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Cell Cycle/Checkpoint

Nucleoside Antimetabolite/Analog

Poly(ADP-ribose) Glycohydrolase (PARG)

Serine/threonin kinase

DNA Damage/DNA Repair

DNA Alkylator/Crosslinker

Nucleoside Antimetabolite/Analog

Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(43)

Glyoxalase

(2)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(36)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(103)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(48)

Stearoyl-CoA Desaturase (SCD)

DHFR

Dihydrofolate reductase, or DHFR, is an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, using NADPH as electron donor, which can be converted to the kinds of tetrahydrofolate cofactors used in 1-carbon transfer chemistry. In humans, the DHFR enzyme is encoded by the DHFR gene. It is found in the q11→q22 region of chromosome 5.[7] Bacterial species possess distinct DHFR enzymes (based on their pattern of binding diaminoheterocyclic molecules), but mammalian DHFRs are highly similar.

Filter HomeSignaling PathwaysDNA Damage/DNA Repair-Cell Cycle/Checkpoint-MetabolismDHFR

Gentamicin sulfate

T13261405-41-0

Gentamicin sulfate (SCH9724) is a wide-spectrum, aminoglycoside antibiotic used to inhibit protein synthesis in sensitive organisms.

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Piritrexim

T2464472732-56-0In house

Piritrexim (BW 301U) is an orally available fat-soluble dihydrofolate reductase inhibitor with pulmonary toxicity used in the study of uroepithelial carcinoma and metastatic breast cancer.

$350

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Methotrexate Diglutamate

T2588641600-13-9In house

Methotrexate Diglutamate Small molecule compound present in the liver that acts as a partially purified human dihydrofolate reductase inhibitor.

$1,630

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DS18561882

T111032227149-22-4In house

DS18561882 is an orally available, selective and potent inhibitor of methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) with antitumor activity, inhibits MTHFD1 activity and can be used in the study of breast cancer.

$117

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Pemetrexed

T0189137281-23-3

Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).

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Pralatrexate

T6120146464-95-1

Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

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Epiroprim

T2538173090-70-7

Epiroprim (Ro11-8958) is a selective dihydrofolate reductase (DHFR) inhibitor with antibacterial activity, inhibiting Staphylococcus, Enterococcus, Pneumococcus, and Streptococcus.

$293

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Pemetrexed disodium

T0189L150399-23-8

Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.

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Lometrexol

T15826106400-81-1In house

Lometrexol (LY 264618), an antipurine Antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and Apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1 2 (hSHMT1 2) inhibitor.

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Trimethoprim

T1153738-70-5

Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor, and Cytochrome P450 2C8 Inhibitor, and Organic Cation Transporter 2 Inhibitor.

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Talotrexin ammonium

T64295648420-92-2In house

Talotrexin ammonium is a non-polyglutamic acid antifolate. Talotrexin ammonium inhibits tumor growth by targeting dihydrofolate reductase (DHFR), thereby improving anti-tumor activity in a wide range of cancer models, helping to inhibit tumor growth.

$350

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LY 345899

T1582710538-99-5

LY 345899 is a folate analog that inhibits methylenetetrahydrofolate dehydrogenase and MTHFD2, with IC50 values of 96 nM and 663 nM, respectively, and a Ki of 18 nM for MTHFD1.

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Pemetrexed disodium hemipenta hydrate

T6226357166-30-4

Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Disodium Hydrate for TS, DHFR and GARFT is 1.3 nM, 7.2 nM and 65 nM, respectively.

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Pyrimethamine

T084958-14-0

Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.

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P 218

T73328L1142407-60-0In house

P 218 is a novel DHFR inhibitor with antimalarial activity and antifolate effects and can be used to study Buruli ulcer.

$129

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DS44960156

T376552361327-08-2

DS44960156 is a novel selective inhibitor of methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) that inhibits both MTHFD2 and MTHFD1 and can be used in cancer research.

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WR99210

T1725747326-86-3

WR99210 (BRL 6231 free base) is an orally available dihydrofolate reductase (DHFR) inhibitor with antiparasitic activity, often used in combination with dapsone to study Mycobacterium avium complex (MAC).

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Trioxsalen

T45583902-71-4

Trioxsalen (Trioxysalen) is a furanocoumarin and a psoralen derivative, in conjunction with UV-A for phototherapy treatment of vitiligo and hand eczema. After photoactivation it creates interstrand cross-links in DNA, which can cause programmed cell death.

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Fanotaprim

T366922120282-75-7

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor, suppressing the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM, a hDHFR IC50 of 308 ± 71 nM, and a hDHFR to TgDHFR selectivity ratio of 196.

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Brodimoprim

T1985856518-41-3

Brodimoprim is an inhibitor of dihydrofolate reductase(DHFR). Brodimoprim is also a long-acting broad-spectrum antibacterial agent characterized by a good pharmacokinetic profile.

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Sulfadoxine

T08362447-57-6

Sulfadoxine (Sulphadoxine) is a broad-spectrum sulfanilamide and a synthetic analog of para-aminobenzoic acid (PABA) with bacteriostatic and antimalarial properties.

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Urea

T073857-13-6

Urea (Carbonyldiamide) is formed in the liver from ammonia produced by the deamination of amino acids. It is the principal end metabolite of protein catabolism and accounts for about one-half of the total urinary solids.

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Sulfameter

T0748651-06-9

Sulfameter (Sulfametoxydiazine) is a long-acting sulfonamide antibacterial agent used to treat urinary tract infections and leprosy.

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Diaveridine

T22045355-16-8

Diaveridine (AI3-23935) (DVD) is a popular antibacterial synergist that is widely used in combination with sulfonamide. It has been reported to be genotoxic to mammalian cells, but more studies are required to clarify this.

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