IMPDH2 Inhibitor

VX-148 is an orally active immunosuppressant, which is a non-competitive inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor with K_i values for IMPDH Ⅱ and IMPDH Ⅰ of 6 and 14 nM respectively. VX-148 can significantly inhibit the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated by T-cell mitogen (PHA) or B-cell mitogen (SPAS). VX-148 has high selectivity for lymphocytes (such as L1210, Jurkat T cells, and Raji B cells), but has no significant toxicity to non-lymphoid cells. VX-148 can inhibit antibody responses in mouse models and significantly prolong the survival time of transplanted skin in allogeneic skin transplantation models. VX-148 can be used in the research of autoimmune diseases (such as rheumatoid arthritis, psoriasis) and organ transplantation anti-rejection.

IMPDH II/HDAC1-IN-1 (Compound C12) is an orally active, selective dual IMPDH II/HDAC1 inhibitor, with an IC₅₀ of 84.69 nM against hIMPDH II and an IC₅₀ of 81.75 nM against HDAC1. IMPDH II/HDAC1-IN-1 inhibits the proliferation of chronic myeloid leukemia cells. IMPDH II/HDAC1-IN-1 can be used for the research of chronic myeloid leukemia.

β-Benzamide adenine dinucleotide is a biologically active metabolite of benzamide riboside. β-Benzamide adenine dinucleotide is a competitive inhibitor of human NAD kinase with a K_i value of 90 μM, and inhibits human IMPDH with IC₅₀ values of 0.787 μM and 0.884 μM for type I and type II, respectively. β-Benzamide adenine dinucleotide exhibits inhibitory activities against lactate dehydrogenase, glutamate dehydrogenase, and malate dehydrogenase. β-Benzamide adenine dinucleotide can be used for the study of chronic myelogenous leukemia.