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 (133):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-17383R
    Levomefolate calcium (Standard)
    		Chemical
    Levomefolate (calcium) (Standard) is the analytical standard of Levomefolate (calcium). This product is intended for research and analytical applications. Levomefolate (calcium) is an orally active, BBB-penetrable and active form of folic acid. Levomefolate (calcium) can be used as a food supplement for folic acid and in the research of neural tube defect diseases.
    Levomefolate calcium (Standard)
  • HY-114306
    EC0489
    		Chemical
    EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor. Small molecule-agent conjugate (SMDC).
    EC0489
  • HY-14519D
    Methotrexate monohydrate
    Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
    Methotrexate monohydrate
  • HY-121151
    (±)-Methotrexate
    (±)-Methotrexate ((±)-Amethopterin) is a racemate of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of Folic acid into Tetrahydrofolate, and inhibiting DNA synthesis.
    (±)-Methotrexate
  • HY-128939
    EC0488
    EC0488 is used to synthesize EC0531 with folate receptor (FR)-specific and anti-tumor activities.
    EC0488
  • HY-P10740
    CBP-1018
    CBP-1018 is a PDC (peptide drug conjugate) consisting of a dual targeting FRα/prostate-specific membrane antigen (PSMA) ligand (blue part) coupled to Monomethyl auristatin E (HY-15162) (red part) via a linker (HY-78738) (black part). CBP-1018 is expected to be used in breast cancer research.
    CBP-1018
  • HY-P990935
    Opugotamig
    HY-P990935 is an FOLR1-targeting half-IG G1 -κ/(scFv -κ-heavy) -h-CH2-CH3 type chimeric antibody.
    Opugotamig
  • 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-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 (HY-14519) as a rescue agent to decrease Methotrexate-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