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VDAC

Voltage-dependent anion channels, or mitochondrial porins, are a class of porin ion channel located on the outer mitochondrial membrane. There is debate as to whether or not this channel is expressed in the cell surface membrane. This major protein of the outer mitochondrial membrane of eukaryotes forms a voltage-dependent anion-selective channel (VDAC) that behaves as a general diffusion pore for small hydrophilic molecules. The channel adopts an open conformation at low or zero membrane potential and a closed conformation at potentials above 30–40 mV. VDAC facilitates the exchange of ions and molecules between mitochondria and cytosol and is regulated by the interactions with other proteins and small molecules.

Erastin
T1765571203-78-6
Erastin is an iron death activator that acts on the mitochondrial VDAC in a ROS- and iron-dependent manner. Erastin has anti-tumor activity and acts selectively on tumor cells with RAS-carcinogenic mutations.
  • $41
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VBIT-4
T132872086257-77-2
VBIT-4 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 17 μM). VBIT-4 can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).
  • $68
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DIDS sodium salt
MDL101114ZA
T1897567483-13-0In house
DIDS sodium salt (MDL101114ZA) is a small molecule inhibitor that acts as a dual-target inhibitor of both ABCA1 and VDAC1, suppressing RAD51-mediated homologous recombination. This compound inhibits anion exchange and Caspase-3/-9 activation, and is used in cancer research.
  • $33
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VBIT-12
T82152089227-65-4
VBIT-12 is a potent inhibitor of VDAC1.
  • $42
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Tuvatexib
T680182055404-90-3In house
Tuvatexib is a small molecule VDAC/HK2 dual modulator.
  • $82
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NSC 15364
NSC15364, 1,3-Bis(4-aminophenyl)urea
T35724550-72-5
NSC 15364 (1,3-Bis(4-aminophenyl)urea) can be used for screening of ALR inhibitors by detection of hydrogen peroxide production Measured in Biochemical System.
  • $32
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VBIT-3
T132862088463-66-3
VBIT-3 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 31.3 μM). VBIT-3 also is an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).
  • $1,520
6-8 weeks
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WEHI-9625
T133382595314-46-6
WEHI-9625 is a tricyclic sulfone small molecule apoptosis inhibitor (EC50: 69 nM).
  • $1,970
10-14 weeks
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DIDS
T2069453005-05-3
DIDS, an anion exchange inhibitor, acts by blocking reversibly and later irreversibly, exchangers such as chloride-bicarbonate exchanger. It is also a RAD51 inhibitor.
  • $1,820
10-14 weeks
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TargetMol | Citations Cited
AKOS-22
T14150878983-38-1
AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (Kd=15.4 μM). AKOS-22 protects against mitochondrial dysfunction[1]. AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis.
  • $627
35 days
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Ferroptosis-IN-20
T210683
Ferroptosis-IN-20 (Compound 34a) is an inhibitor of ferroptosis targeting voltage-dependent anion channels (VDAC) with an EC50 of 24.2 nM. It prevents VDAC oligomerization and lipid peroxidation. Additionally, Ferroptosis-IN-20 reduces ROS levels, diminishes TFR1-mediated iron uptake, inhibits Fe2+ levels, and restores glutathione (GSH) levels. It also alleviates acute kidney injury (AKI) caused by folic acid.
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NCATS-SM0225
T2178751212623-02-3
NCATS-SM0225 is an ER-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2, and VDAC3. It has an IC50 of 1.02 μM for ERAD inhibition and a Kd of 3.13 μM for binding to human VDAC1. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling, and activates PERK. The compound selectively kills cancer cells and has shown tumor growth inhibition in melanoma xenograft models. It is useful for research into various cancers, including melanoma, as well as studies on ERAD and calcium homeostasis regulatory mechanisms.
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10-14 weeks
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SW016789
T210734292613-04-8
SW016789 is a potent high-secretion inducer targeting VDAC1, which directly stimulates insulin secretion and calcium ion influx in β cells. It transiently induces endoplasmic reticulum stress (ER stress) without causing β cell death. The response it triggers is reversible and non-apoptotic, making SW016789 useful for studying β cell dysfunction in type 2 diabetes (T2DM).
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10-14 weeks
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HK2-IN-4
T2186712748366-80-3
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. It disrupts the interaction between HK2 and the voltage-dependent anion channel 1 (VDAC1). HK2-IN-4 reduces lactate and ATP levels in cancer cells and induces apoptosis markers, including increased p-AMPK/AMPK ratio and Bax levels, along with decreased Bcl2 levels. Additionally, HK2-IN-4 inhibits the proliferation of cancer cells with high HK2 expression and can be utilized in research related to colorectal cancer and non-small cell lung cancer.
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10-14 weeks
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