2. Metabolic Enzyme/Protease Apoptosis Cell Cycle/DNA Damage
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD) Apoptosis DNA/RNA Synthesis
  4. TH9028

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.

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

TH9028

TH9028 Chemical Structure

CAS No. : 2379556-15-5

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TH9028 Related Antibodies

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Description

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[1][2].

IC50 & Target

13169

11 nM (IC50)

13168

7.97 nM (IC50)

13170

27 nM (IC50)

13171

0.5 nM (IC50)

In Vitro

TH9028 (10-10 to 10-4 M; 96 h) reduces HL-60 AML cell viability with high potency, corresponding to a pEC50 of 7.6 after 96 hours of incubation[2].
TH9028 (50 nM; 24 h) reduces DNA replication fork speed in HL-60 and THP-1 AML cells at a concentration of 50 nM after 24 hours of incubation[2].
TH9028 (10-10 to 10-4 M; 96 h) induced cell viability loss in HL-60 AML, THP-1 AML, and SW620 colorectal cancer cells, which was fully rescued by thymidine supplementation, confirming thymidine depletion as the mechanism of action[2].

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

TH9028 Related Antibodies

Cell Viability Assay[2]

Cell Line: HL-60 AML cell line, THP-1 AML cell line, SW620 colorectal cancer cell line
Concentration: 0.1, 1, 10, 100 nM, 1, 10, 10 μM
Incubation Time: 96 h
Result: Induced viability defects in HL-60, THP-1, and SW620 cells, which were completely rescued by thymidine supplementation.
In Vivo
Animal Model: NOG mice[2]
Dosage: 30 mg/kg
Administration: subcutaneous; twice daily
Result: Extended median survival.
Reached peak plasma concentrations post-subcutaneous dosing.
Increased MTHFD2 protein thermal stability in tumor tissue (CETSA).
Caused no significant weight loss or hematological toxicity at therapeutic doses.
Molecular Weight

458.39

Formula

C16H18N12O5
CAS No.
SMILES

NC(NC(N)=NC1=O)=C1NC(NC2=CN=C(C(N[C@H](C(O)=O)CCC3=NN=NN3)=O)C=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TH9028 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:

TH90282379556-15-5TH 9028TH-9028Methylenetetrahydrofolate Dehydrogenase (MTHFD)ApoptosisDNA/RNA SynthesisdUTPaseMTHFD1HL-60 AML cellsATRTHP-1 AML cellsT-ALL cellsMTHFD2SW620 colorectal cancer cellsMTHFD2Lacute myeloid leukaemiaInhibitorinhibitorinhibit

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