2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Apoptosis Epigenetics PI3K/Akt/mTOR
  3. Hexokinase VDAC Apoptosis AMPK Bcl-2 Family
  4. HK2-IN-4

HK2-IN-4 is a selective hexokinase 2 (HK2) inhibitor with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. HK2-IN-4 blocks the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1). HK2-IN-4 reduces lactate and ATP levels in cancer cells. HK2-IN-4 induces the production of apoptosis (apoptosis) markers in cancer cells, including increased p-AMPK/AMPK ratio and Bax levels, as well as decreased Bcl2 levels. HK2-IN-4 inhibits the proliferation of cancer cells with high HK2 expression. HK2-IN-4 can be used in research related to colorectal cancer and non-small cell lung cancer.

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HK2-IN-4

HK2-IN-4 Chemical Structure

CAS No. : 2748366-80-3

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HK2-IN-4 Related Antibodies

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Description

HK2-IN-4 is a selective hexokinase 2 (HK2) inhibitor with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. HK2-IN-4 blocks the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1). HK2-IN-4 reduces lactate and ATP levels in cancer cells. HK2-IN-4 induces the production of apoptosis (apoptosis) markers in cancer cells, including increased p-AMPK/AMPK ratio and Bax levels, as well as decreased Bcl2 levels. HK2-IN-4 inhibits the proliferation of cancer cells with high HK2 expression. HK2-IN-4 can be used in research related to colorectal cancer and non-small cell lung cancer[1].

IC50 & Target[1]

VDAC1

 

In Vitro

HK2-IN-4 (Compound 106) (5 μM; 30 min) potently and selectively inhibits the activity of recombinant HK2 enzyme, with an IC50 of 0.79 μM, while its IC50 values against HK1, HK3 and HK4 are 78.47 μM, 60.86 μM and 46.14 μM, respectively[1].
HK2-IN-4 (10-100 μM; 24-72 h) selectively inhibits the viability of colorectal cancer cells with high HK2 expression (SW480, LOVO, HCT116), with an IC50 value as low as 5.00 μM after 72 h under hypoxic conditions; compared with normoxic conditions, its efficacy is enhanced under hypoxic conditions, and its cytotoxicity depends on HK2 expression[1].
HK2-IN-4 (0-40 μM; 6 h) reduces mitochondrial HK2 levels in HCT116 and SW480 cells in a dose-dependent manner under hypoxic conditions[1].
Treatment with HK2-IN-4 (50 μM; 7 h) significantly reduces the colocalization level of HK2 and VDAC1 in SW480 cells and disrupts the HK2-VDAC1 interaction[1].
HK2-IN-4 (50-100 μM; 2 h) inhibits glycolysis in SW480 and HCT116 WT cells under hypoxic conditions, but exerts no such effect on HK2 KO cells, indicating that its glycolysis-inhibiting effect is HK2-dependent[1].
HK2-IN-4 (2.5-20 μM; 12-24 h) reduces lactate and ATP levels in hypoxic SW480 colorectal cancer cells in a dose-dependent manner, increases the p-AMPK/AMPK ratio, regulates the expression levels of Bax/Bcl2, and induces bioenergetic stress and apoptosis[1].

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

HK2-IN-4 Related Antibodies

Cell Viability Assay[1]

Cell Line: human cancer cell lines (6 NSCLC cell lines: NCI-H1299, NCI-H1975, SK-LU-1, A549, NCI-H2122, NCI-H460; 3 colorectal cancer cell lines: HCT116, LOVO, SW480; HK2 knockout and wild-type SW480, HCT116 cells)
Concentration: 10 μM, 100 μM (24 h treatment for NCI-H1975)
Incubation Time: 24 h (NCI-H1975); 72 h (IC50 determination under normoxia and hypoxia); 48 h (CoCl2 pre-treatment for hypoxia induction)
Result: Reduced NCI-H1975 cell viability by 4.66% at 10 μM and 93.19% at 100 μM after 24 h.
Exhibited 72 h IC50 values under hypoxia of 59.95 μM (NCI-H1299), 49.37 μM (NCI-H1975), 48.82 μM (NCI-H460), 48.39 μM (NCI-H2122), 49.67 μM (SK-LU-1), 44.8 μM (A549), 16.17 μM (HCT116), 11.11 μM (LOVO), and 5 μM (SW480).
Showed significantly lower IC50 values under hypoxia compared to normoxia: 16.17 μM vs.
43.33 μM (HCT116), 11.11 μM vs.
27.14 μM (LOVO), 5 μM vs.
14.33 μM (SW480).
Showed IC50 ratio of HK2 KO vs.
WT cells of 8.02 (HCT116) and 9.36 (SW480), indicating HK2 KO significantly rescued cells from cytotoxicity.

Western Blot Analysis[1]

Cell Line: HCT116 and SW480 colorectal cancer cells (under hypoxia)
Concentration: 20 μM, 30 μM, 40 μM (HCT116); 10 μM, 20 μM, 40 μM (SW480)
Incubation Time: 6 h
Result: Decreased mitochondrial HK2 levels in a dose-dependent manner in both HCT116 and SW480 cells.

Immunofluorescence[1]

Cell Line: SW480 cells co-transfected with HK2-GFP and VDAC1-mCherry plasmids
Concentration: 50 μM
Incubation Time: 7 h (imaging every 15 min)
Result: Reduced the colocalization coefficient of HK2-GFP and VDAC1-mCherry significantly from the 17th time point (4 h post-treatment) onward, with increasing significance at later time points.

Western Blot Analysis[1]

Cell Line: SW480 colorectal cancer cells under hypoxia
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Increased the p-AMPK/AMPK ratio, elevated Bax levels, and decreased Bcl2 levels in a dose-dependent manner.
Molecular Weight

391.46

Formula

C24H25NO4
CAS No.
SMILES

O=C(C1=CC=CC=C1)OC(C2)C=C[C@]3(C2O4)C5=C4C(OC)=CC=C5CN(C)CC3
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Room temperature in continental US; may vary elsewhere.
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HK2-IN-4 Related Classifications

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  • 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:

HK2-IN-42748366-80-3HexokinaseVDACApoptosisAMPKBcl-2 FamilyVoltage-dependent anion channel AMP-activated protein kinaseHK2 inhibitorSW480 cellsnon-small cell lung cancerHCT116 cellsLOVO cellscolorectal cancer and non-small cell lung cancerInhibitorinhibitorinhibit

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