s9

J54

Molecule NameJ54
 Id 
StructureAdd image
Molecular FormulaC10H20N2Os
Molecular Weight312.43 g/mol
AppearanceBuff colour s
Purity> 95%
Solubility100 mM in DMSO
 J54 is a potent human TLK inhibitor. It has been shown to exhibit a micromolar range of enzyme inhibition through in vitro assays
Biological Activity

1. Potent TLK1 non-ATP dependent inhibitor with an IC50 of 15 µM in ADP-Glo kinase assay.

2. Displays lowered dopaminergic activity compared to Thioridazine (THD).

3. Cytotoxic towards androgen-sensitive LNCaP cells

4. Reduces PCa tumors in 51 days when administered at a dose of 10mg/kg along with Bicalutamide.

Storage20ºC for long term, 4ºC for short term use

References:
1. Priya, B., Chhabria, D., Dhongdi, J. M., & Kirubakaran, S. (2024). A novel approach to investigate the combinatorial effects of TLK1 (Tousled-Like Kinase1) inhibitors with Temozolomide for glioblastoma therapy. Bioorganic Chemistry, 151, 107643.
2. Olatunde, D., & De Benedetti, A. (2024). TLK1> Nek1 Axis Promotes Nuclear Retention and Activation of YAP with Implications for Castration-Resistant Prostate Cancer. Cancers, 16(16), 2918.
3. Bhoir, S., Ogundepo, O., Yu, X., Shi, R., & De Benedetti, A. (2023). Exploiting TLK1 and Cisplatin Synergy for Synthetic Lethality in Androgen-Insensitive Prostate Cancer. Biomedicines, 11(11), 2987.
4. Khalil, M. I., & De Benedetti, A. (2022). The TLK1–MK5 Axis Regulates Motility, Invasion, and Metastasis of Prostate Cancer Cells. Cancers, 14(23), 5728.
5. Khalil, M. I., Madere, C., Ghosh, I., Adam, R. M., & De Benedetti, A. (2021). Interaction of TLK1 and AKTIP as a potential regulator of AKT activation in castration-resistant prostate cancer progression. Pathophysiology, 28(3), 339-354.
6. Singh, V., Bhoir, S., Chikhale, R. V., Hussain, J., Dwyer, D., Bryce, R. A., … & De Benedetti, A. (2020). Generation of phenothiazine with potent anti-TLK1 activity for prostate cancer therapy. Iscience, 23(9).

en_GBEnglish (UK)