Structure of VBIT 4
CAS No.: 2086257-77-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
VBIT-4 is a voltage-dependent anion channel (VDAC) oligomerization inhibitor.
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Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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Search for reports by entering the product batch number.
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CAS No. : | 2086257-77-2 |
Formula : | C21H23ClF3N3O3 |
M.W : | 457.87 |
SMILES Code : | O=C(CC(CO)N1CCN(CC1)C2=CC=C(C=C2)OC(F)(F)F)NC3=CC=C(C=C3)Cl |
MDL No. : | MFCD32663268 |
InChI Key : | QYSQXVAEFPWMEM-UHFFFAOYSA-N |
Pubchem ID : | 126697666 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H315-H319-H335 |
Precautionary Statements: | P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P313-P337+P313-P362-P403+P233-P405-P501 |
Description |
VBIT-4 inhibits the oligomerization of voltage-dependent anion channel 1 (VDAC1) with a binding affinity (Kd) of 17 μM. As an inhibitor of apoptosis, it has potential therapeutic applications in conditions associated with apoptosis, including neurodegenerative and cardiovascular diseases [1].
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In Vitro:
Cell Line
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Concentration | Treated Time | Description | References |
HeLa cells | 10µM | 1 hour | VBIT-4 suppressed the release of mtDNA caused by Phb1 knockdown | PMC9753472 |
J774A.1 cells | 10µM | 1 hour | VBIT-4 suppressed the release of mtDNA caused by Phb1 knockdown | PMC9753472 |
NSC-34 cells | 15 µM | 12 hours | VBIT-12 partially prevented the mutant SOD1-induced cell toxicity | PMC9456491 |
mouse lung endothelial cells | 5 µM | 36 hours | VBIT-4 prevented hyperglycemia-induced cell death and mitochondrial dysfunction, inhibiting spontaneous MPT pore opening and ROS generation. | PMC10376467 |
Rat cortical neurons | 10 μM | 6, 24, 48 hours | VBIT-4 prevented Aβ-induced VDAC1 overexpression and apoptotic cell death | PMC9795455 |
Endog−/− MEFs | 10 μM | VBIT-4 decreased cmtDNA levels and ISG expression | PMC8325171 | |
MDA231 | 10 μM | VBIT-4 induces VDAC1 monomerization and promotes PRKN-mediated polyubiquitination | PMC10392732 | |
MDA468 | 10 μM | VBIT-4 induces VDAC1 monomerization and promotes PRKN-mediated polyubiquitination | PMC10392732 |
In Vivo:
Species
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Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | MpJ- Faslpr lupus-prone mice | 10 μM | not specified | VBIT-4 ameliorated lupus-like symptoms, including the reduction of skin lesions, renal immune complex deposition, proteinuria, anti-dsDNA antibody, antinuclear antibody, IgG, and cell-free mtDNA levels | PMC8325171 | |
Mice | SOD1G93A mutant mice | Intraperitoneal injection | 26 mg/kg | Every other day for 12 weeks | VBIT-12 significantly improved muscle endurance in SOD1G93A mutant mice | PMC9456491 |
C57BL/6 mice | DSS-induced colitis model | Drinking water | 20 mg/kg | From day 2 or day 5 until day 14 | VBIT-12 significantly alleviated DSS-induced colitis pathology, inhibited inflammatory cell infiltration, apoptosis, mtDNA release, and NLRP3 inflammasome activation, and reduced the inflammatory response | PMC8821898 |
Mice | 5 × FAD mouse model | Drinking water | 20 mg/kg | Twice a week for 5 months | VBIT-4 prevented cognitive decline, neuronal loss, neuroinflammation, and neuro-metabolic dysfunctions | PMC9795455 |
Tags: VBIT 4 | VDAC1 inhibitor | Voltage-Dependent Anion Channel 1 | Voltage Dependent Anion Channel 1 | apoptosis | mitochondrial dysfunction | outer mitochondrial membrane | adenine nucleotide translocator | mitochondrial bioenergetics | BAX | BCL-2 | cytochrome c | caspase cascade | 2086257-77-2
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