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 番号: 3034297-25-8
- 分子式: C30H23N3O5
- 分子量:505.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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Bax |
Caspase-9 |
Caspase 3 |
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.
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Cell Line:THP-1, MV-4-11, OCI-AML3, U937, NB4, A549, HCT116, SW480, BxPC-3, COS7, HEK293T, STO, THLE-2 cells
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Concentration:Serial dilutions
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Incubation Time:48 h total
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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).
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Cell Line:THP-1 cells
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Concentration:Serial dilutions
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Incubation Time:6 h total
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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.
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Cell Line:THP-1 cells
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Concentration:2 μmol/L, 4 μmol/L, 8 μmol/L, 10 μmol/L
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Incubation Time:20 h total
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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).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (male, 25-30 g)[1]
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Dosage:10 mg/kg (i.p.); 5 mg/kg (i.v.)
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Administration:i.p.; single dose; i.v.; single dose
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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.).
化学情報
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CAS 番号 3034297-25-8
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分子量 505.52
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分子式 C30H23N3O5
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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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献
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Bax activator-2 関連分類
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