Thymidylate Synthase 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.

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.

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.

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.

Doxifluridine (Standard) is the analytical standard of Doxifluridine. This product is intended for research and analytical applications. Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs.

MAHS-3 is a thymidylate synthase (TS) and dihydrofolate reductase (DHFR) inhibitor, with IC₅₀ values of 5.279 μM and 52.60 μM against human targets, respectively. MAHS-3 exhibits broad-spectrum antiproliferative activity against cancer cells, induces cell cycle arrest, activates endogenous caspase-dependent apoptosis, reduces MMP levels, inhibits cell migration, increases intracellular NO levels, and promotes autophagy activity. MAHS-3 can be used in cancer-related research.

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.

MtTMPK-IN-6 (compound 1) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC₅₀ value of 29 μM. MtTMPK-IN-6 can be used for researching tuberculosis.

MAHS-4 is an inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR), with IC₅₀ values of 1.918 μM and 83.53 μM, respectively. MAHS-4 inhibits thymidylate biosynthesis, reduces tetrahydrofolate pool maintenance, and interferes with extracellular matrix remodeling. MAHS-4 induces G2/M phase cell cycle arrest, activates endogenous caspase-dependent apoptosis, decreases MMP protein levels, inhibits cell migration, increases intracellular NO levels, and promotes autophagy activity. MAHS-4 is applicable for cancer-related research.

2',2'-Difluorodeoxyuridine 5'-monophosphate (dFdUMP) is a metabolite of Gemcitabine (HY-17026) and an inhibitor of Thymidylate synthase, with an inhibition constant of 130 μM. 2',2'-Difluorodeoxyuridine 5'-monophosphate can be used in research related to ovarian cancer, hematologic malignancies, non-small cell lung cancer, pancreatic cancer, soft tissue sarcoma, and glioblastoma multiforme.

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.

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.

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.

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.

CB 3703 is an inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR). CB 3703 has an IC₅₀ of 0.25 μM against rat TS, a K_i of 0.47 μM against mouse TS, an IC₅₀ of 6.8 nM against rat DHFR, and a K_i of 0.6 pM against mouse DHFR. CB 3703 is transported via the reduced folate pathway, has a short plasma half-life, and can prolong the survival of tumor-bearing mice. CB 3703 can be used in the research of L1210 ascites tumors.

N-Acetyl-4-S-mercaptoaminophenol (N-Ac-4-S-CAP) is a compound that is selectively cytotoxic to melanocytes of black mouse hair follicles. It can cause 98% depigmentation of black mouse hair follicles. N-Ac-4-S-CAP can produce visible changes in hair follicle melanocytes 4 hours after intraperitoneal injection, including aggregation of melanin granules and nuclear condensation. Electron microscopy observations showed that it caused progressive destruction of melanocytes, including swelling of membranous organelles, nuclear condensation, and cytoplasmic vacuolation, ultimately leading to complete cell necrosis. N-Ac-4-S-CAP has a specific cytotoxic effect on melanocytes that actively produce eumelanin, but may not affect precursor or dormant melanocytes. These properties suggest that N-Ac-4-S-CAP may have potential application value in the treatment of melanoma or skin whitening.

BGC638 is a thymidylate synthase inhibitor with a K_i value of 0.24 nM. BGC638 binds to α-FR with high affinity and enters cells via receptor-mediated endocytosis, thereby potently inhibiting thymidylate synthase to block DNA synthesis and ultimately induce apoptosis. BGC638 is applicable to studies related to α-FR-overexpressing tumors and epithelial carcinomas (ovarian cancer and endometrial cancer).

Fosifloxuridine nafalbenamide (Standard) is the analytical standard of Fosifloxuridine nafalbenamide (HY-109115). This product is intended for research and analytical applications. 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.

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.

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.