An orally bioavailable inhibitor of mitochondrial complex I
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IACS-010759

Item No. 25867

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(methylsulfonyl)-1-[3-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-1,2,4-triazol-1-yl]methyl]phenyl]-piperidine
CAS Number
1570496-34-2
Molecular Formula
C25H25F3N6O4S
Formula Weight
562.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.1 mg/mlDMSO: 0.2 mg/mlEthanol: Slightly soluble
λmax
244 nm
SMILES
CS(C1CCN(C2=CC=CC(CN3C(C)=NC(C4=NC(C5=CC=C(OC(F)(F)F)C=C5)=NO4)=N3)=C2)CC1)(=O)=O
InChi Code
InChI=1S/C25H25F3N6O4S/c1-16-29-23(24-30-22(32-38-24)18-6-8-20(9-7-18)37-25(26,27)28)31-34(16)15-17-4-3-5-19(14-17)33-12-10-21(11-13-33)39(2,35)36/h3-9,14,21H,10-13,15H2,1-2H3
InChi Key
HWJWNWZJUYCGKV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    IACS-010759 is an orally bioavailable inhibitor of complex I of the mitochondrial electron transport chain.1,2 It inhibits the ubiquinone reduction activity of isolated murine mitochondrial complex I when used at a concentration of 60 nM.1 IACS-010759 (100 nM) reduces basal and spare respiratory capacities and increases glycolytic flux in primary chronic lymphocytic leukemia (CLL) cells.2 It also induces apoptosis in CLL cells grown under low glucose conditions or when administered in combination with 2-deoxy-D-glucose (Item No. 14325). IACS-010759 (5 and 10 mg/ml) induces tumor regression in a glycolysis-deficient NB1 mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Molina, J.R., Sun, Y., Protopopova, M., et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat. Med. 24(7), 1036-1046 (2018).

    2. Vangapandu, H.V., Alston, B., Morse, J., et al. Biological and metabolic effects of IACS-010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells. Oncotarget 9(38), 24980-24991 (2018).