS ANTITUMOR AGENTS

Compounds which are 2-amino-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1-C8 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally further substituted group selected from: i) straight or branched C1-C8 alkyl or C2-C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease

High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320 nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved.