IMPDH
Inosine-5’-monophosphate dehydrogenase
IMPDH is a purine biosynthetic enzyme that catalyzes the conversion of inosine 5'-monophosphate (IMP) to xanthosine 5'-monophosphate (XMP). This is the rate-limiting step in the de novo biosynthesis of guanine nucleotides (GMP), and the reaction requires the coenzyme nicotinamide adenine dinucleotide (NAD+). There are mainly two subtypes of IMPDH, IMPDH1 and IMPDH2. IMPDH is a regulator of the intracellular guanine nucleotide pool, and is therefore important for DNA and RNA synthesis, signal transduction, energy transfer, glycoprotein synthesis, as well as other process that are involved in cellular proliferation. In addition, IMPDH can regulate the activation and proliferation of lymphocytes and affect the immune response. The abnormal expression of IMPDH is closely related to cancer and autoimmune diseases[1][2].
References:
- [1]. Juvale K, et al. Inhibitors of inosine 5'-monophosphate dehydrogenase as emerging new generation antimicrobial agents. Medchemcomm. 2019 May 2;10(8):1290-1301.
- [2]. Cuny GD, et al. Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitors: a patent and scientific literature review (2002-2016). Expert Opin Ther Pat. 2017 Jun;27(6):677-690. [Content Brief]
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IMPDH Related Products (12)
Related Products (12)
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(R)-Merimepodib
0 ImagesSynonyms: (R)-VX-497; (R)-MMPD(R)-Merimepodib is the isomer of Merimepodib (HY-13986), and can be used as an experimental control. Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.
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BMS-566419
0 ImagesBMS-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.
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IMPDH-IN-4
0 ImagesIMPDH-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.
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Mizoribine 5'-monophosphate
0 ImagesCat. No.: HY-W743767CAS No.: 62025-48-3Synonyms: MZR-PMizoribine 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 Ki 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.
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VX-148
0 ImagesCat. No.: HY-118917CAS No.: 297730-05-3VX-148 is an orally active immunosuppressant, which is a non-competitive inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor with Ki 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.
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IMPDH II/HDAC1-IN-1
0 ImagesCat. No.: HY-174221IMPDH 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.
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β-Benzamide adenine dinucleotide
0 ImagesCat. No.: HY-147342CAS No.: 156724-91-3β-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 Ki 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.
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IMPDH-IN-3
0 ImagesCat. No.: HY-128214CAS No.: 401822-29-5
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BMS-337197
0 ImagesCat. No.: HY-117124CAS No.: 267645-83-0BMS-337197 is an inosine monophosphate dehydrogenase (IMPDH) inhibitor.
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