Thymidylate Synthase

Related Products

Thymidylate synthase (TSase) is a key enzyme in cell proliferation as it catalyzes a reaction essential for DNA replication, a reductive methylation of 2′-deoxyuridine-5′-monophosphate (dUMP) to form 2′-deoxythymidine-5′-monophosphate (dTMP) using the co-substrate N5,N10-methylene-5,6,7,8-tetrahydrofolate (CH2H4F).

The activity and expression of TSase are tightly controlled throughout the cell cycle, particularly at the translational level. The TSase protein itself binds to the TSase mRNA both at the translational start site (TSS) and in the coding region, inhibiting translational processing of the message. TSase can also bind to the mRNA of at least nine other important gene products, including those of p53 and c-myc. Therefore, manipulating the level of the TSase protein could induce a cascade of consequential effects on cell growth. Because of its importance in DNA precursor synthesis and repair, TSase has proved to be an important target for many chemotherapeutic and antibiotic drugs. Structural analogs of dUMP (e.g., fluoropyrimidines) and CH2H4F (e.g., antifolates) are well-established drugs targeting thymidylate synthase.

Thymidylate Synthase Inhibitors (46)

Thymidylate Synthase Related Products (50)
Antibodies (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-162698

JMF4073	Inhibitor
JMF4073 is a thymidylate (TMP) and cytidylate (CMP) kinases inhibitor with IC₅₀s of 0.16 μM and 0.17 μM, respectively. JMF4073 eliminates wild-type (WT)-Bcr-Abl-transformed myeloid cells in vitro and in vivo.

HY-123259

CB3731
CB3731 is an analogue of N-10-(fluoroethyl)quinazolinylfolate and can be used for fluorine-19 nuclear magnetic resonance studies of binary and ternary complexes of thymidylate synthase.

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].

HY-144664

MtTMPK-IN-2	Inhibitor
MtTMPK-IN-2 (compound 15) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC₅₀ value of 1.1 μM. MtTMPK-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-2 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC₅₀ = 6.1 μM). MtTMPK-IN-2 can be used for researching tuberculosis.

HY-16638

CB 3717	Inhibitor
CB 3717 is a potent inhibitor of human thymidylate synthetase, competitively binding with 5,10-methylenetetrahydrofolate (Ki = 4.9 X 10(-9) M). It also competitively inhibits human dihydrofolate reductase with dihydrofolate (Ki = 2.3 X 10(-8) M). In WI-L2 human lymphoblastoid cells, CB 3717 treatment led to a significant decrease in cellular dTTP levels and a notable increase in dUMP levels, indicating a disruption in nucleotide metabolism. The growth-inhibitory effect of CB 3717 was reversed by thymidine supplementation, demonstrating that thymidylate synthetase became rate-limiting in the presence of this compound. Delayed thymidine supplementation beyond 8 hours resulted in severe cytotoxicity, underscoring the critical timing of nucleotide rescue strategies in CB 3717-treated cells.

HY-144663

MtTMPK-IN-1	Inhibitor
MtTMPK-IN-1 (compound 3) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC₅₀ value of 2.5 μM. MtTMPK-IN-1 has moderate to weak activity against Mtb H37Rv and low cytotoxicity in human fibroblast cells MRC-5. MtTMPK-IN-1 can be used for researching tuberculosis.

HY-105262

Galocitabine	Inhibitor
Galocitabine (Ro 09-1390) is a nucleoside analog with anticancer and antiviral activity.

HY-W142014

N,O-Didansyl-L-tyrosine cyclohexylammonium	Inhibitor
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-146239

EGFR/HER2/TS-IN-2	Inhibitor
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-10822A

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

HY-146702

MtTMPK-IN-8	Inhibitor
MtTMPK-IN-8 (compound 27) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor. MtTMPK-IN-8 has sub-micromolar activity against mycobacteria (MICs = 0.78~9.4 μM) without significant cytotoxicity. MtTMPK-IN-8 can be used for researching tuberculosis.

HY-122795

Vanoxonin	Inhibitor
Vanoxonin is an inhibitor of thymidylate synthase found in Saccharopolyspora hirsuta with an IC₅₀ value of 0.7 μg/mL.

HY-146701

MtTMPK-IN-7	Inhibitor
MtTMPK-IN-7 (compound 26) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC₅₀ value of 47 μM. MtTMPK-IN-7 has sub-micromolar activity against mycobacteria (MICs = 2.3~4.7 μM) without significant cytotoxicity. MtTMPK-IN-7 can be used for researching tuberculosis.

HY-13728B

(Rac)-Plevitrexed	Inhibitor
(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-19157

Metesind glucuronate	Inhibitor
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-144665

MtTMPK-IN-3	Inhibitor
MtTMPK-IN-3 (compound 25) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC₅₀ value of 0.12 μM. MtTMPK-IN-3 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-3 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC₅₀ = 12.5 μM). MtTMPK-IN-3 can be used for researching tuberculosis.

HY-146238

EGFR/HER2/TS-IN-1	Inhibitor
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-146703

MtTMPK-IN-9	Inhibitor
MtTMPK-IN-9 (compound 28) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC₅₀ value of 48 μM. MtTMPK-IN-9 has sub-micromolar activity against mycobacteria (MICs = 6.25~9.4 μM) without significant cytotoxicity. MtTMPK-IN-9 can be used for researching tuberculosis.

HY-121256

Chlorasquin	Inhibitor
Chlorasquin inhibits thymidylate synthetase with an approximate K_i value of 4.9 μM. Chlorasquin is also a folate antagonist, testing the Methotrexate (HY-14519) effect. Chlorasquin binds tighter to dihydrofolate reductase at alkaline pH than does Methotrexate, which is promising for research of antipsoriatic agents.

HY-149352

DG1	Inhibitor
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.

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Thymidylate Synthase

Thymidylate Synthase

Thymidylate Synthase Related Products (50)

Antibodies (1)

Thymidylate Synthase Related Products (50):