2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Antifolate

Antifolate

Antifolate

Related Products

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Antifolates agents work by antagonizing (blocking) the actions of folic acid (vitamin B9). Antifolates act specifically during DNA and RNA synthesis, exerting a cytotoxic effect during the S- phase of the cell cycle. Antifolates targeting folate metabolism played a pivotal role in drug treatment of malignant, microbial, parasitic and chronic inflammatory diseases.

Folate (folic acid) cofactors are essential for the synthesis and metabolism of amino acids, consequently antifolates inhibit cell division, DNA/RNA synthesis and repair and protein synthesis. Some such as Proguanil, Pyrimethamine and Trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi. Major antifolate enzyme targets and exemplary antifolates that target these enzymes include: dihydrofolate reductase (DHFR), thymidylate synthase (TS), GARFTase and AICARFTase.

Antifolate Related Products (130):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-108251S
    Methotrexate metabolite-d3
    Methotrexate metabolite-d3 is the deuterium labeled Methotrexate metabolite. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent.
    Methotrexate metabolite-d<sub>3</sub>
  • HY-14523
    LY 254155
    LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
    LY 254155
  • HY-B0806S1
    Proguanil-d4
    Proguanil-d4 is the deuterium labeled Proguanil. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil-d<sub>4</sub>
  • HY-14518A
    Aminopterin sodium
    		Antagonist
    Aminopterin sodium (4-Aminofolic acid sodium) is an anti-tumor drug with immunosuppressive activity. Aminopterin sodium blocks the metabolism of folic acid by inhibiting the activity of dihydrofolate reductase, thereby affecting nucleic acid synthesis. Aminopterin sodium is mainly used to inhibit acute lymphoblastic leukemia and certain other types of cancer. Aminopterin sodium is also used clinically as an immunosuppressant to suppress autoimmune diseases.
    Aminopterin sodium
  • HY-14519CS
    (R)-Methotrexate-d3
    (R)-Methotrexate-d3 is the deuterium labeled (R)-Methotrexate.
    (R)-Methotrexate-d<sub>3</sub>
  • HY-149200
    Lysine-methotrexate
    Lysine-methotrexate, an analogue of Methotrexate (HY-14519), is a dihydrofolate reductase (DHFR) inhibitor.
    Lysine-methotrexate
  • HY-13714
    Nolatrexed
    Nolatrexed (AG 337 free base) is a compound with antifolate activity, high oral bioavailability, and major toxicity at inhibitory doses is gastrointestinal reactions. It can be safely taken orally at specific doses for inhibition, with effects on platelets and neutrophils.
    Nolatrexed
  • HY-10820S
    Pemetrexed-d5
    Pemetrexed-d5 is the deuterium labeled Pemetrexed. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
    Pemetrexed-d<sub>5</sub>
  • HY-117058
    LY243246
    LY243246 ((6S)-DDATHF), the 6S diastereomer of DDATHF, is a potent competitive inhibitor of 5’-phosphoribosylglycinamide formyltransferase (GAR transformylase). 6R- and 6S-diastereomers of DDATHF are remarkably similar and equiactive antimetabolites inhibitory to de novo purine synthesis.
    LY243246
  • HY-157217
    Antitumor agent-99
    		Inhibitor
    Antitumor agent-99 (compound 7) is an anticancer agent targeting FRα/β and PCFT. Antitumor agent-99 inhibits R2/PCFT4 (PCFT), RT16(FRα), and D4(FRβ) cells with IC50s of 51.46 nM, 2.53 nM, and 2.98 nM, respectively.
    Antitumor agent-99
  • HY-17556B
    Folinic acid calcium hydrate
    		Chemical
    Folinic acid (Leucovorin) calcium hydrate is a biological folic acid and is generally administered along with Methotrexate (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity.
    Folinic acid calcium hydrate
  • HY-17383S
    Levomefolate-13C5 calcium
    		Chemical
    Levomefolate-13C5 (calcium) is the 13C-labeled Levomefolate (calcium). Levomefolate calcium is an artificial form of folate.
    Levomefolate-<sup>13</sup>C<sub>5</sub> calcium
  • HY-10820BR
    Pemetrexed disodium heptahydrate (Standard)
    		Inhibitor
    Pemetrexed (disodium heptahydrate) (Standard) is the analytical standard of Pemetrexed (disodium heptahydrate). This product is intended for research and analytical applications. Pemetrexed disodium heptahydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
    Pemetrexed disodium heptahydrate (Standard)
  • HY-147661
    DHFR-IN-2
    		Inhibitor
    DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research.
    DHFR-IN-2
  • HY-108251R
    Methotrexate metabolite (Standard)
    Methotrexate metabolite (Standard) is the analytical standard of Methotrexate metabolite. This product is intended for research and analytical applications. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent.
    Methotrexate metabolite (Standard)
  • HY-P990417
    Anti-FOLR1/FRA Antibody
    Anti-FOLR1/FRA Antibody is a humanized antibody expressed in CHO cells, targeting FOLR1/FRA. The Anti-FOLR1/FRA Antibody contains a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 146.46 kDa. The isotype control for the Anti-FOLR1/FRA Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-FOLR1/FRA Antibody
  • HY-17556A
    Folinic acid disodium
    		Chemical
    Folinic acid (Leucovorin) disodium is a biological folic acid and is a forms of vitamin B9. Folinic acid disodium is generally administered along with Methotrexate (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity. Folinic acid disodium and Sfluorouracil adjuvant chemotherapy shows effective in colon carcinoma.
    Folinic acid disodium
  • HY-B0510A
    Trimethoprim sulfate
    Trimethoprim sulfate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim sulfate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim sulfate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim sulfate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc.
    Trimethoprim sulfate
  • HY-10373B
    Trimetrexate isethionate
    Trimetrexate (CI-898) isethionate is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
    Trimetrexate isethionate
  • HY-137267
    10-Methyl-10-deazaaminopterin
    10-Methyl-10-deazaaminopterin is a folate analog and an antifolate. 10-Methyl-10-deazaaminopterin can be used for the research of cancer.
    10-Methyl-10-deazaaminopterin