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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
9 Results for "
MTHFD1 Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (9)
9 Results for "MTHFD1 Inhibitors" in MCE Product Catalog:
21
21 Cited Publications
Research Areas:
DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile .
1
1 Cited Publications
Research Areas:
TH9619 is a potent inhibitor of dehydrogenase and cyclohydrolase activities in both MTHFD1 and MTHFD2 with a IC50 value of 47 nM, and selectively kills cancer cells. TH9619 induces apoptosis by blocking the S phase. TH9619 has antitumor activity .
Cat. No.: HY-155219
CAS No.: 2379556-15-5
Research Areas:
TH9028 is an inhibitor of MTHFD1, MTHFD2 and MTHFD2L, with IC50 values of 0.5 nM, 11 nM and 27 nM, respectively. TH9028 reduces replication fork speed, induces replication stress, triggers S-phase arrest, initiates apoptosis, impairs thymidine production, and causes erroneous uracil incorporation into DNA. TH9028 can be used in research related to acute myeloid leukemia .
Cat. No.: HY-149825
Research Areas:
MTHFD2-IN-1 is a MTHFD2 inhibitor with selectivity for MTHFD2 binding over MTHFD1. MTHFD2-IN-1 binds to the substrate-binding site of MTHFD2 and interacts with Arg43, Asn87, Lys88, Gln132, Gly310 and Tyr84. MTHFD2-IN-1 can be used in cancer-related research .
Cat. No.: HY-149826
Research Areas:
MTHFD2-IN-2 is a selective MTHFD2 inhibitor with poor binding to MTHFD1. MTHFD2-IN-2 binds to the MTHFD2 substrate binding site, forming π-π stacking with Tyr84, hydrogen bond/salt-bridge contacts with Arg43 and Asn87, and lipophilic interactions with Ile276. MTHFD2-IN-2 exhibits predicted anticancer activity. MTHFD2-IN-2 can be used for the research of cancer .
Cat. No.: HY-149828
Research Areas:
MTHFD2-IN-4 is a selective MTHFD2 inhibitor. MTHFD2-IN-4 binds to the substrate-binding site of MTHFD2, interacts with Arg43, Tyr84, Asn87, Lys88, Gln132 and Gly310, and does not interact with the key selective residues of MTHFD1. MTHFD2-IN-4 exerts its function through selective inhibition of MTHFD2 in cancer cells. MTHFD2-IN-4 can be used in cancer-related research .
Cat. No.: HY-149828A
Research Areas:
MTHFD2-IN-4 sodium is a selective MTHFD2 inhibitor. MTHFD2-IN-4 sodium binds to the substrate-binding site of MTHFD2, interacts with Arg43, Tyr84, Asn87, Lys88, Gln132 and Gly310, and does not interact with the key selective residues of MTHFD1. MTHFD2-IN-4 sodium exerts its function through selective inhibition of MTHFD2 in cancer cells. MTHFD2-IN-4 sodium can be used in cancer-related research .
Cat. No.: HY-182356
CAS No.: 3125953-25-2
Research Areas:
MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models .
Cat. No.: HY-148014
CAS No.: 1415648-20-2
TH7299 is a TbFolD inhibitor with antiparasitic activity. TH7299 binds the tetrahydrofolate-binding pocket of MTHFD2, and inhibits MTHFD2L and the dehydrogenase/cyclohydrolase domain of MTHFD1. TH7299 reduces cancer cells viability, induces apoptosis, DNA damage. TH7299 can be used for the researches of african trypanosomiasis and acute myeloid leukemia.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
