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Molecule- J54

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Molecule- J54

J54

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.

Physiochemical properties:

Molecular Weight312.43 g/mol
Cas number4734-59-2
AppearanceSolid
Storage20ºC for long term, 4ºC for short term use
Solubility100 mM in DMSO

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).

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