Scientific Reviews
Product Guides
Blogs
Topics
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
23 Results for "
MTHFD2
" in MedChemExpress (MCE) Product Catalog:
Products (23)
23 Results for "MTHFD2" in MCE Product Catalog:
21
21 Publications Verification
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 .
9
9 Cited Publications
Research Areas:
LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC50 values of 96 nM and 663 nM, respectively and a Ki of 18 nM for MTHFD1 [2] .
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 [2].
Research Areas:
DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration (IC50=1.6 μM, Ki=1.23 μM). DS44960156 specifically binds to the active site of MTHFD2, disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD +/NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers [2] .
Cat. No.: HY-170361
CAS No.: 3068001-31-7
Research Areas:
MTHFD2-IN-5 (Compound 16e) is a selective MTHFD2 inhibitor with an IC50 of 66 nM. MTHFD2-IN-5 selectively inhibits MTHFD2. MTHFD2-IN-5 exhibits anticancer activity against acute myeloid leukemia. MTHFD2-IN-5 acts synergistically with Alimta to inhibit the proliferation of acute myeloid leukemia cells .
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 [2].
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-172910
CAS No.: 3077252-76-4
Research Areas:
MTHFD2-IN-6 is an orally active selective inhibitor of MTHFD2, with a human IC50 of 1.46 μM. MTHFD2-IN-6 binds directly to MTHFD2, selectively inhibits cancer cell proliferation, promotes ROS accumulation in cancer cells, and induces cancer cell cycle arrest and apoptosis. MTHFD2-IN-6 inhibits tumor growth in Mus musculus xenograft models. MTHFD2-IN-6 can be used for lung cancer research .
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-149827
Research Areas:
MTHFD2-IN-3 is a selective inhibitor of MTHFD2. MTHFD2-IN-3 binds to the substrate-binding site of MTHFD2, forms hydrogen bonds with Arg43, Lys88, Gln132, Asn87 and Gly310, and undergoes π-π stacking with Tyr84. MTHFD2-IN-3 can be used in cancer-related research .
Cat. No.: HY-RS08776
Target:
Research Areas:
MTHFD2 Human Pre-designed siRNA Set A contains three designed siRNAs for MTHFD2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-RS23082
Target:
Research Areas:
Mthfd2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Mthfd2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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-RS16648
Target:
Research Areas:
Mthfd2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mthfd2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-182355
Research Areas:
MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research .
Cat. No.: HY-183364
Target:
Methylenetetrahydrofolate Dehydrogenase (MTHFD) Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism
Research Areas:
MTHFD2-IN-8 is a selective MTHFD2 inhibitor with an IC50 of 0.066 μM. MTHFD2-IN-8 directly binds to intracellular mitochondrially localized protein MTHFD2 and accumulates selectively in tumor mitochondria. MTHFD2-IN-8 increases intracellular ROS levels, induces mitochondrial membrane potential depolarization, arrests cell cycle at G0/G1 phase, promotes apoptosis in cancer cells. MTHFD2-IN-8 inhibits tumor growth in a mouse colon cancer graft model .
Cat. No.: HY-RS08777
Target:
Research Areas:
MTHFD2L Human Pre-designed siRNA Set A contains three designed siRNAs for MTHFD2L gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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 .
- 1
- 2
-
-
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
