Antifolate
<div class="colum_1 clearer"><p>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.</p></div>
Targets for Antifolate
Products for Antifolate
- Cat.No. Product Name Information
- GC42789 Aminopterin Aminopterin is a synthetic folic acid derivative whose metabolite is a competitive inhibitor of dihydrofolate reductase, which is a cofactor for nucleic acid synthesis.
- GC15306 Calcium N5-methyltetrahydrofolate Calcium salt of levomefolic acid
- GC34309 Cycloguanil D6 (Chlorguanide triazine D6)
- GC35781 Cycloguanil D6 Nitrate Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
- GC65617 DHFR-IN-3 DHFR-IN-3 is a dihydrofolate reductase (DHFR) inhibitor with the IC50 values of 19 μM and 12 μM in rat liver and P. carinii DHFR, respectively.
- GC32343 Diaveridine (EGIS-5645) Diaveridine (EGIS-5645) (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
- GC19495 DL-Folinic Acid (calcium salt) DL-Folinic Acid (calcium salt) (Leucovorin calcium) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.
- GC32401 EC0489 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-drug conjugate (SMDC).
- GC62968 Fanotaprim Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively.
- GC14331 Folinic acid NULL
- GC16203 Leucovorin Calcium Leucovorin Calcium (Leucovorin calcium salt pentahydrate) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.
- GC16680 Levoleucovorin Calcium Levoleucovorin Calcium (Calcium levofolinate), a levo isoform of Leucovorin Calcium, possesses antineoplastic effects. Levoleucovorin Calcium is also an augmentor of 5-fluorouracil cytotoxicity against cancer.
- GC11558 Levomefolate calcium A biologically active form of folic acid
- GC18404 Lometrexol Glycinamide ribonucleotide formyltransferase (GART) is a folate-dependent enzyme required for de novo purine synthesis.
- GC66387 Lometrexol disodium Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
- GC39820 Lometrexol hydrate A GART inhibitor
- GC36486 LSN 3213128 LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
- GC33322 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.
- GC33373 LY309887 LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
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GC10405
Methotrexate
Methotrexate, a folate antagonist, is a potent anti-inflammatory agent when used weekly in low concentrations, the anti-phlogistic action of which is due to increased adenosine release at inflamed sites.
- GC61047 Methotrexate disodium Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
- GC36589 Methotrexate metabolite Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate.
- GC61058 Metoprine Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor.
- GC11610 Pemetrexed An antifolate with anticancer activity
- GC17694 Pemetrexed disodium hemipenta hydrate
- GC12919 Pralatrexate A dihydrofolate reductase inhibitor
- GC17867 Pyrimethamine A dihydrofolate reductase inhibitor
- GC63612 Tetroxoprim Tetroxoprim is an antimicrobial DHFR inhibitor.
- GC10137 Trimethoprim bacteriostatic antibiotic
- GC66422 Trimethoprim-d9 Trimethoprim-d9 is the deuterium labeled Trimethoprim. Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment.
- GC37938 WR99210 WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM).