Signaling Pathway

Antifolate

Antifolate

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Antifolates are compounds that antagonise the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis. 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. The majority of antifolates work by inhibiting dihydrofolate reductase (DHFR). Many are primarily DHFR inhibitors, but raltitrexed is an inhibitor of thymidylate synthase, and pemetrexed inhibits both and a third enzyme. Antifolates act specifically during DNA and RNA synthesis, and thus are cytotoxic during the S-phase of the cell cycle. Thus, they have a greater toxic effect on rapidly dividing cells.

Antifolate Inhibitors & Modulators (16)

Product Name Catalog No. Brief Description
Calcium N5-methyltetrahydrofolate

HY-17557

Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt of levomefolic acid, which  has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers.

Cycloguanil D6

HY-12784S

Cycloguanil D6 is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.

Cycloguanil D6 Nitrate

HY-12784S1

Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.

Folinic acid

HY-17556

Folinic acid is an adjuvant used in cancer chemotherapy involving the drug methotrexate.

Folinic acid Calcium

HY-13664

Leucovorin Calcium is a reduced folic acid.

Folinic acid calcium salt pentahydrate

HY-B0080

Folinic Acid is a reduced folic acid, which is used in combination with other chemotherapy drugs.

Levoleucovorin Calcium

HY-13667

Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.

Levomefolate calcium

HY-17383

Levomefolate is an artificial form of folate.

Levomefolic acid

HY-14781

Levomefolic acid (5-MTHF) is the natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions.

Methotrexate

HY-14519

Methotrexate(WR19039; CL14377) can interfere with the growth of certain cells of the body, especially cells that reproduce quickly, such as cancer cells, bone marrow cells, and skin cells.

Pemetrexed

HY-10820

Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

Pemetrexed disodium

HY-10820A

Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

Pemetrexed disodium hemipenta hydrate) 1:2:2.5

HY-13781

Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

Pralatrexate

HY-10446

Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog.

Pyrimethamine

HY-18062

Pyrimethamine(RP4753) is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR).

Trimethoprim

HY-B0510

Trimethoprim is a bacteriostatic antibiotic used mainly in the prophylaxis and treatment of urinary tract infections.