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Cat. No.: HY-182349

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Bax activator-2

Bax activator-2 is a pro-apoptotic agent targeting BAX, with an IC₅₀ of 0.30 μM 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, cleavage of caspase-3/9 and PARP, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against a variety of cancer cell lines. Bax activator-2 can be used in research related to acute myeloid leukemia and solid tumors.

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CAS No.: 3034297-25-8
화학식: C₃₀H₂₃N₃O₅
분자량:505.52

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Bax activator-2 Chemical Structure

CAS No.: 3034297-25-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

Bax

Caspase-9

Caspase 3

All Bcl-2 Family Isoforms :

All Caspase Isoforms :

All PARP Isoforms :

In Vitro

Bax activator-2 (compound 27c) (0.024-100 μM) selectively binds to recombinant human BAX with a submicromolar IC₅₀ of 0.30 μmol/L in a competitive fluorescence polarization binding assay^[1].
Bax activator-2 (100 μM; 1-4 h) induces time-dependent oligomerization of recombinant human BAX protein in vitro^[1].
Bax activator-2 (40 μM; 1 h) selectively binds to BAX (but not BAK) in BxPC-3 cells, which is evidenced by the significant increase in the thermal stability of BAX after treatment^[1].
Bax activator-2 induces dose-dependent translocation of recombinant human BAX to mitochondria-mimicking liposomes, and its activity is enhanced when used in combination with BIM SAHB^[1].
Bax activator-2 (40 μM) acts synergistically with the BIM-BH3 peptide to enhance the permeability of ANTS/DPX-loaded liposomes mediated by recombinant human BAX^[1].
Bax activator-2 (serial dilution; 48 h) exhibits BAX-dependent cytotoxicity, with IC₅₀ values in the submicromolar to low micromolar range against hematologic cancer cell lines, while showing low toxicity toward non-cancerous cell lines^[1].
Bax activator-2 (serial dilution; 6 h) induces dose-dependent translocation of BAX to mitochondria and cytochrome c release in THP-1 cells^[1].
Bax activator-2 (2-10 μM; 20 h) induces dose-dependent apoptosis in THP-1 cells, and 62.8% of cells are in the late apoptotic stage after treatment with 10 μM for 20 h^[1].

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

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 μM), U937 (IC₅₀ = 3.14 μM), NB4 (IC₅₀ = 4.52 μM), OCI-AML3 (IC₅₀ = 3.69 μM), MV-4-11 (IC₅₀ = 7.47 μM).
Showed moderate potency in wild-type A549 cells (IC₅₀ = 6.97 μM) but drastically reduced potency in BAX^-/^- A549 cells (IC₅₀ > 80 μM).
Cytotoxicity was low in non-cancerous cell lines: HEK293T (IC₅₀ = 41.55 μM), COS7, STO, THLE-2 (IC₅₀ > 80 μM).

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 (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.).

Chemical Information

CAS No. 3034297-25-8
분자량 505.52
화학식 C₃₀H₂₃N₃O₅
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
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Cai W, et al. Design, Synthesis, and Evaluation of Phenylpyrrole Derivatives as Small-Molecule Activators of BAX. J Med Chem. Published online March 20, 2026. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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Bax activator-2

All Bcl-2 Family Isoforms

All Caspase Isoforms

All PARP Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

Bax activator-2 Related Classifications

HY-182349 Related Classifications