VDAC (Voltage-dependent anion channel)

Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.

RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.

WEHI-9625 is a tricyclic sulfone small molecule inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK, but is completely inactive against both human BAK and the closely related apoptosis effector BAX.

NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.

DIDS sodium salt is a potent inhibitor of voltage-dependent anion channels (VDAC1) and also targets the ABCA1 transporter. This compound effectively disrupts RAD51-mediated homologous pairing and strand exchange reactions, making it valuable for studying DNA repair mechanisms. Additionally, DIDS is known to inhibit anion exchange and interfere with caspase-3 and -9 activation, facilitating its application in cancer research and apoptosis studies.

NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor that functions as a direct binder to VDAC1, VDAC2, and VDAC3. It demonstrates an IC50 of 1.02 μM for inhibiting ERAD and a Kd of 3.13 μM for binding human VDAC1. By disrupting cellular calcium homeostasis and enhancing VDAC1-IP3R coupling, NCATS-SM0225 activates the PERK pathway and selectively induces apoptosis in cancer cells. This reagent is valuable for investigating cancer biology, particularly in melanoma, as well as exploring the underlying mechanisms of ERAD and calcium homeostasis regulation.

DIDS is a RAD51 inhibitor that disrupts RAD51-mediated homologous pairing and strand exchange reactions, thereby impacting DNA repair processes. In addition to its primary function, DIDS also inhibits ABCA1 and VDAC1, affecting anion exchange and binding to red blood cell membranes. Furthermore, it has been shown to inhibit the activation of caspase-3 and -9, making it a valuable tool for cancer research applications.

VBIT-4 is a selective inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization, exhibiting a binding affinity of 17 μM. This compound is recognized for its potential to inhibit apoptosis, making it suitable for therapeutic investigations in apoptosis-related conditions, including neurodegenerative and cardiovascular diseases. Researchers may utilize VBIT-4 to explore its effects on cell survival and disease progression in relevant biological models.

VBIT-12 is a potent inhibitor of Voltage-Dependent Anion Channel 1 (VDAC1) that functions by directly binding to the channel and preventing its oligomerization. This interaction effectively inhibits the pro-apoptotic actions mediated by VDAC1. VBIT-12 is valuable in studies aimed at elucidating the role of VDAC1 in apoptosis and mitochondrial function, making it a key reagent for research in cell death pathways and mitochondrial-related diseases.

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.

AKOS-22 is a selective inhibitor of the mitochondrial protein VDAC1 (voltage-dependent anion channel 1), exhibiting an affinity with a Kd of 15.4 μM. This compound prevents VDAC1 oligomerization and inhibits apoptosis, thereby offering protection against mitochondrial dysfunction. AKOS-22 serves as a valuable tool in research focused on mitochondrial biology and related pathways in disease.

SW016789 is a potent inducer targeting the voltage-dependent anion channel 1 (VDAC1). It effectively promotes insulin hypersecretion and enhances Ca2+ influx in pancreatic β-cells, leading to a transient endoplasmic reticulum (ER) stress response without inducing cell death. This compound exhibits reversible and non-apoptotic properties, making it a valuable tool for exploring β-cell dysfunction associated with type 2 diabetes mellitus (T2DM).

VBIT-3 is a selective inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization, exhibiting a binding affinity (Kd) of 31.3 μM. It functions as an apoptosis inhibitor, providing potential therapeutic applications in managing apoptosis-related disorders, including neurodegenerative and cardiovascular diseases. This reagent is valuable for research focused on understanding the biochemical pathways of apoptosis and exploring treatment strategies for related conditions.

Tuvatexib is an antineoplastic agent that inhibits cancer cell proliferation by targeting specific pathways involved in tumor growth. It exhibits significant cytotoxic activity against various cancer cell lines, making it a valuable tool for cancer research. Applications include the study of cancer cell metabolism and the evaluation of combination therapies in preclinical models.