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

HK2-IN-4 是一种选择性己糖激酶 2 (HK2) 抑制剂，IC50 值为 0.79 μM，Kd 值为 0.41 μM。HK2-IN-4 可阻断 HK2 与电压依赖性阴离子通道 1 (VDAC1) 之间的相互作用。HK2-IN-4 可降低癌细胞内的乳酸和 ATP 水平。HK2-IN-4 可诱导癌细胞产生凋亡 (apoptosis) 标志物，包括 p-AMPK/AMPK 比值和 Bax 水平升高，以及 Bcl2 水平降低。HK2-IN-4 可抑制高表达 HK2 的癌细胞的增殖。HK2-IN-4 可用于结直肠癌、非小细胞肺癌的相关研究。

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HK2-IN-4

HK2-IN-4 Chemical Structure

CAS No. : 2748366-80-3

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HK2-IN-4 相关抗体

Top Publications Citing Use of Products

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VDAC1 VDAC2 VDAC3

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

HK2-IN-4 (Compound 106) (5 μM; 30 min) 可强效且选择性地抑制重组 HK2 酶活性，其 IC50 为 0.79 μM，对 HK1、HK3 和 HK4 的 IC50 值分别为 78.47 μM、60.86 μM 和 46.14 μM[1]。
HK2-IN-4 (10-100 μM; 24-72 h) 可选择性抑制高表达 HK2 的结直肠癌细胞 (SW480、LOVO、HCT116) 的活力，在缺氧条件下 72 h IC50 值低至 5.00 μM；与常氧条件相比，其在缺氧条件下的功效增强，且细胞毒性依赖于 HK2 的表达[1]。
HK2-IN-4 (0-40 μM; 6 h) 可在缺氧条件下以剂量依赖的方式降低 HCT116 和 SW480 细胞中的线粒体 HK2 水平[1]。
HK2-IN-4 (50 μM; 7 h) 处理可显著降低 SW480 细胞中 HK2 与 VDAC1 的共定位水平，破坏 HK2-VDAC1 的相互作用[1]。
HK2-IN-4 (50-100 μM; 2 h) 可抑制缺氧环境下 SW480 和 HCT116 WT 细胞的糖酵解能力，但对 HK2 KO 细胞无此作用，糖酵解抑制作用具有 HK2 依赖性[1]。
HK2-IN-4 (2.5-20 μM; 12-24 h) 以剂量依赖的方式降低缺氧状态下 SW480 结直肠癌细胞的乳酸和 ATP 水平，提高 p-AMPK/AMPK 比值，并调控 Bax/Bcl2 的表达水平，诱导生物能量应激与细胞凋亡[1]。

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

HK2-IN-4 相关抗体:

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.
分子量

391.46

Formula

C24H25NO4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HK2-IN-4 相关分类

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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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