2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. IACS-4619

IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC50=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target.

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

IACS-4619

IACS-4619 Chemical Structure

CAS No. : 1884209-98-6

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Description

IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC50=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target[1].

In Vitro

IACS-4619 shows good MDCK cell permeability, high human plasma protein binding, high liver microsomal turnover, and good plasma stability in rats and humans[1].
IACS-4619 (up to 50 μM) does not confer a robust anti-proliferative phenotype in human cancer cell lines (U2OS, SaOS2, etc.) and normal cell lines (WI38, BJ, etc.)[1].

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

IACS-4619 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human cancer cell lines (U2OS, SaOS2, SW480, HCT116, MDAMB231, HeLa, UOK262, 293T, A549, H460, H358) and normal cell lines (WI38, BJ, hMEC, MRC5)
Concentration: 0-50 μM
Incubation Time: /
Result: Did not exhibit significant antiproliferative effects or cytotoxicity in any tested cell lines, even with prolonged treatment, and cell lines with high intrinsic ROS levels tolerated the compound well.
Molecular Weight

195.27

Formula

C10H17N3O
CAS No.
SMILES

N=1C=C(C(=NC1N)OCC(C)(C)C)C
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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IACS-4619 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:

IACS-46191884209-98-6IACS4619IACS 4619DNA/RNA Synthesisliver microsomal turnoverhuman plasma protein bindingintact cellsMTH1recombinant MTH1plasma stabilitynormal cell linesMTH1-overexpressing cell lysateshuman cancer cell linesMDCK cell permeabilityInhibitorinhibitorinhibit

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