diaminopyrimidine

Kopexil is a compound similar to minoxidil that promotes hair growth and treats hair loss by inhibiting 5α-reductase and possibly activating potassium channel switches, which improve hair follicles by prolonging the anagen phase of the hair growth cycle and improving.

Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.

Aumitin, a diaminopyrimidine-based autophagy inhibitor, dose-dependently inhibits starvation- and rapamycin-induced autophagy with IC50s of 0.12 μM and 0.24 μM, respectively [1], and also inhibits mitochondrial respiration by targeting complex I.

DHFR-IN-22 (Compound 8) is a DHFR (Dihydrofolate Reductase) inhibitor that falls under the category of 2,4-diaminopyrimidine compounds. It demonstrates significant inhibitory activity against isolated DHFR enzyme and major nontuberculous mycobacteria (NTM) species, specifically Mycobacterium avium and Mycobacterium abscessus. The compound has an IC50 of 1.1 nM and a MIC of 1.5 μg mL for M. abscessus, and an IC50 of 6.3 nM and a MIC of 0.1 μg mL for M. avium, while its IC50 for human DHFR is 2100 nM. DHFR-IN-22 may be promising for developing new strategies to combat NTM infections.

KRCA-0008 is an effective and specific ALK Ack1 inhibitor (IC50: 12 4 nM); displays drug-like properties without hERG liability.

DAP-81 is a diaminopyrimidine derivative that targets PLKs, destabilizing kinetochore microtubules. Other spindle tubules are stabilized, resulting in monopolar mitotic spindles. In vitro, DAP-81 inhibits Plk1 at an IC50 of 0.9 nM. DAP-81 is currently in ongoing preclinical evaluations.

CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK (anaplastic lymphoma kinase) inhibitor with an IC50 value of 1.9 nM against recombinant ALK kinase activity. It shows antitumor efficacy in ALK-positive human cancer models and has favorable pharmacodynamic and pharmacokinetic profiles.

CEP-28122 mesylate hydrochloride, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor with an IC50 of 1.9 nM, exhibiting antitumor and good pharmacokinetic activity [1].

Trimethoprim pentanoic acid is a hapten that exhibits an IC50 of 0.15 ng mL when its diaminopyrimidine moiety is exposed to the immune system [1].