1. Metabolic Enzyme/Protease
  2. Lactate Dehydrogenase
  3. MEDS433

MEDS433 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 1.2 nM. MEDS433 exerts a potent antiviral activity against RSV-A and RSV-B in the one-digit nanomolar range. MEDS433 induces the expression of antiviral proteins encoded by interferon stimulated genes (ISGs) able to reduce RSV replication.

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MEDS433 Chemical Structure

MEDS433 Chemical Structure

CAS No. : 2241027-61-0

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Description

MEDS433 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 1.2 nM. MEDS433 exerts a potent antiviral activity against RSV-A and RSV-B in the one-digit nanomolar range. MEDS433 induces the expression of antiviral proteins encoded by interferon stimulated genes (ISGs) able to reduce RSV replication[1].

Cellular Effect
Cell Line Type Value Description References
Jurkat IC50
0.75 μM
Compound: 4
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
[PMID: 29939742]
Jurkat IC50
68.69 μM
Compound: 4
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
[PMID: 29939742]
PBMC IC50
0.78 μM
Compound: 4
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by Hoechst 33258 dye-based fluorescence assay
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by Hoechst 33258 dye-based fluorescence assay
[PMID: 29939742]
PBMC IC50
57.15 μM
Compound: 4
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
[PMID: 29939742]
THP-1 EC50
0.0397 μM
Compound: 1
Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis
Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis
[PMID: 33844533]
THP-1 EC50
0.0723 μM
Compound: 1
Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry
Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry
[PMID: 33844533]
THP-1 EC50
40 nM
Compound: MEDS433
Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis
Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis
[PMID: 36162075]
THP-1 EC50
72 nM
Compound: MEDS433
Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
[PMID: 36162075]
U-937 EC50
0.026 μM
Compound: 1
Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis
Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis
[PMID: 33844533]
U-937 EC50
0.0404 μM
Compound: 1
Induction of apoptosis in human U-937 cells after 3 days by Annexin-V-FITC staining based flow cytometry
Induction of apoptosis in human U-937 cells after 3 days by Annexin-V-FITC staining based flow cytometry
[PMID: 33844533]
U-937 EC50
26 nM
Compound: MEDS433
Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis
Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis
[PMID: 36162075]
U-937 EC50
40 nM
Compound: MEDS433
Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
[PMID: 36162075]
Molecular Weight

401.31

Formula

C20H11F4N3O2

CAS No.
SMILES

O=C(C1=C2C=CC=CN2N=C1O)NC3=C(F)C(F)=C(C4=CC=CC=C4)C(F)=C3F

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
MEDS433
Cat. No.:
HY-156442
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