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-10373A
    Trimetrexate trihydrochloride
    Trimetrexate (CI-898) trihydrochloride 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 trihydrochloride can also inhibit the growth of various cancer cells. Trimetrexate trihydrochloride can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
    Trimetrexate trihydrochloride
  • HY-10824B
    Talotrexin ammonium
    Talotrexin ammonium is a nonpolyglutamatable antifolate. Talotrexin ammonium improves antitumor activity in a broad spectrum of cancer models by targeting DHFR to inhibit tumor growth.
    Talotrexin ammonium
  • HY-14522
    LY 222306
    LY 222306 is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor with a Ki of 0.77 nM.
    LY 222306
  • HY-121207
    Denopterin
    		Inhibitor
    Denopterin is a dihydrofolate reductase (DHFR) inhibitor and an antifolate agent. Denopterin is an antimetabolite that has toxic effects on cells and can be used for cancer.
    Denopterin
  • HY-121927
    Mobiletrex
    Mobiletrex is an anti folate and dihydrofolate reductase inhibitor that can be used in research on rheumatoid arthritis.
    Mobiletrex
  • HY-17557R
    Calcium N5-methyltetrahydrofolate (Standard)
    		Chemical
    Calcium N5-methyltetrahydrofolate (Standard) is the analytical standard of Calcium N5-methyltetrahydrofolate. This product is intended for research and analytical applications. 0
    Calcium N5-methyltetrahydrofolate (Standard)
  • HY-19095
    TNP-351
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
    TNP-351
  • HY-B0806AR
    Proguanil hydrochloride (Standard)
    Proguanil (hydrochloride) (Standard) is the analytical standard of Proguanil (hydrochloride). This product is intended for research and analytical applications. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil hydrochloride (Standard)
  • HY-121256
    Chlorasquin
    		Chemical
    Chlorasquin inhibits thymidylate synthetase with an approximate Ki value of 4.9 μM. Chlorasquin is also a folate antagonist, testing the Methotrexate (HY-14519) effect. Chlorasquin binds tighter to dihydrofolate reductase at alkaline pH than does Methotrexate, which is promising for research of antipsoriatic agents.
    Chlorasquin
  • HY-162975
    NVP-EVS459 (175Lu)
    		Chemical
    NVP-EVS459 (175Lu) is a folate receptor targeting radio-conjugate, and can be used for cancer research.
    NVP-EVS459 (175Lu)
  • HY-124350R
    10-Formylfolic acid (Standard)
    		Inhibitor
    10-Formylfolic acid (Standard) is the analytical standard of 10-Formylfolic acid. This product is intended for research and analytical applications. 10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.
    10-Formylfolic acid (Standard)
  • HY-10820AS
    Pemetrexed-d5 disodium
    Pemetrexed-d5 disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium 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> disodium
  • HY-10819
    AG2034
    AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 28 nM against human GARFT, and it binds with high affinity to the folate receptor (Kd of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a Km of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED.
    AG2034
  • HY-147699
    FRα-IN-1
    		Chemical
    FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells.
    FRα-IN-1
  • HY-P99225A
    Mirvetuximab (powder)
    Mirvetuximab (M9346A) (powder) is an anti-FOLR1 (folate receptor 1) monoclonal antibody. Mirvetuximab (powder) is the antibody moiety of folate receptor alpha (FRα)-targeting ADC (Mirvetuximab soravtansine). Mirvetuximab soravtansine can be used in ovarian and other FRα-positive cancer research.
    Mirvetuximab (powder)
  • HY-10823
    OSI-7904L
    OSI-7904L (GW1843) is a noncompetitive inhibitor of thymidylate synthase (TS). OSI-7904L is an antifolate compound and a substrate for folylpolyglutamate synthetase. OSI-7904L has cytotoxicity against solid tumor lines, and the toxicity can be selectively blocked by folic acid.
    OSI-7904L
  • HY-12784S1
    Cycloguanil-d6 nitrate
    Cycloguanil-d6 (nitrate) is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
    Cycloguanil-d<sub>6</sub> nitrate
  • HY-B0510CR
    Trimethoprim lactate (Standard)
    Actein (Standard) is the analytical standard of Actein. This product is intended for research and analytical applications. Actein, a triterpene glycoside, shows an inhibitory effect on cancer cells, which is isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in bladder cancer. Actein has little toxicity in vivo.
    Trimethoprim lactate (Standard)
  • HY-10824A
    Talotrexin monoammonium
    Talotrexin monoammonium is the monoammonium salt form of Talotrexin (HY-10824). Talotrexin monoammonium is an analog of Aminopterin (HY-14518), and is a nonpolyglutamatable classic antifolate. Talotrexin monoammonium is a reduced folate carrier (RFC) specific inhibitor and selectively inhibits RFC transport. Talotrexin monoammonium shows antitumor activity by targeting DHFR to inhibit tumor growth.
    Talotrexin monoammonium
  • HY-P991164
    Torvutatug
    		Inhibitor
    Torvutatug is an anti-FOLR1 human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Torvutatug