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DHFR-TS

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By Targets:	Dihydrofolate reductase (DHFR) (4) E3 Ligase Ligand-Linker Conjugates (1) Ligands for E3 Ligase (1) Parasite (5) PROTACs (2)
By Research Areas:	Endocrinology (1) Infection (6)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-178728

BION106	PROTACs Parasite Dihydrofolate reductase (DHFR)	Infection
BION106 is a *dihydrofolate reductasethymidylate synthase (DHFR-TS) PROTAC* degrader. BION106 exhibits extremely strong anti-malarial activity with a K_i and toxicity of 2.68 nM and 0.2 μM against Plasmodium falciparum, and > 100 μM and 44.2 μM in mammalian cells. BION106 can be used for the study of antimalarial parasites (Blue: Idasanutlin ligand (HY-15676); Pink: DHFR-TS ligand (HY-153007); Black: Linker (HY-W021401)) .

HY-149958

Antileishmanial agent-17	Parasite	Infection
Antileishmanial agent-17 is a coumarin hybrid compound with antileishmanial effects (IC₅₀ <0.78 μM). Antileishmanial agent-17 is safe to normal VERO cells. Antileishmanial agent-17 binds to folate pathway enzymes pteridine reductase and DHFR-TS. And Antileishmanial agent-17 shows the most potent with IC₅₀ value of 0.40 μM against promastigote and 0.68 μM against amastigote, respectivley.

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-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-178759

DHFR-IN-5-amino-PEG3-C2-azido	E3 Ligase Ligand-Linker Conjugates	Infection
DHFR-IN-5-amino-PEG3-C2-azido is a synthesized E3 ligase ligand-linker conjugate that can be used to synthesize BION106 (HY-178728). BION106 is a potent DHFR-TS PROTAC degrader with anti-malarial activity .

HY-181813

*PROTAC DHFR* Degrader-1**	PROTACs Ligands for E3 Ligase Dihydrofolate reductase (DHFR) Parasite	Infection
PROTAC DHFR Degrader-1 is a selective PROTAC degrader targeting Plasmodium falciparum *DHFR-TS* with a K_i of 2.01 nM. PROTAC DHFR Degrader-1 exhibits no inhibitory activity against human DHFR and suppresses the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 can be used for the research of Plasmodium falciparum and malaria .

HY-105714

Etoprine	Dihydrofolate reductase (DHFR)	Endocrinology
Etoprine is a potent orally active dihydrofolate reductase (DHFR) inhibitor. Etoprine competitively inhibits testicular *DHFR* to disrupt tetrahydrofolate and DNA synthesis in rapidly dividing cells. Etoprine acts as an antifertility agent in male mice and reduces fecundity in male rats .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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DHFR-TS

Inhibitors & Agonists