IMPDH Inhibitor

BMS-566419 is an orally active IMPDH inhibitor with an IC₅₀ of 91 nM against human IMPDH I and 68 nM against human IMPDH II. BMS-566419 exerts anti-heart transplant rejection and anti-renal fibrosis effects, and inhibits the expression of MCP-1, TGF-β1 as well as antibody production. BMS-566419 can be used in research on renal fibrosis and organ transplantation.

IMPDH-IN-2 (compound 2) is an inhibitor of inosine monophosphate dehydrogenase (IMPDH) with IC₅₀IMPDH I and IMPDH II >Values are 0.15 and 0.17 μM, respectively. IMPDH-IN-2 has antitumor activity.

IMPDH-IN-4 is a derivative of N-pyridinylthiophene carboxamid that exhibits activity against peripheral nerve sheath carcinoma cells. IMPDH-IN-4 is metabolized by NAMPT and NMNAT1 to an adenine dinucleotide (AD) derivative, which is an NAD analog and can inhibit inosine monophosphate dehydrogenase (IMPDH), leading to the accumulation of inosine monophosphate (IMP) in cells. IMPDH-IN-4 has good blood-brain barrier permeability and can be used in the study of central and peripheral nervous system cancers.

IMPDH2-IN-4 (Compound 2d) is a selective IMPDH2 inhibitor with a K_i,app value of 1.8 μM. IMPDH2-IN-4 exhibits anti-cancer activity against osteosarcoma. IMPDH2-IN-4 can be used in research related to osteosarcoma.

Mizoribine 5'-monophosphate (MZR-P) is the active metabolite of Mizoribine (HY-17470). Mizoribine 5'-monophosphate is an inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH), and its K_i values for IMPDH of Trypanosoma brucei, Bacillus subtilis and Oceanobacillus iheyensis are 3.3, 72 and 157 nM respectively. Mizoribine 5'-monophosphate can be used in anti-trypanosomiasis and immunosuppression research.

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.

IMPDH-IN-3 (Compound C67) is an inhibitor of C. parvum IMPDH (CpIMPDH) with an IC₅₀ of 35 nM. IMPDH-IN-3 can be used in the research of anti-Cryptosporidium drugs.

N-(2,5-Dimethoxyphenyl)-3-hydroxy-2-naphthamide is a IMPDH inhibitor with a K_i ranging from 10 μM to 20 μM. N-(2,5-Dimethoxyphenyl)-3-hydroxy-2-naphthamide can be used in studies of HBV and HCV infection.

BMS-337197 is an inosine monophosphate dehydrogenase (IMPDH) inhibitor.