VDAC Inhibitor

Erastin is a ferroptosis inducer. Erastin exhibits the mechanism of ferroptosis induction related to ROS and iron-dependent signaling. Erastin inhibits voltage-dependent anion channels (VDAC2/VDAC3) and accelerates oxidation, leading to the accumulation of endogenous reactive oxygen species. Erastin also disrupts mitochondrial permeability transition pore (mPTP) with anti-tumor activity. Furthermore, Erastin can block the uptake of cystine mediated by SLC7A11 and also spares UMRC6-EV and -C91A cells from disulfidptosis under glucose starvation.

VBIT-4 is an inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization with a binding affinity (K_d) of 17 μM. VBIT-4, as an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders, such as neurodegenerative and cardiovascular diseases.

DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research.

VBIT-12 is a potent VDAC1 inhibitor. VBIT-12 directly interacts with VDAC1 and prevents VDAC1 oligomerization, and thus inhibits apoptotic action of VDAC1.

NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.

HK2-IN-4 is a selective hexokinase 2 (HK2) inhibitor with an IC₅₀ value of 0.79 μM and a K_d 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.

Cyanidin-3-O-arabinoside is a p38 MAPK phosphorylation inhibitor. Cyanidin-3-O-arabinoside reduces the expression of VDAC1, inhibits mtROS accumulation, reverses cellular senescence, blocks excessive mitochondrial calcium influx, reduces the formation of mitochondria-associated endoplasmic reticulum membranes, and suppresses the VDAC1-IP3R1 interaction. Cyanidin-3-O-arabinoside activates hair follicle stem cell proliferation and improves the condition of slowed hair growth. Cyanidin-3-O-arabinoside is applicable to research related to colon cancer and androgenetic alopecia.

WEHI-9625 is a tricyclic sulfone, first-in-class 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. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX.

AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (K_d=15.4 μM). AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis. AKOS-22 protects against mitochondrial dysfunction.

VBIT-3 is an inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization with a binding affinity (K_d) of 31.3 μM. VBIT-3, as an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders, such as neurodegenerative and cardiovascular diseases.

Ferroptosis-IN-20 (Compound 34a) is a Ferroptosis inhibitor (EC₅₀: 24.2 nM) targeting voltage-dependent anion channel (VDAC). Ferroptosis-IN-20 inhibits VDAC oligomerization and lipid peroxidation. Ferroptosis-IN-20 reduces content of ROS, attenuates TFR1-mediated iron uptake, inhibits Fe²⁺ level and restores glutathione (GSH) level. Ferroptosis-IN-20 alleviates Folic acid (HY-16637)-induced acute kidney injury (AKI).

DIDS is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research.

NSC 15364 (Standard) is the analytical standard of NSC 15364 (HY-108937). This product is intended for research and analytical applications. NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.