**Background**
Cyclin-dependent kinase 9 (CDK9) is a critical regulator of transcription elongation, playing a pivotal role in the phosphorylation of the RNA polymerase II C-terminal domain. Due to its essential role in the expression of short-lived proteins, including various oncogenes and anti-apoptotic factors, CDK9 has become a highly attractive target for the development of novel anticancer therapies. Dysregulation of CDK9 is often associated with the progression of various malignancies, making the search for highly selective inhibitors a priority in oncology. In this context, we will introduce a potent CDK9 inhibitor – CDK9-IN-14.
**Definition**
CDK9-IN-14 is a potent and selective CDK9 inhibitor with an IC50 value of 6.92 nM.
**In Vitro and In Vivo Studies**
According to the CDK9-IN-14 description, this compound exhibits high selectivity and low toxicity with minimal side effects. In terms of CDK9-IN-14 in vitro activity, the compound demonstrated a strong inhibitory effect in MV4;11 cells, with an IC50 value of 34 nM across a concentration range of 0-1000 nM. Furthermore, the CDK9-IN-14 biological activity has been validated in animal models to assess its therapeutic potential. In CDK9-IN-14 In Vivo studies, female Nu/Nu mice (6-8 weeks old, 18-22 g) injected with HL-60 cells were administered the compound at a dosage of 5 mg/kg via oral administration (p.o.) once daily (qd) for 9 days. The results indicated a significant anti-tumor effect, achieving a tumor growth inhibition (TGI) value of 58%. In conclusion, CDK9-IN-14 is a potent and selective CDK9 inhibitor that holds promise for the treatment of CDK9-dependent cancer.
Keywords
CDK9-IN-14, 2650640-17-6, CDK, Cyclin dependent kinase, CDK9, Cancer, HL-60 cells, MV4;11 cells, Cell proliferation, Inhibitor, inhibitor, inhibit
References
[1] WANG Zhenyu. Compound as cyclin-dependent kinase 9 inhibitor and use thereof. WO2021115335A1