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Results for "

GARFT

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antifolate (17) Apoptosis (8) Autophagy (9) Bcl-2 Family (3) Caspase (3) Isotope-Labeled Compounds (1)
By Research Areas:	Cancer (18)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14521

Lometrexol 1 Publications Verification DDATHF	Antifolate Apoptosis Caspase Bcl-2 Family	Cancer
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .

HY-14521B

Lometrexol hydrate 1 Publications Verification DDATHF hydrate	Antifolate Apoptosis Caspase Bcl-2 Family	Cancer
Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .

HY-14521A

Lometrexol disodium 1 Publications Verification DDATHF disodium	Antifolate Apoptosis Caspase Bcl-2 Family	Cancer
Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .

HY-10818

LY309887	Antifolate	Cancer
LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a K_i of 6.5 nM, and has antitumor activity.

HY-13781

Pemetrexed disodium hemipenta hydrate Maximum Cited Publications 24 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 24 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 24 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 24 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-14522

LY 222306	Antifolate	Cancer
LY 222306 is a glycinamide ribonucleotide formyltransferase *(GARFT)* inhibitor with a K_i of 0.77 nM.

HY-10819

AG2034	Others	Cancer
AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a K_i of 28 nM against human *GARFT, and it binds with high affinity to the folate receptor (K_d* of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a K_m of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC₅₀ values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED .

HY-126119

5,10-Dideazafolic acid	Antifolate	Cancer
5,10-Dideazafolic acid is a 5,10-dideaza-5,6,7,8-tetrahydrofola analogue, which exhibits some inhibitory activity against glycine amide ribonucleotide formyltransferase (GARFT) (K_i=13 μM) .

HY-14530

Pelitrexol 1 Publications Verification AG 2037	Antifolate	Cancer
Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice .

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-10820R

Pemetrexed (Standard)	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-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-10820AR

Pemetrexed disodium (Standard)	Antifolate Autophagy Apoptosis	Cancer
Pemetrexed (disodium) (Standard) is the analytical standard of Pemetrexed (disodium). This product is intended for research and analytical applications. 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-10820BR

Pemetrexed disodium heptahydrate (Standard)	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-126830

Antifolate C2	Antifolate Apoptosis	Cancer
Antifolate C2 is an anti-folate compound that has inhibitory effects on the proliferation of non-squamous non-small cell lung cancer (NS-NSCLC). Antifolate C2 achieves tumor selectivity by targeting proton-coupled folate transporter (PCFT), which is more selective to PCFT than the commonly used anti-folate drug Pemetrexed (HY-10820). Antifolate C2 blocks the biosynthesis of deoxypurine nucleotides by inhibiting glycinamide ribonucleotide formyltransferase (GARFTase), ultimately inhibiting the proliferation of tumor cells. Antifolate C2 can be used in studies of NS-NSCLC, especially in patients who do not respond well to Pemetrexed .

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].

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