>98%,Standard References

A novel antifolate modulator compound..

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.

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

Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.

Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent.

Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

Trimethoprim lactic is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim lactic is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim lactic has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment.

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.

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

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. Fanotaprim has the potential for the research of toxoplasmosis.

Tetroxoprim is an antimicrobial DHFR inhibitor.

TH9028 (TH-9028) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 11 nM.TH9028demonstrated efficacy on HL-60 cell viability with EC50 of 11 nM.TH9028 potently inhibits related MTHFD proteins MTHFD2L and MTHFD1-(DC) with IC50 of 47 and 16 nM, respectively.

TH9619 (TH-9619) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 47 nM.TH9619 demonstrated efficacy on HL-60 cell viability with EC50 of 11 nM.TH9619 potently inhibits related MTHFD proteins MTHFD2L and MTHFD1-(DC) with IC50 of 47 and 16 nM, respectively.TH9619 displays high potency and cancer selectivity in AML models. induce thymine-less DNA damage and apoptosis, causes uracil misincorporation into DNA, sensitize cancer cells to ATR-signaling blockade.TH9619 impairs cancer progression in vivo.TH9619 displays high selectivity toward binding and stabilizing MTHFD2 over other common folate metabolism targets such as DHFR, thymidylate synthase (TYMS), serine hydroxymethyltransferase (SHMT) 1 and SHMT2.

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).

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.

Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential anti-tumour activity.

Edatrexate (CGP 30694), as known as 10-Ethyl-10-deazaaminopterin, is Methotrexate analog, exhibits antitumor activity against MTX-resistant tumors. Edatrexate is an antifolate antimetabolite, can be used for reasearch of non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and cancer of the head and neck.

Talotrexin (PT523), an analog of Aminopterin, is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth.

TH7299 is a potent mitochondrial inhibitor of mitochondrial MTHFD2L with IC50 of 274 nM.