2. Metabolic Enzyme/Protease Anti-infection Apoptosis Cell Cycle/DNA Damage
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD) Parasite Apoptosis DNA/RNA Synthesis
  4. TH7299

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.

For research use only. We do not sell to patients.

TH7299

TH7299 Chemical Structure

CAS No. : 1415648-20-2

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TH7299 Related Antibodies

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

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.[1][2]

In Vitro

TH7299 (Compound 2) (0-100 μM; 5 minutes) inhibits recombinant Trypanosoma brucei FolD dehydrogenase activity with a Ki of 1.1 ± 0.8 μM and an IC50 of 2.2 μM[1].
TH7299 (72 h) inhibits in vitro growth of bloodstream-form Trypanosoma brucei brucei with an IC50 of 49 ± 3.2 μM[1].
TH7299 potently inhibits the enzymatic activity of recombinant human MTHFD2 with an IC50 of 254 nM, and also inhibits the related folate enzymes MTHFD2L (IC50 = 126 nM)and MTHFD1-(DC) (IC50 = 89 nM)[2].
TH7299 (96 h) reduces the viability of HL-60 AML cells with an EC50 of 1110 nM[2].
TH7299 (30 μM; 2 h) engages with and stabilizes MTHFD2 in intact HL-60 AML cells[2].
TH7299 (10 μM; 24 h) reduces replication fork speed by ~50% in THP-1 AML cells, and this effect is completely rescued by co-treatment with 50 μM Thymidine (HY-N1150)[2].
TH7299 (3 μM; 24-48 h) induces time-dependent DNA damage (γH2AX positivity) primarily in S-phase and G2/M-phase HL-60 AML cells[2].
TH7299 (10-8-10-5 M; 96 h) dose-dependently induces late-stage apoptosis in HL-60 AML cells, with minimal apoptosis induction in nontumorigenic LCL-889 cells[2].
TH7299 (10-9-10-4 M; 96 h)-induced viability loss in HL-60 AML, THP-1 AML, and SW620 colorectal cancer cells is completely rescued by co-treatment with 50 μM Thymidine[2].
TH7299 (10 μM; 24 h) increases replication origin firing in THP-1 AML cells[2].
TH7299 (10 μM; 24 h) increases p-CHK1 and p-RPA32 levels in THP-1 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TH7299 Related Antibodies

Apoptosis Analysis[2]

Cell Line: HL-60 AML cells, LCL-889 nontumorigenic lymphoblastoid cells
Concentration: 10-8-10-5 M
Incubation Time: 96 h
Result: Induced late-stage apoptosis (annexin-V+/PI+) in ~60% of HL-60 cells at the highest concentration tested.
Induced late-stage apoptosis in <20% of LCL-889 cells at equivalent concentrations.

Cell Viability Assay[2]

Cell Line: HL-60 AML cells, THP-1 AML cells, SW620 colorectal cancer cells
Concentration: 10-9-10-4 M
Incubation Time: 96 h
Result: Reduced viability of HL-60, THP-1, and SW620 cells, and this viability reduction was completely rescued by co-treatment with 50 μM Thymidine.

Western Blot Analysis[2]

Cell Line: THP-1 cells
Concentration: 10 μM
Incubation Time: 6， 24， 48, 72 h
Result: Incresaed p-CHK1 and p-RPA32 levels at 24 h.
Increased p-CDK levels at 24 and 48 h.
Increased p21 levels at 48 and 72 h.
Increased γH2AX levels at 48 h.
Molecular Weight

433.38

Formula

C17H19N7O7
CAS No.
SMILES

N(C(NC1=CC=C(C(N[C@@H](CCC(O)=O)C(O)=O)=O)C=C1)=O)C2=C(N)NC(N)=NC2=O
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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TH7299 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TH72991415648-20-2TH 7299TH-7299Methylenetetrahydrofolate Dehydrogenase (MTHFD)ParasiteApoptosisDNA/RNA SynthesisHL-60 AML cellsMTHFD1MTHFD2TbFolDNADP+Trypanosoma bruceiTHP-1 AML cellsT-ALL cellsMTHFD2Lacute myeloid leukemiaInhibitorinhibitorinhibit

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