2. Apoptosis
  3. Bcl-2 Family
  4. Bax activator-2

Bax activator-2 (compound 27c) is a pro-apoptotic agent targeting BAX, with an IC50 of 0.30 μmol/L against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, caspase-3/9 cleavage and PARP cleavage, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against various cancer cell lines, shows reduced cytotoxicity in BAX-knockout A549 cells, and has low cytotoxicity against non-cancerous cell lines. Bax activator-2 can be used in studies related to acute myeloid leukemia and solid tumors.

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Bax activator-2

Bax activator-2 Chemical Structure

CAS No. : 3034297-25-8

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Bax activator-2 Related Antibodies

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Description

Bax activator-2 (compound 27c) is a pro-apoptotic agent targeting BAX, with an IC50 of 0.30 μmol/L against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, caspase-3/9 cleavage and PARP cleavage, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against various cancer cell lines, shows reduced cytotoxicity in BAX-knockout A549 cells, and has low cytotoxicity against non-cancerous cell lines. Bax activator-2 can be used in studies related to acute myeloid leukemia and solid tumors[1].

In Vitro

Bax activator-2 (compound 27c) (0.024-100 μmol/L) binds selectively to recombinant human BAX with a submicromolar IC50 of 0.30 μmol/L in a competitive FP binding assay[1].
Bax activator-2 (100 μmol/L; 1-4 h) induces time-dependent oligomerization of recombinant human BAX protein in vitro[1].
Bax activator-2 (40 μmol/L; 1 h) selectively binds to BAX (but not BAK) in BxPC-3 cells, as demonstrated by a significant increase in BAX's thermal stability after treatment[1].
Bax activator-2 induces dose-dependent translocation of recombinant human BAX to mitochondria-mimetic liposomes, with enhanced activity when combined with BIM SAHB[1].
Bax activator-2 (40 μmol/L) synergizes with BIM-BH3 peptide to enhance recombinant human BAX-mediated permeabilization of ANTS/DPX-loaded liposomes[1].
Bax activator-2 (Serial dilutions; 48 h) exhibits BAX-dependent cytotoxicity with submicromolar to low-micromolar IC50 values against hematologic cancer cell lines, and low toxicity against non-cancerous cell lines[1].
Bax activator-2 (Serial dilutions; 6 h) induces dose-dependent translocation of BAX to mitochondria and cytochrome c release in THP-1 cells after treatment[1].
Bax activator-2 (2-10 μmol/L; 20 h) induces dose-dependent apoptosis in THP-1 cells, with 62.8% of cells in late apoptosis after treatment with 10 μmol/L for 20 h[1].

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

Bax activator-2 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: THP-1, MV-4-11, OCI-AML3, U937, NB4, A549, HCT116, SW480, BxPC-3, COS7, HEK293T, STO, THLE-2 cells
Concentration: Serial dilutions
Incubation Time: 48 h total
Result: Exhibited potent cytotoxicity against hematologic cancer cell lines: THP-1 (IC50 = 2.36 μmol/L), U937 (IC50 = 3.14 μmol/L), NB4 (IC50 = 4.52 μmol/L), OCI-AML3 (IC50 = 3.69 μmol/L), MV-4-11 (IC50 = 7.47 μmol/L).
Showed moderate potency in wild-type A549 cells (IC50 = 6.97 μmol/L) but drastically reduced potency in BAX-/- A549 cells (IC50 > 80 μmol/L).
Cytotoxicity was low in non-cancerous cell lines: HEK293T (IC50 = 41.55 μmol/L), COS7, STO, THLE-2 (IC50 > 80 μmol/L).

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: Serial dilutions
Incubation Time: 6 h total
Result: Induced dose-dependent translocation of BAX from the cytosol to mitochondria, accompanied by dose-dependent release of cytochrome c from mitochondria to the cytosol.

Apoptosis Analysis[1]

Cell Line: THP-1 cells
Concentration: 2 μmol/L, 4 μmol/L, 8 μmol/L, 10 μmol/L
Incubation Time: 20 h total
Result: Induced dose-dependent apoptosis in THP-1 cells, with 62.8% of cells undergoing late apoptosis at 10 μmol/L, which was more potent than BTSA1 (36.8% late apoptosis at 10 μmol/L).
In Vivo

Bax activator-2 (compound 27c) (5-10 mg/kg; i.p., i.v.; single dose) exhibits rapid absorption, favorable distribution, moderate bioavailability, relatively short half-life, and rapid clearance in healthy male ICR mice following single i.p. or i.v. administration[1].

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

Animal Model: ICR (male, 25-30 g)[1]
Dosage: 10 mg/kg (i.p.); 5 mg/kg (i.v.)
Administration: i.p.; single dose; i.v.; single dose
Result: Reached Tmax of 0.25 h, Cmax of 3391 ng/mL, AUClast of 6126 h·ng/mL, AUCINF_obs of 6240 h·ng/mL, MRTINF_obs of 1.86 h, bioavailability (F) of 58.60%, and T1/2 of 1.30 h (10 mg/kg i.p.).
Reached Tmax of 0.08 h, AUClast of 5294 h·ng/mL, AUCINF_obs of 5324 h·ng/mL, CL_obs of 16.10 mL/min/kg, MRTINF_obs of 0.84 h, VSS_obs of 791 mL/kg, and T1/2 of 1.24 h (5 mg/kg i.v.).
Molecular Weight

505.52

Formula

C30H23N3O5
CAS No.
SMILES

OC(C1=CC=C(C2=CC(NC3=CC=CC=C3[N+]([O-])=O)=CC=C2OC4=CC=C(C(C)=C4)C5=CC=CC=C5)N1)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Bax activator-2 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:

Bax activator-23034297-25-8Bax activator2Bax activator 2Bcl-2 FamilyICR miceBIM-BH3 peptidehuman liver microsomesA549 cellsacute myelogenous leukemiasolid tumorsmonkey liver microsomesTHP-1 cellsdog liver microsomesBAXInhibitorinhibitorinhibit

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