Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations. Additionally, Rezivertinib demonstrates excellent central nervous system (CNS) penetration and exhibits antitumor activity[1][2].
Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK), which can penetrate the central nervous system (CNS). It exhibits a high affinity for ROCK2 with an inhibition constant (IC50) of 3 nM. This compound is of potential interest for further investigations in the field of Huntington's disease research [1].
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist with an EC 50 of 0.18 μM. It exhibits selectivity for α4β2 receptors over α2β4, α4β4, and α3β4 receptors, with EC 50 s ranging from 10 to 30 μM. TC-2559 difumarate also demonstrates antinociceptive effects.
ASP3662, also known as SPI-62, is a potent, selective and CNS-penetrable inhibitor of 11β-HSD1. The effects of ASP3662 suggest that selective inhibition of 11β-HSD1 may be an attractive approach for the treatment of neuropathic and dysfunctional pain, as observed in fibromyalgia. ASP3662 inhibited human, mouse and rat 11β-HSD1 but not human 11β-HSD2, in vitro. ASP3662 inhibited in vitro conversion of glucocorticoid from its inactive to active form in extracts of rat brain and spinal cord.
DLK-IN-1 is a selective oral active inhibitor of bisleucine zipper kinase (DLK, MAP3K12) with Ki of 3 nM. DLK-IN-1 is active in the Alzheimer's disease model, retains excellent CNS permeability, and after multiple days of administration, its concentration
3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50 = 13.4 µM). It is also active against L. donovani amastigotes when used at a concentration of 50 µM.