T6173

BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.

Tyrosine kinase-IN-4 (EXAMPLE 107) is a protein tyrosine kinase inhibitor [1].

PPARγ agonist 4 (Compound 18b), a potent and selective PPARγ agonist, demonstrates antitumor efficacy only when used in conjunction with Imatinib and does not exhibit cytotoxic effects on either non-resistant or resistant cells [1].

EGFR/HER2-IN-6 (compound 43) is a dual EGFR/HER2 and DHFR inhibitor with potent activity against EGFR kinase, HER2 kinase, and DHFR, characterized by IC50 values of 0.122 μM, 0.078 μM, and 0.585 μM, respectively. This compound displays notable anticancer properties in various cancer cell lines, while demonstrating a favorable safety profile and selectivity indices. Consequently, EGFR/HER2-IN-6 holds promise as a valuable tool in cancer research [1].

HPK1-IN-25 (example 94), an inhibitor of hematopoietic progenitor kinase 1 (HPK1), demonstrates enzymatic activity with an IC50 value of 129 nM, indicating its potential utility in cancer research [1].

IRAK4-IN-9 (compound 73) is a highly potent IRAK4 inhibitor with an IC50 value of 1.5 nM, effectively blocking MyD88-dependent signaling and showing significant potential for researching inflammatory diseases, autoimmune diseases, and cancer [1].

MI-1 inhibits Menin-MLL interaction with an IC₅₀ of 1.9 μM [1].

CB1/2 agonist 3 is a competitive and potent CB1/CB2 agonist with high affinity for hCB1 and hCB2 and can be used to study neurological disorders.

FtsZ-IN-4, an orally active inhibitor of FtsZ (filamenting temperature-sensitive mutant Z), demonstrates remarkable antibacterial activity and favorable pharmaceutical properties. With low cytotoxicity (CC 50 >20 μg/mL) [1], FtsZ-IN-4 exhibits promising potential for therapeutic applications.

CDK4/6-IN-7, a highly potent and selective orally active inhibitor of CDK4/6, demonstrates impressive inhibition activity with IC50 values of 1.58 nM and 4.09 nM respectively. This compound is particularly valuable for breast cancer research [1].

Dyrk1A-IN-5 (compound 5j) is a highly potent and selective DYRK1A inhibitor with an IC50 of 6 nM, reducing the phosphorylation of Thr434 in SF3B1 dose-dependently (IC50 = 0.5 μM) and inhibiting tau phosphorylation at Thr212 (IC50 = 2.1 μM), making it valuable for Down syndrome research [1].