2. Membrane Transporter/Ion Channel Apoptosis
  3. VDAC Bcl-2 Family Apoptosis
  4. WEHI-3773

WEHI-3773 is a VDAC2 ligand and apoptosis modulator. WEHI-3773 directly binds to the β7-β10 region of VDAC2 and disrupts its interaction with BAX and BAK. WEHI-3773 regulates BAX-mediated apoptosis in BAK-deficient cells by modulating conformational activation of BAX, mitochondrial redistribution, and cytochrome c release. WEHI-3773 overcomes Venetoclax (HY-15531) resistance, resensitizes leukemia cells carrying BAX mutations to BH3 mimetics, and enables long-term clonogenic survival of BAK-deficient cells treated with BH3 mimetics. WEHI-3773 is applicable to research related to acute myeloid leukemia.

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WEHI-3773

WEHI-3773 Chemical Structure

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Based on 1 publication(s) in Google Scholar

WEHI-3773 Related Antibodies

Top Publications Citing Use of Products

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VDAC1 VDAC2 VDAC3

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

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Description

WEHI-3773 is a VDAC2 ligand and apoptosis modulator. WEHI-3773 directly binds to the β7-β10 region of VDAC2 and disrupts its interaction with BAX and BAK. WEHI-3773 regulates BAX-mediated apoptosis in BAK-deficient cells by modulating conformational activation of BAX, mitochondrial redistribution, and cytochrome c release. WEHI-3773 overcomes Venetoclax (HY-15531) resistance, resensitizes leukemia cells carrying BAX mutations to BH3 mimetics, and enables long-term clonogenic survival of BAK-deficient cells treated with BH3 mimetics. WEHI-3773 is applicable to research related to acute myeloid leukemia[1][2].

IC50 & Target

VDAC2

 

Bax

 

Bak

 

In Vitro

WEHI-3773 inhibits BAX-mediated apoptosis in BAK-deficient cells by blocking the conformational activation, mitochondrial redistribution and cytochrome c release of BAX. In BAX-deficient cells, WEHI-3773 promotes BAK-mediated apoptosis by inducing the conformational activation of BAK, cytochrome c release and VDAC2 dissociation[1].
WEHI-3773 (0.1-10000 nM; pre-incubated for 2 h followed by co-incubation with BH3 mimetics for 22 h) dose-dependently enhances BAK-mediated apoptosis in Bax-/- Vdac2-/- mouse embryonic fibroblasts (MEFs) expressing VDAC2 or a chimeric VDAC protein containing the β7 to β10 region of VDAC2, but exerts no such effect in cells expressing VDAC1 or a chimeric protein lacking this region[1].
WEHI-3773 (200 nM; 48 h) enhances BH3 mimetic-induced cell death in BAX-/- MV4;11 acute myeloid leukemia (AML) cells and reverses venetoclax resistance caused by BAX deletion[1].
WEHI-3773 (200 nM; 48 h) enhances BH3 mimetic-induced cell death in venetoclax-resistant OCI-AML3 acute myeloid leukemia cells harboring BAX mutations, thereby overcoming acquired venetoclax resistance[1].
WEHI-3773 (80-10000 nM) dose-dependently promotes BAK conformational activation and cytochrome c release in BAK-/- HeLa cells treated with ABT-737 + S63845[2].
WEHI-3773 (200 nM; 48 h) restores the sensitivity of BAX-/- MV4;11 human acute myeloid leukemia (AML) cells to venetoclax, S63845, and their combination following 48 h of co-treatment[2].

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

WEHI-3773 Related Antibodies

Cell Viability Assay[1]

Cell Line: Bax-/- Vdac2-/- mouse embryonic fibroblasts (MEFs) expressing VDAC1/VDAC2 chimeric proteins, full-length VDAC1, or full-length VDAC2
Concentration: 0.1-10000 nM
Incubation Time: 2 h pre-incubation, followed by 22 h incubation with BH3 mimetics
Result: Reduced cell viability dose-dependently in cells expressing full-length VDAC2, VDAC1/2-a, or VDAC1/2-c chimeric proteins. Reduced viability in cells expressing VDAC1/2-d chimeric proteins, but to a lesser extent at higher concentrations. Had no effect on viability in cells expressing full-length VDAC1 or VDAC1/2-b chimeric proteins.

Cell Viability Assay[1]

Cell Line: BAX-/- MV4;11 human acute myeloid leukemia (AML) cells
Concentration: 200 nM
Incubation Time: 48 h
Result: Significantly sensitized cells to cell death induced by venetoclax, S63845, or the combination of venetoclax and S63845, with statistically significant reductions in cell viability observed across multiple concentrations of each BH3 mimetic treatment.

Cell Viability Assay[1]

Cell Line: BAX-mutant OCI-AML3 human acute myeloid leukemia (AML) cells resistant to venetoclax (BCL-2i R)
Concentration: 200 nM
Incubation Time: 48 h
Result: Significantly sensitized cells to cell death induced by venetoclax, S63845, or the combination of venetoclax and S63845, with statistically significant reductions in cell viability observed across multiple concentrations of each BH3 mimetic treatment.
Significantly sensitized cells to cell death induced by BH3 mimetics.

Cell Viability Assay[2]

Cell Line: BAX-/- MV4;11 human acute myeloid leukemia (AML) cells
Concentration: 200 nM (combined with serial dilutions of venetoclax, S63845, or venetoclax + S63845)
Incubation Time: 48 h
Result: Significantly sensitized cells to cell death induced by venetoclax, S63845, and the combination of venetoclax + S63845.
Significantly sensitized cells to cell death induced by venetoclax, S63845, and the combination of venetoclax + S63845.
Molecular Weight

618.69

Formula

C30H22N10O2S2
Appearance

Solid

Color

Brown to red

SMILES

CSC1=CC=C(N2C(/C(C3=C(N)C(C#N)=C(N)N=C32)=C4C(N(C5=CC=C(SC)C=C5)C6=NC(N)=C(C#N)C(N)=C6/4)=O)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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WEHI-3773 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WEHI-3773WEHI3773WEHI 3773VDACBcl-2 FamilyApoptosisVoltage-dependent anion channel leukemic cellsacute myeloid leukemiaOCI-AML3 AML cellsMEFsVDAC2BAKBAXBH3 mimeticsMV4;11 AML cellscytochrome cInhibitorinhibitorinhibit

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