Product Data Sheet

HK2-IN-4

Catalog No. A68922

main product photo
HK2-IN-4 is a selective inhibitor of hexokinase 2 (HK2) with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. It disrupts the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1), leading to reduced lactate and ATP levels in cancer cells. Additionally, HK2-IN-4 promotes the activation of apoptosis pathways, evidenced by an increased p-AMPK/AMPK ratio and elevated Bax levels, alongside decreased Bcl2 levels. This compound is applicable in research focusing on colorectal cancer and non-small cell lung cancer, particularly in models with high HK2 expression.
Chemical Information
Catalog NumA68922
M. Wt391.46
FormulaC24H25NO4
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2748366-80-3
Synonyms
SMILESO=C(C1=CC=CC=C1)OC(C2)C=C[C@]3(C2O4)C5=C4C(OC)=CC=C5CN(C)CC3
Biological Activity
DescriptionHK2-IN-4 is a selective inhibitor of hexokinase 2 (HK2) with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. It disrupts the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1), leading to reduced lactate and ATP levels in cancer cells. Additionally, HK2-IN-4 promotes the activation of apoptosis pathways, evidenced by an increased p-AMPK/AMPK ratio and elevated Bax levels, alongside decreased Bcl2 levels. This compound is applicable in research focusing on colorectal cancer and non-small cell lung cancer, particularly in models with high HK2 expression.
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