Dihydrofolate reductase (DHFR) Inhibitor

Dihydrofolate reductase (DHFR) Inhibitors (65):

Cat. No.	Product Name	Effect	Purity

HY-10373

Trimetrexate	Inhibitor	99.60%
Trimetrexate (CI-898) 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 can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.

HY-116387

WR99210	Inhibitor	99.10%
WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC₅₀<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine< (HY-18062)-resistant P. falciparum strains) as well as T. gondii.

HY-108251

Methotrexate metabolite	Inhibitor	98.44%
Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC₅₀ values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation.

HY-W587663

4′-DTMP	Inhibitor
4 '-DTMP is a DHFR inhibitor with Ki of 5.1 nM (DHFR^WT) and 34.3 nM (DHFR^L28R), respectively. 4 '-DTMP carries a polar modification that induces additional local interactions with the enzyme. In particular, the hairpin structure on the M20 ring is related to the internal communication of the DHFR. 4 '-DTMP has potential inhibition of E.coli.

HY-160254

1954U89	Inhibitor
1954U89 is a potent, lipid-soluble and orally active inhibitor of dihydrofolate reductase (DHFR). 1954U89 exhibits anticancer activity.

HY-137357

5-Monobutyl methotrexate	Inhibitor
5-Monobutyl methotrexate (NSC 305986; γ-MBMTX) is a dihydrofolate reductase (DHFR) inhibitor and esterase substrate. 5-Monobutyl methotrexate is hydrolyzed by esterases to produce methotrexate. In rhesus monkeys, 5-Monobutyl methotrexate clears more slowly from cerebrospinal fluid than from serum, and its serum protein binding rate exceeds 99%. At the same dose rate, 5-Monobutyl methotrexate achieves cerebrospinal fluid concentrations comparable to those of Methotrexate (HY-14519), and exhibits activity against Methotrexate-resistant cells (with transport defects) that is comparable to that against sensitive parental cells. 5-Monobutyl methotrexate can be used in studies related to Methotrexate-resistant tumors.

HY-185443

UCP1172	Inhibitor
UCP1172 is an antibacterial (Antibacterial) agent and Dihydrofolate reductase inhibitor, with an IC₅₀ of 0.0089 μM against Staphylococcus aureus DfrB, 0.22 μM against DfrG, 0.41 μM against DfrA, and 0.030 μM against DfrK. UCP1172 potently inhibits the growth of MRSA/MSSA isolates carrying dfrG and dfrK (MIC values of 0.3125-0.625 μg/mL), shows weak activity against MRSA carrying dfrA (MIC of 5 μg/mL), and exerts extremely potent inhibitory effects on wild-type S. aureus ATCC 43300 (MIC of 0.0098 μg/mL). UCP1172 can be used in studies related to tuberculosis and Staphylococcus aureus infections.

HY-116387A

WR99210 hydrochloride	Inhibitor	98.34%
WR99210 hydrochloride is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC₅₀<0.075 nM). WR99210 hydrochloride shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains as well as T. gondii.

HY-106434

Piritrexim	Inhibitor	99.07%
Piritrexim (BW 301U) is a potent dihydrofolate reductase (DHFR) inhibitor against Pneumocystis carinii and Toxoplasma gondii, with IC₅₀ values of 0.038 and 0.011 μM, respectively. Piritrexim can be used for acquired immune deficiency syndrome (AIDS) research. Piritrexim also is an anticancer agent.

HY-B0921

Succinylsulfathiazole	Inhibitor	99.22%
Succinylsulfathiazole (Succinylsulphathiazole) is a long-acting sulfonamide antibiotic with localized gut-specific antibacterial activity and is orally active. Succinylsulfathiazole inhibits bacterial folate synthesis, reduces coliform counts, suppresses intestinal bacterial growth and vitamin biosynthesis, and depletes gut folate-producing bacteria. Succinylsulfathiazole modulates hepatic mTOR signaling, diminishes cecal fermentation, decreases hepatic folate levels and total folate excretion, elevates nitrogen excretion and reduces the fermentability of certain dietary fibers. Succinylsulfathiazole induces folate deficiency and triggers biotin- and folate-related nutritional deficiency symptoms in rats and C57BL/6 mice.

HY-162475

Fluorofolin	Inhibitor	99.85%
Fluorofolin is a dihydrofolate reductase (DHFR) inhibitor with an IC₅₀ of 2.5 nM. Fluorofolin exhibits significant activity against P. aeruginosa.

HY-124350

10-Formylfolic acid	Inhibitor
10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.

HY-151159

DHFR-IN-4	Inhibitor	99.19%
DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC₅₀ value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC₅₀s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells.

HY-169790

Phomarin	Inhibitor	98.53%
Phomarin is an inhibitor for dihydrofolate reductase (DHFR). Phomarin exhibits activity against Plasmodium parasites and fungi including Mycrobotryum violaceum and Botrytis cinerea. Phomarin can be used for the research of malaria and fungal infections.

HY-153007

DHFR-IN-5	Inhibitor	99.27%
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a K_i value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity.

HY-122045

CB 3705	Inhibitor
CB 3705 is a dihydrofolate reductase (DHFR) and thymidylate synthetase (TS) inhibitor. CB 3705 inhibits L1210 cells and mutant L1210 cell line (L1210:C15) with ID₅₀s of 4.77 μM and 408 μM, respectively.

HY-151458

VEGFR-2/DHFR-IN-1	Inhibitor
VEGFR-2/DHFR-IN-1 (compound 8b) is an inhibitor of VEGFR-2 and DHFR with IC₅₀s of 0.384 and 7.881 μM, respectively. VEGFR-2/DHFR-IN-1 shows good antibacterial activities against Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA and MRSA with MIC values of 16, 16, 16, 8, and 16 μg/mL, respectively. VEGFR-2/DHFR-IN-1 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC₅₀ values of 2.97-7.12 μM. VEGFR-2/DHFR-IN-1 can be used for the research of cancer.

HY-122289

Metioprim	Inhibitor
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria.

HY-168918

Insecticidal agent 19	Inhibitor
Insecticidal agent 19 (Compound 7b) exhibits antimalarial activity by inhibiting dihydrofolate reductase-thymidylate synthase (DHFR-TS) and pteridine reductase 1 (PTR1) through the folic acid metabolic pathway. Insecticidal agent 19 inhibits Leishmania major promastigote and amastigote with IC₅₀ of 1.43 μM and 3.78 μM.

HY-108251R

Methotrexate metabolite (Standard)	Inhibitor
Methotrexate metabolite (Standard) is the analytical standard of Methotrexate metabolite. This product is intended for research and analytical applications. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent.

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