Thymidylate Synthase

By Targets:	Thymidylate Synthase (16) Antifolate (6) Apoptosis (5) Autophagy (7) DNA Methyltransferase (1) DNA/RNA Synthesis (1) EGFR (2) Endogenous Metabolite (2) HSV (2) Isotope-Labeled Compounds (1) Nucleoside Antimetabolite/Analog (4) Orthopoxvirus (2) Parasite (1)
By Research Areas:	Cancer (25) Infection (1) Metabolic Disease (2)
Click Chemistry:	Alkynes (5)

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-16110

Tegafur-Uracil UFT; BMS-200604	Others	Cancer
Tegafur-Uracil is an orally active fluoropyrimidines anticancer agent. Tegafur-Uracil inhibits thymidylate synthase. Tegafur-Uracil can be used for researching anti solid tumors .

HY-16478

Trifluridine/tipiracil hydrochloride mixture 1 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-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-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-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-10822

Idetrexed BGC 945; ONX-0801	Thymidylate Synthase	Others
Idetrexed is a **thymidylate synthase** inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a K_i of 1.2 nmol/L .

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-10821

Raltitrexed 5 Publications Verification ZD1694; D1694; ICI-D1694	Thymidylate Synthase Nucleoside Antimetabolite/Analog	Cancer
Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting **thymidylate synthase**.

HY-108474

Nolatrexed dihydrochloride 1 Publications Verification AG 337; Thymitaq	Thymidylate Synthase	Cancer
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of **thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a K_i** of 11 nM for human thymidylate synthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .

HY-143207

10-Formyl-5,8-dideazafolic acid

Thymidylate Synthase Cancer

10-Formyl-5,8-dideazafolic acid is a thymidylate synthase inhibitor .

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

HY-10822A

ONX 0801 trisodium BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium	Thymidylate Synthase	Cancer
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors .

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-106168

Thymectacin NB1011	Others	Cancer
Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylate synthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin) .

HY-13781

Pemetrexed disodium hemipenta hydrate Maximum Cited Publications 17 Publications Verification LY231514 disodium hemipenta hydrate	Antifolate Autophagy Apoptosis	Cancer
Pemetrexed disodium hemipenta hydrate 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-10820B

Pemetrexed disodium heptahydrate Maximum Cited Publications 17 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-10820

Pemetrexed Maximum Cited Publications 17 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-10820A

Pemetrexed disodium Maximum Cited Publications 17 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-W011142

2'-Deoxyuridine 5'-monophosphate disodium	Endogenous Metabolite	Metabolic Disease
2'-Deoxyuridine 5'-monophosphate disodium is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylate synthase (TS). dTMP is a nucleotide required for DNA synthesis .

HY-109115

Fosifloxuridine nafalbenamide 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-10820S

Pemetrexed-d5 LY231514-d₅	Antifolate Autophagy	Cancer
Pemetrexed-d₅ is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki 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[2].

HY-116217

5-Fluoro-2'-deoxycytidine	DNA Methyltransferase	Cancer
5-Fluoro-2'-deoxycytidine, a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of the potent thymidylate synthase inhibitor 5-fluoro-2′-dUMP .

HY-10820AS

Pemetrexed-d5 disodium LY231514-dd₅ 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 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[1].

HY-A0061

Trifluridine 1 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-14520A

(6S)-Tetrahydrofolic acid (6S)-5,6,7,8-Tetrahydrofolic acid; (6S)-Tetrahydrofolic acid	Endogenous Metabolite	Metabolic Disease
(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylate synthase and 600-fold more active as a growth factor of P. cerevisiae. (6S)-Tetrahydrofolic acid also has a low affinity and high dissociation rate for folate-binding protein .

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[1]. 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[2].

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-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-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.

Cat. No.	Product Name

HY-L044

Nucleotide Compound Library	491 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 491 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).

Nucleotide Compound Library

491 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 491 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).

Cat. No.	Product Name	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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W011142

2'-Deoxyuridine 5'-monophosphate disodium	Natural Products Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
2'-Deoxyuridine 5'-monophosphate disodium is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylate synthase (TS). dTMP is a nucleotide required for DNA synthesis .

HY-14520A

(6S)-Tetrahydrofolic acid (6S)-5,6,7,8-Tetrahydrofolic acid; (6S)-Tetrahydrofolic acid	Human Gut Microbiota Metabolites Microorganisms Source classification Endogenous metabolite	Endogenous Metabolite
(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylate synthase and 600-fold more active as a growth factor of P. cerevisiae. (6S)-Tetrahydrofolic acid also has a low affinity and high dissociation rate for folate-binding protein .

Cat. No.	Product Name	Chemical Structure

HY-10820S

Pemetrexed-d5
Pemetrexed-d₅ is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki 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[2].

HY-10820AS

Pemetrexed-d5 disodium
Pemetrexed-d₅ (disodium) is the deuterium labeled Pemetrexed disodium. 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[1].

HY-A0061S

Trifluridine-13C,15N2
Trifluridine- ¹³C, ¹⁵N₂ is the ¹³C and ¹⁵N labeled Trifluridine[1]. 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[2].

Cat. No.	Product Name	Application	Reactivity

HY-P80973

Thymidylate Synthase Antibody TS; TMS; HST422	WB, IHC-F, IHC-P, ICC/IF, IP	Human
Thymidylate Synthase Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 36 kDa, targeting to thymidylate synthase. It can be used for WB, IHC-F, IHC-P, ICC/IF, IP assays with tag free, in the background of Human.

Cat. No.	Product Name		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-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-10822

Idetrexed BGC 945; ONX-0801		Alkynes
Idetrexed is a **thymidylate synthase** inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a K_i of 1.2 nmol/L .

HY-10822A

ONX 0801 trisodium BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium		Alkynes
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors .

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