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Thymidylate Synthase Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Thymidylate Synthase (38) Antifolate (12) Apoptosis (14) Autophagy (12) Bacterial (1) Bcl-2 Family (2) Biochemical Assay Reagents (1) Caspase (1) Dihydrofolate reductase (DHFR) (2) DNA Methyltransferase (2) DNA/RNA Synthesis (4) EGFR (2) Fungal (1) HSV (3) Isotope-Labeled Compounds (3) Nucleoside Antimetabolite/Analog (9) Orthopoxvirus (3) Parasite (5) PI3K (1) Reactive Oxygen Species (ROS) (1) Reference Standards (7) STAT (1)
By Research Areas:	Cancer (53) Infection (9) Inflammation/Immunology (2) Neurological Disease (1)
Click Chemistry:	Alkynes (7)
Oligonucleotides:	Nucleoside Analogs (1) Uridine (1)

Inhibitors & Agonists

Screening-Bibliotheken

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

Targets Recommended: Thymidylate Synthase Serpin PGE synthase Acetolactate Synthase (ALS) Cellulose Synthase ATP Synthase GSK-3 Fatty Acid Synthase (FASN) Glucosylceramide Synthase (GCS) Cyclic GMP-AMP Synthase NO Synthase

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-10820

Pemetrexed Maximum Cited Publications 39 Publications Verification LY231514	Antifolate Autophagy	Cancer
Pemetrexed (LY231514) is an antifolate, the K_i values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .

HY-10821

Raltitrexed 10+ Cited Publications ZD1694; D1694; ICI-D1694	Thymidylate Synthase Nucleoside Antimetabolite/Analog	Cancer
Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting **thymidylate synthase**.

HY-16478

Trifluridine/tipiracil hydrochloride mixture 3 Publications Verification TAS-102; FTD/TPI	Nucleoside Antimetabolite/Analog Thymidylate Synthase	Cancer
Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA .

HY-10820A

Pemetrexed disodium Maximum Cited Publications 39 Publications Verification LY231514 disodium	Antifolate Autophagy Apoptosis	Cancer
Pemetrexed disodium (LY231514 disodium) is an antifolate, the K_is 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 .

HY-A0061

Trifluridine 3 Publications Verification Trifluorothymidine; 5-Trifluorothymidine; TFT	Thymidylate Synthase HSV Nucleoside Antimetabolite/Analog Orthopoxvirus DNA/RNA Synthesis Apoptosis Autophagy	Cancer
Trifluridine (Trifluorothymidine) is an irreversible and orally active **thymidylate synthase** inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .

HY-W016819

5-Fluoroorotic acid	Thymidylate Synthase Parasite	Infection
5-Fluoroorotic acid is the inhibitor for **thymidylate synthase** that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid exhibits antimalarial activity .

HY-13728

Plevitrexed ZD 9331; BGC9331	Thymidylate Synthase	Cancer
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a K_i of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical . Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-13781

Pemetrexed disodium hemipenta hydrate Maximum Cited Publications 39 Publications Verification LY231514 disodium hemipenta hydrate	Antifolate Autophagy Apoptosis	Infection Neurological Disease Inflammation/Immunology Cancer
Pemetrexed (LY231514) disodium hemipenta hydrate is a CNS-penetrant antifolate, the K_i 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.

HY-108474

Nolatrexed dihydrochloride 2 Publications Verification AG 337	Thymidylate Synthase	Cancer
Nolatrexed dihydrochloride (AG 337) is an orally active and non-competitive lipophilic inhibitor of **thymidylate synthase with a K_i** of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride interacts at the folate cofactor binding site of the enzyme. Nolatrexed dihydrochloride increases sulfotransferases. Nolatrexed dihydrochloride induces cell cycle arrest in S phase of cancer cells. Nolatrexed dihydrochloride exhibits anticancer activity against cervical cancer.

HY-10820B

Pemetrexed disodium heptahydrate Maximum Cited Publications 39 Publications Verification LY231514 disodium heptahydrate	Antifolate Autophagy	Cancer
Pemetrexed disodium heptahydrate is a novel antifolate, the K_i 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.

HY-W016819B

5-Fluoroorotic acid monohydrate 5-Fluorouracil-6-carboxylic acid Monohydrate; 5-FOA; 5-fluoro OA	Thymidylate Synthase Parasite	Infection
5-Fluoroorotic acid monohydrate is the monohydrate salt form of 5-Fluoroorotic acid (HY-W016819). 5-Fluoroorotic acid monohydrate is the inhibitor for **thymidylate synthase** that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid monohydrate exhibits antimalarial activity .

HY-10820R

Pemetrexed (Standard) LY231514 (Standard)	Reference Standards Antifolate Autophagy	Cancer
Pemetrexed (Standard) is the analytical standard of Pemetrexed. This product is intended for research and analytical applications. Pemetrexed (LY231514) is an antifolate, the K_i values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .

HY-116217

5-Fluoro-2'-deoxycytidine 3 Publications Verification FdCyd; NSC-48006	DNA Methyltransferase	Cancer
5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity .

HY-109115

Fosifloxuridine nafalbenamide 2 Publications Verification NUC-3373	Thymidylate Synthase	Cancer
Fosifloxuridine nafalbenamide (NUC-3373), a pyrimidine nucleotide analogue, is a **Thymidylate synthase** inhibitor. Fosifloxuridine nafalbenamide has anticancer activity. Fosifloxuridine nafalbenamide has the potential to evoke a host immune response and enhance immunoresearch .

HY-154508

FdUMP triethylammonium 2’-Deoxy-5-Fluorouridine 5’-phosphate triethylammonium	Nucleoside Antimetabolite/Analog Thymidylate Synthase	Cancer
FdUMP triethylammonium is the intracellular active form of 5-fluorouracil (5-FU). 5-FU is converted to FdUMP after being transported into the cell by various enzymes. FdUMP forms a ternary complex with thymidylate synthase and its cofactor 5,10-methylene tetrahydrofolate, inhibiting the activity of thymidylate synthase, which in turn leads to the suppression of DNA synthesis.

HY-10822

Idetrexed BGC 945; ONX-0801; CB 300945	Thymidylate Synthase	Cancer
Idetrexed (ONX 0801) is a thymidylate synthase (TS) inhibitor with a K_i of 1.2 nM. Idetrexed can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer .

HY-134160

5,6-Dihydro-5-Fluorouracil 5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil	Nucleoside Antimetabolite/Analog	Cancer
5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.

HY-143207

10-Formyl-5,8-dideazafolic acid	Thymidylate Synthase	Cancer
10-Formyl-5,8-dideazafolic acid is a **thymidylate synthase** inhibitor .

HY-16110

Tegafur-Uracil UFT; BMS-200604	Thymidylate Synthase	Cancer
Tegafur-Uracil (UFT; BMS-200604) is an effective oral chemotherapy drug based on fluoropyrimidine. Tegafur-Uracil inhibits **thymidylate synthase**. Tegafur-Uracil can be used in combination with leucovorin (LV) and polysaccharide K (PSK) for research on solid tumors .

HY-122795

Vanoxonin	Thymidylate Synthase	Others
Vanoxonin is an inhibitor of **thymidylate synthase** found in Saccharopolyspora hirsuta with an IC₅₀ value of 0.7 μg/mL .

HY-W016819R

5-Fluoroorotic acid (Standard)	Reference Standards Thymidylate Synthase Parasite	Infection
5-Fluoroorotic acid is the inhibitor for thymidylate synthase that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid exhibits antimalarial activity .

HY-10822A

Idetrexed trisodium BGC 945 trisodium; ONX 0801 trisodium; CB 300945 trisodium	Thymidylate Synthase	Cancer
Idetrexed (ONX 0801) trisodium is a thymidylate synthase (TS) inhibitor with a K_i of 1.2 nM. Idetrexed trisodium can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer .

HY-10820BR

Pemetrexed disodium heptahydrate (Standard) LY231514 disodium heptahydrate (Standard)	Reference Standards Antifolate Autophagy	Cancer
Pemetrexed (disodium heptahydrate) (Standard) is the analytical standard of Pemetrexed (disodium heptahydrate). This product is intended for research and analytical applications. 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.

HY-A0061S

Trifluridine-13C,15N2 Trifluorothymidine-¹³C,¹⁵N₂; 5-Trifluorothymidine-¹³C,¹⁵N₂; TFT-¹³C,¹⁵N₂	Thymidylate Synthase Nucleoside Antimetabolite/Analog HSV Orthopoxvirus	Cancer
Trifluridine- ¹³C, ¹⁵N₂ is the ¹³C and ¹⁵N labeled Trifluridine . Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity .

HY-10823

OSI-7904L GW1843; 1843U89; OSI-7904	Thymidylate Synthase DNA/RNA Synthesis	Cancer
OSI-7904L (GW1843; 1843U89; OSI-7904) is a thymidylate synthase (TS) inhibitor with a K_i of 90 pM. OSI-7904L blocks de novo synthesis of thymidine nucleotides, DNA synthesis and induces cell death. OSI-7904L inhibits the growth of human cells, induces tumor regression, and achieves durable antitumor effects in mouse xenograft models. OSI-7904L can be used in research related to colon adenocarcinoma .

HY-134160S

5,6-Dihydro-5-Fluorouracil-13C,15N2 5-DHFU-¹³C,¹⁵N₂; 5-Fluorodihydropyrimidine-2,4-dione-¹³C,¹⁵N₂; 5-Fluorodihydrouracil-¹³C,¹⁵N₂	Isotope-Labeled Compounds Nucleoside Antimetabolite/Analog	Cancer
5,6-Dihydro-5-Fluorouracil- ¹³C, ¹⁵N₂ (5-DHFU- ¹³C, ¹⁵N₂) is the ¹³C- and ¹⁵N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC₅₀=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.

HY-146239

EGFR/HER2/TS-IN-2	EGFR Thymidylate Synthase	Cancer
EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC₅₀ values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC₅₀ of 1.69 µM .

HY-162155

Diarctigenin	Parasite	Infection
Diarctigenin is a selective Leishmania major dihydrofolate reductase-thymidylate synthase (LmDHFR-TS) inhibitor. Diarctigenin can be used for the research of tropical disease .

HY-10821R

Raltitrexed (Standard) ZD1694 (Standard); D1694 (Standard); ICI-D1694 (Standard)	Thymidylate Synthase Nucleoside Antimetabolite/Analog Reference Standards	Cancer
Raltitrexed (Standard) is the analytical standard of Raltitrexed. This product is intended for research and analytical applications. Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting thymidylate synthase.

HY-118251

PD130883	Antifolate Dihydrofolate reductase (DHFR)	Cancer
PD130883 is an antifolate DHFR inhibitor that directly inhibits thymidylate synthase at the 5,10-methylenetetrahydrofolate binding site, reducing the net conversion of tetrahydrofolate cofactor to dihydrofolate.

HY-178288

TS-IN-7	Thymidylate Synthase	Cancer
TS-IN-7 (Compound 6) is a thymidylate synthase (TS) inhibitor with an IC₅₀ of 39 nM. TS-IN-7 can be used for the study of cancer chemotherapy .

HY-N14161

Diazaquinomycin A	Thymidylate Synthase Apoptosis	Cancer
Diazaquinomycin A (DAQA), a diaza-anthracene antibiotic, is a **thymidylate synthase** inhibitor. Diazaquinomycin A (DAQA) induces DNA damage, cell cycle arrest, and apoptosis through cleaved-PARP .

HY-117247

5,6,7,8-Tetrahydro-8-deazahomofolic acid	DNA/RNA Synthesis	Infection
5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor with inhibitory activity against other folate-related enzymes. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed mild growth inhibition against enterococci, lactic acid bacteria, and L1210 cells in culture. 5,6,7,8-Tetrahydro-8-deazahomofolic acid also showed weak inhibition against thymidylate synthase, dihydrofolate reductase, glycyl-ribonucleoside aminotransferase, and aminoimidazole-carboxyacyl-ribonucleoside aminotransferase. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed low substrate activity for thymidylate synthase .

HY-120293

CB30900	Thymidylate Synthase	Cancer
CB30900 is an inhibitor for **thymidylate synthase with an IC₅₀ of 0.2 μM. CB30900 exhibits cytotoxicity in W1L2 with an IC₅₀** of 0.13 μM .

HY-19157

Metesind glucuronate AG 331	Thymidylate Synthase	Cancer
Metesind glucuronate (AG 331) is an inhibitor for **thymidylate synthase with K_i** of 1.2 nM. Metesind glucuronate inhibits the DNA synthesis and thus inhibits the cell viability of cancer cells with IC₅₀ of 0.4-0.9 μM .

HY-W142014

N,O-Didansyl-L-tyrosine cyclohexylammonium	Thymidylate Synthase	Cancer
N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylate synthase (TS) inhibitor, acts on TS of Escherichia coli, Lactobacillus casei and human with the IC₅₀ values of 5.0, 3.4 and 119 μM, respectively .

HY-149849

TS-IN-2	Thymidylate Synthase	Cancer
TS-IN-2 (compound 17) is a thymidylate synthase (TS) inhibitor with an IC₅₀ of 0.81 μM. TS-IN-2 induces cancer cell apoptosis and cell cycle arrest in S phase, and also inhibit DNA synthesis, resulting in DNA damage .

HY-10820S

Pemetrexed-d5 LY231514-d₅	Antifolate Autophagy	Cancer
Pemetrexed-d₅ is the deuterium labeled Pemetrexed . Pemetrexed (LY231514) is an antifolate, the K_i values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .

HY-10820AS

Pemetrexed-d5 disodium LY231514-d5 disodium	Isotope-Labeled Compounds Antifolate Autophagy Apoptosis	Cancer
Pemetrexed-d₅ disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the K_is 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 .

HY-168918

Insecticidal agent 19	Parasite Dihydrofolate reductase (DHFR)	Infection
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-170648

TS-IN-5	Thymidylate Synthase Apoptosis PI3K STAT Bcl-2 Family	Cancer
TS-IN-5 (Compound 15) is a thymidylate synthase (TS) inhibitor. TS-IN-5 induces Apoptosis by modulating Bax, BCL-2, PI3K, and STAT1 proteins. TS-IN-5 shows antitumor effects against liver, breast and colon cancers .

HY-149352

DG1	Thymidylate Synthase	Cancer
DG1 (Compound 8Nc) is a **Thymidylate Synthase** (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .

HY-13781R

Pemetrexed disodium hemipenta hydrate (Standard) LY231514 disodium hemipenta hydrate (Standard)	Antifolate Autophagy Apoptosis Reference Standards	Cancer
Pemetrexed (disodium hemipenta hydrate) (Standard) is the analytical standard of Pemetrexed (disodium hemipenta hydrate). This product is intended for research and analytical applications. Pemetrexed disodium hemipenta hydrate 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.

HY-13728B

(Rac)-Plevitrexed (Rac)-ZD 9331; (Rac)-BGC9331	Thymidylate Synthase	Cancer
(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor. (Rac)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-13728A

(R)-Plevitrexed (R)-ZD 9331; (R)-BGC9331	Biochemical Assay Reagents	Cancer
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-172172

TS-IN-6	Thymidylate Synthase Apoptosis	Cancer
TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC₅₀ value of 0.54 μM, demonstrating significant antiproliferative activity. TS-IN-6 induces G1 phase cell cycle arrest and apoptosis (marked by substantial increases in both early and late apoptotic rates) and shows potential for research on cancers such as colon, breast, and liver cancers .

HY-W769288

Pemetrexed disodium-13C5 LY231514 disodium-13C5	Isotope-Labeled Compounds Apoptosis Antifolate Autophagy	Cancer
Pemetrexed disodium- ¹³C₅ (LY231514 disodium- ¹³C₅) is the ¹³C-labeled Pemetrexed disodium (HY-10820A). 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 .

HY-146238

EGFR/HER2/TS-IN-1	EGFR Thymidylate Synthase Apoptosis	Cancer
EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC₅₀ values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis .

HY-124093

8-Deazahomofolic acid	Thymidylate Synthase Bacterial	Infection Cancer
8-Deazahomofolic acid is an inhibitor of thymidylate synthase (TS) and other folate-related enzymes. 8-Deazahomofolic acid shows inhibitory activity against folate-dependent S. faecium, L. casei, and MTX (HY-14519) resistant strains. 8-Deazahomofolic acid also inhibits the growth of L1210 leukemia cells, with an IC₅₀ value of 87.5 μM. 8-Deazahomofolic acid can be used in research on bacterial infections and tumors .

HY-A0061R

Trifluridine (Standard) Trifluorothymidine (Standard); 5-Trifluorothymidine (Standard); TFT (Standard)	Reference Standards Thymidylate Synthase HSV Nucleoside Antimetabolite/Analog Orthopoxvirus DNA/RNA Synthesis Apoptosis Autophagy	Cancer
Trifluridine (Standard) is the analytical standard of Trifluridine. This product is intended for research and analytical applications. Trifluridine (Trifluorothymidine) is an irreversible and orally active **thymidylate synthase** inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .

Art. -Nr.	Produktname

HY-L044

Nucleotide Compound Library

575 compounds

Nucleoside and nucleotide analogues are synthetic, chemically modified compounds that have been developed to mimic their physiological counterparts in order to exploit cellular metabolism and subsequently be incorporated into DNA and RNA to inhibit cellular division and viral replication. In addition to their incorporation into nucleic acids, nucleoside and nucleotide analogues can interact with and inhibit essential enzymes such as human and viral polymerases (that is, DNA-dependent DNA polymerases, RNA-dependent DNA polymerases or RNA-dependent RNA polymerases), kinases, ribonucleotide reductase, DNA methyltransferases, purine and pyrimidine nucleoside phosphorylase and thymidylate synthase. These actions of nucleoside and nucleotide analogues have potential therapeutic benefits — for example, in the inhibition of cancer cell growth, the inhibition of viral replication as well as other indications.

MCE offers a unique collection of 575 nucleotide compounds including nucleotide, nucleoside and their structural analogues. MCE Nucleotide Compound Library is a useful tool to discover anti-cancer and antiviral drugs for high throughput screening (HTS) and high content screening (HCS).

Art. -Nr.	Produktname	Target	Research Area

HY-W142014

N,O-Didansyl-L-tyrosine cyclohexylammonium	Thymidylate Synthase	Cancer
N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylate synthase (TS) inhibitor, acts on TS of Escherichia coli, Lactobacillus casei and human with the IC₅₀ values of 5.0, 3.4 and 119 μM, respectively .

Art. -Nr.	Produktname	Category	Target	Chemical Structure

HY-122795

Vanoxonin	Natürliche Produkte Microorganisms Source Classification	Thymidylate Synthase
Vanoxonin is an inhibitor of **thymidylate synthase** found in Saccharopolyspora hirsuta with an IC₅₀ value of 0.7 μg/mL .

HY-N14161

Diazaquinomycin A	Microorganisms Antibiotics Other Antibiotics Source Classification	Thymidylate Synthase Apoptosis
Diazaquinomycin A (DAQA), a diaza-anthracene antibiotic, is a **thymidylate synthase** inhibitor. Diazaquinomycin A (DAQA) induces DNA damage, cell cycle arrest, and apoptosis through cleaved-PARP .

HY-124900

Tylophorinicine	Apocynaceae Structural Classification Alkaloids Piperidine Alkaloids Plants Tylophora ovata (Lindl.) Hook. ex Steud. Source Classification	Fungal
Tylophorinicine is an anti-leukemic and anti-fungal agent. Tylophorinicine exhibits minimum inhibitory concentrations (MIC) in the range of 2-4 mg/mL for TdnH and 0.6-2.5 mg/mL for TnnH against Candida species. Tylophorinicine is a phenanthroindolizidine alkaloid from tylophora asthamatica and pergulatia pallid. Tylophorinicine inhibits thymidylate synthase by pergularinine .

Art. -Nr.	Produktname	Chemical Structure

HY-A0061S

Trifluridine-13C,15N2
Trifluridine- ¹³C, ¹⁵N₂ is the ¹³C and ¹⁵N labeled Trifluridine . Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity .

HY-134160S

5,6-Dihydro-5-Fluorouracil-13C,15N2

5,6-Dihydro-5-Fluorouracil- ¹³C, ¹⁵N₂ (5-DHFU- ¹³C, ¹⁵N₂) is the ¹³C- and ¹⁵N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC₅₀=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.

HY-10820S

Pemetrexed-d5
Pemetrexed-d₅ is the deuterium labeled Pemetrexed . Pemetrexed (LY231514) is an antifolate, the K_i values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .

HY-10820AS

Pemetrexed-d5 disodium
Pemetrexed-d₅ disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the K_is 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 .

HY-W769288

Pemetrexed disodium-13C5
Pemetrexed disodium- ¹³C₅ (LY231514 disodium- ¹³C₅) is the ¹³C-labeled Pemetrexed disodium (HY-10820A). 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 .

Art. -Nr.	Produktname		Classification

HY-13728

Plevitrexed ZD 9331; BGC9331		Alkynes
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a K_i of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical . Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-10822

Idetrexed BGC 945; ONX-0801; CB 300945		Alkynes
Idetrexed (ONX 0801) is a thymidylate synthase (TS) inhibitor with a K_i of 1.2 nM. Idetrexed can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer .

HY-10822A

Idetrexed trisodium BGC 945 trisodium; ONX 0801 trisodium; CB 300945 trisodium		Alkynes
Idetrexed (ONX 0801) trisodium is a thymidylate synthase (TS) inhibitor with a K_i of 1.2 nM. Idetrexed trisodium can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer .

HY-120293

CB30900		Alkynes
CB30900 is an inhibitor for **thymidylate synthase with an IC₅₀ of 0.2 μM. CB30900 exhibits cytotoxicity in W1L2 with an IC₅₀** of 0.13 μM .

HY-13728B

(Rac)-Plevitrexed (Rac)-ZD 9331; (Rac)-BGC9331		Alkynes
(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor. (Rac)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-13728A

(R)-Plevitrexed (R)-ZD 9331; (R)-BGC9331		Alkynes
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-113798

ICI 198583		Alkynes
ICI 198583 is a thymidylate synthase (TS) inhibitor with a K_i value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a K_m of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia .

Art. -Nr.	Produktname		Classification

HY-154508

FdUMP triethylammonium 2’-Deoxy-5-Fluorouridine 5’-phosphate triethylammonium		Nucleoside Analogs Uridine
FdUMP triethylammonium is the intracellular active form of 5-fluorouracil (5-FU). 5-FU is converted to FdUMP after being transported into the cell by various enzymes. FdUMP forms a ternary complex with thymidylate synthase and its cofactor 5,10-methylene tetrahydrofolate, inhibiting the activity of thymidylate synthase, which in turn leads to the suppression of DNA synthesis.

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